DGIdb - PTGS2 Gene Record

PTGS2 5743 Druggable GenomeDrug Resistance

Alternate Names:

5743
PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE 2
PTGS2
COX-2
COX2
GRIPGHS
PGG/HS
PGHS-2
PHS-2
hCox-2
600262
9605
ENSG00000073756
OTTHUMG00000035473
BE0000262
P35354
PA293
PGH2_HUMAN
PROSTAGLANDIN G/H SYNTHASE 2 PRECURSOR (EC 1.14.99.1) (CYCLOOXYGENASE- 2) (COX-2) (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE 2) (PROSTAGLANDIN H2 SYNTHASE 2) (PGH SYNTHASE 2) (PGHS-2) (PHS II). [SOURCE:UNIPROT/SWISSPROT;ACC:P35354]
Prostaglandin G/H synthase 2
Cyclooxygenase-2
PHS II
Prostaglandin H2 synthase 2
PGH synthase 2
4659
T66665
1376

Gene Info:

Target Class	Enzymes
Target Subclass	EC:1.14.99.1
Target Subclass	1.14.99.1
Target Main Class	Enzymes
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Interpro Type	Family
Interpro Acc	IPR002007
Interpro Name	Haem peroxidase, animal
Interpro Short Name	Haem_peroxidase_animal
Uniprot Evidence	1: Evidence at protein level
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	Cyclooxygenase
GuideToPharmacology Gene Category ID	269

(15 More Sources)

Gene Categories: Category Details

TUMOR SUPPRESSOR
DRUG RESISTANCE
PROTEASE
DRUGGABLE GENOME
ENZYME

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Mazaleuskaya LL et al., 2015, PharmGKB summary: ibuprofen pathways., Pharmacogenet Genomics
Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med
Lee YS et al., 2006, Genetically mediated interindividual variation in analgesic responses to cyclooxygenase inhibitory drugs., Clin Pharmacol Ther
Ouellet et al., 2004, Detergents profoundly affect inhibitor potencies against both cyclo-oxygenase isoforms., Biochem. J.
Gallego-Sandín et al., 2004, Effect of ibuprofen on cyclooxygenase and nitric oxide synthase of gastric mucosa: correlation with endoscopic lesions and adverse reactions., Dig. Dis. Sci.
Sánchez-Fidalgo et al., 2004, Angiogenesis, cell proliferation and apoptosis in gastric ulcer healing. Effect of a selective cox-2 inhibitor., Eur. J. Pharmacol.
Chavez et al., 2003, Valdecoxib: a review., Clin Ther
Murphey et al., 2004, Quantification of the major urinary metabolite of PGE2 by a liquid chromatographic/mass spectrometric assay: determination of cyclooxygenase-specific PGE2 synthesis in healthy humans and those with lung cancer., Anal. Biochem.
Gross et al., 1999, Natriuretic response to increased pressure is preserved with COX-2 inhibitors., Hypertension
Blanco et al., 1999, Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes., J. Rheumatol.
Tegeder et al., 1999, Comparison of inhibitory effects of meloxicam and diclofenac on human thromboxane biosynthesis after single doses and at steady state., Clin. Pharmacol. Ther.
Panara et al., 1999, Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects., J. Pharmacol. Exp. Ther.
Poulsen Nautrup et al., 1999, [Pharmacodynamic and pharmacokinetic aspects of the non-inflammatory non-steroidal agent meloxicam in dogs]., DTW. Dtsch. Tierarztl. Wochenschr.
Gates BJ et al., 2005, Meloxicam: a reappraisal of pharmacokinetics, efficacy and safety., Expert Opin Pharmacother
Bekker A et al., 2018, Meloxicam in the management of post-operative pain: Narrative review., J Anaesthesiol Clin Pharmacol
Arifah et al., 2002, Pharmacodynamics and pharmacokinetics of phenylbutazone in calves., J. Vet. Pharmacol. Ther.
Beretta et al., 2005, COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis., Pharmacol. Res.
Takada et al., 2004, Nonsteroidal anti-inflammatory agents differ in their ability to suppress NF-kappaB activation, inhibition of expression of cyclooxygenase-2 and cyclin D1, and abrogation of tumor cell proliferation., Oncogene
Gamache et al., 2000, Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy., Inflammation
Almansa et al., 2004, New water-soluble sulfonylphosphoramidic acid derivatives of the COX-2 selective inhibitor cimicoxib. A novel approach to sulfonamide prodrugs., J. Med. Chem.
Rainsford et al., 2006, Nimesulide -- a multifactorial approach to inflammation and pain: scientific and clinical consensus., Curr Med Res Opin
Simon, 2004, Adverse respiratory reactions to aspirin and nonsteroidal anti-inflammatory drugs., Curr Allergy Asthma Rep
Brzozowski et al., 2006, Interaction of nonsteroidal anti-inflammatory drugs (NSAID) with Helicobacter pylori in the stomach of humans and experimental animals., J. Physiol. Pharmacol.
Shen et al., 2006, Genetic polymorphisms in the cyclooxygenase-2 gene, use of nonsteroidal anti-inflammatory drugs, and breast cancer risk., Breast Cancer Res.
Wang et al., 2006, [Effects of nonsteroidal anti-inflammatory drug celecoxib on expression of cyclooxygenase-2 (COX-2) in ovarian carcinoma cell]., Sichuan Da Xue Xue Bao Yi Xue Ban
Nakano et al., 2007, Interaction between cyclooxygenase (COX)-1- and COX-2-products modulates COX-2 expression in the late phase of acute inflammation., Eur. J. Pharmacol.
McCann et al., 2004, In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in dogs with experimentally induced synovitis., Am. J. Vet. Res.
Yamazaki et al., 2002, Nonsteroidal anti-inflammatory drugs induce apoptosis in association with activation of peroxisome proliferator-activated receptor gamma in rheumatoid synovial cells., J. Pharmacol. Exp. Ther.
Zhou et al., 2009, Design, synthesis, and in-vivo evaluation of 4,5-diaryloxazole as novel nonsteroidal anti-inflammatory drug., Biol. Pharm. Bull.
Kawai et al., 1998, Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells., Eur. J. Pharmacol.
Yood et al., 2006, The impact of NSAID or COX-2 inhibitor use on the initiation of antihypertensive therapy., Pharmacoepidemiol Drug Saf
Kawai, 1998, Cyclooxygenase selectivity and the risk of gastro-intestinal complications of various non-steroidal anti-inflammatory drugs: a clinical consideration., Inflamm. Res.
Ottonello et al., 2009, Delayed apoptosis of human monocytes exposed to immune complexes is reversed by oxaprozin: role of the Akt/IkappaB kinase/nuclear factor kappaB pathway., Br. J. Pharmacol.
Yim et al., 2005, Cyclooxygenase-2 inhibits novel ginseng metabolite-mediated apoptosis., Cancer Res.
Kim et al., 2007, Transgenic Panax ginseng inhibits the production of TNF-alpha, IL-6, and IL-8 as well as COX-2 expression in human mast cells., Am. J. Chin. Med.
Seo et al., 2005, Effect of a fermented ginseng extract, BST204, on the expression of cyclooxygenase-2 in murine macrophages., Int. Immunopharmacol.
Sommerauer et al., 2001, Ketoprofen-induced cyclooxygenase inhibition in renal medulla and platelets of rats treated with caffeine., Pharmacology
Kay-Mugford et al., 2000, In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs., Am. J. Vet. Res.
Zúñiga et al., 2003, Effects of steroidal and non steroidal drugs on the neovascularization response induced by tumoral TA3 supernatant on CAM from chick embryo., Biol. Res.
Wilson et al., 2004, Determination of expression of cyclooxygenase-1 and -2 isozymes in canine tissues and their differential sensitivity to nonsteroidal anti-inflammatory drugs., Am. J. Vet. Res.
Levoin et al., 2002, Synthesis and biological testing of Acyl-CoA-ketoprofen conjugates as selective irreversible inhibitors of COX-2., Bioorg. Med. Chem.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Llorens et al., 2002, Differential binding mode of diverse cyclooxygenase inhibitors., J. Mol. Graph. Model.
Warner et al., 1999, Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis., Proc. Natl. Acad. Sci. U.S.A.
Fackovcova et al., 2000, Renal damage induced by the treatment with non-opioid analgesics--theoretical assumption or clinical significance., Bratisl Lek Listy
Veiga et al., 2004, Prevention by celecoxib of secondary hyperalgesia induced by formalin in rats., Life Sci.
Bugajski et al., 2001, Involvement of constitutive (COX-1) and inducible cyclooxygenase (COX-2) in the adrenergic-induced ACTH and corticosterone secretion., J. Physiol. Pharmacol.
Raju et al., 2002, Differential modulation of transforming growth factor-betas and cyclooxygenases in the platelet lysates of male F344 rats by dietary lipids and piroxicam., Mol. Cell. Biochem.
Giuliano et al., 1999, Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs., Br. J. Pharmacol.
Yip-Schneider et al., 2000, Cyclooxygenase-2 expression in human pancreatic adenocarcinomas., Carcinogenesis
Fosslien, 2000, Biochemistry of cyclooxygenase (COX)-2 inhibitors and molecular pathology of COX-2 in neoplasia., Crit Rev Clin Lab Sci
Taylor et al., 2000, Sulindac sulfone inhibits K-ras-dependent cyclooxygenase-2 expression in human colon cancer cells., Cancer Res.
Molina et al., 1999, Increased cyclooxygenase-2 expression in human pancreatic carcinomas and cell lines: growth inhibition by nonsteroidal anti-inflammatory drugs., Cancer Res.
Wiedmann et al., 2005, Molecularly targeted therapy for gastrointestinal cancer., Curr Cancer Drug Targets
Hada et al., 2004, [A case report of metastatic pancreatic cancer that responded remarkably to the combination of thalidomide, celecoxib and irinotecan]., Gan To Kagaku Ryoho
Payvandi et al., 2004, Immunomodulatory drugs inhibit expression of cyclooxygenase-2 from TNF-alpha, IL-1beta, and LPS-stimulated human PBMC in a partially IL-10-dependent manner., Cell. Immunol.
Du et al., 2005, Thalidomide inhibits growth of tumors through COX-2 degradation independent of antiangiogenesis., Vascul. Pharmacol.
Horrobin, 2003, A low toxicity maintenance regime, using eicosapentaenoic acid and readily available drugs, for mantle cell lymphoma and other malignancies with excess cyclin D1 levels., Med. Hypotheses
Kim et al., 2011, Thalidomide: the tragedy of birth defects and the effective treatment of disease., Toxicol. Sci.
Lee et al., 2007, Acetaminophen selectively suppresses peripheral prostaglandin E2 release and increases COX-2 gene expression in a clinical model of acute inflammation., Pain
Hinz et al., 2008, Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man., FASEB J.
Weinheimer et al., 2007, Resistance exercise and cyclooxygenase (COX) expression in human skeletal muscle: implications for COX-inhibiting drugs and protein synthesis., Am. J. Physiol. Regul. Integr. Comp. Physiol.
Koeberle A et al., 2014, SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase., J Med Chem
Stolfi et al., 2008, Cyclooxygenase-2-dependent and -independent inhibition of proliferation of colon cancer cells by 5-aminosalicylic acid., Biochem. Pharmacol.
Wiggins et al., 2009, Balsalazide: a novel 5-aminosalicylate prodrug for the treatment of active ulcerative colitis., Expert Opin Drug Metab Toxicol
Allgayer, 2003, Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease., Aliment. Pharmacol. Ther.
Das, 2005, Can COX-2 inhibitor-induced increase in cardiovascular disease risk be modified by essential fatty acids?, J Assoc Physicians India
Thuresson et al., 2001, Mutational and X-ray crystallographic analysis of the interaction of dihomo-gamma -linolenic acid with prostaglandin endoperoxide H synthases., J. Biol. Chem.
Levin et al., 2002, Differential metabolism of dihomo-gamma-linolenic acid and arachidonic acid by cyclo-oxygenase-1 and cyclo-oxygenase-2: implications for cellular synthesis of prostaglandin E1 and prostaglandin E2., Biochem. J.
Das, 2005, COX-2 inhibitors and metabolism of essential fatty acids., Med. Sci. Monit.
Chen et al., 2001, Tumor invasiveness and liver metastasis of colon cancer cells correlated with cyclooxygenase-2 (COX-2) expression and inhibited by a COX-2-selective inhibitor, etodolac., Int. J. Cancer
Svendsen et al., 2000, A comparison of the effects of etodolac and ibuprofen on renal haemodynamics, tubular function, renin, vasopressin and urinary excretion of albumin and alpha-glutathione-S-transferase in healthy subjects: a placebo-controlled cross-over study., Eur. J. Clin. Pharmacol.
Chen et al., 2003, Colon cancer cells with high invasive potential are susceptible to induction of apoptosis by a selective COX-2 inhibitor., Cancer Sci.
Kusuhara et al., 1999, Reactive oxygen species are involved in the apoptosis induced by nonsteroidal anti-inflammatory drugs in cultured gastric cells., Eur. J. Pharmacol.
Capasso et al., 1997, Arachidonic acid and its metabolites are involved in the expression of morphine dependence in guinea-pig isolated ileum., Eur. J. Pharmacol.
Burdan et al., 2004, Gastrointestinal and hepatic toxicity of selective and non-selective cyclooxygenase-2 inhibitors in pregnant and non-pregnant rats., Pharmacol. Res.
Kirkova et al., 2007, In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs., Auton Autacoid Pharmacol
Kennedy et al., 2003, Prostaglandin levels in seminal plasma and sperm extracts of the domestic turkey, and the effects of cyclooxygenase inhibitors on sperm mobility., Reprod. Biol. Endocrinol.
Capasso, 1999, Further studies on the involvement of the arachidonic acid cascade in the acute dependence produced by mu, kappa and delta opioid agonists in isolated tissues., Neuropharmacology
Smith et al., 2000, Arachidonic acid and nonsteroidal anti-inflammatory drugs induce conformational changes in the human prostaglandin endoperoxide H2 synthase-2 (cyclooxygenase-2)., J. Biol. Chem.
Bayly et al., 1999, Structure-based design of COX-2 selectivity into flurbiprofen., Bioorg. Med. Chem. Lett.
Hinz et al., 2001, Flurbiprofen enantiomers inhibit inducible nitric oxide synthase expression in RAW 264.7 macrophages., Pharm. Res.
Basselin et al., 2007, Flurbiprofen, a cyclooxygenase inhibitor, reduces the brain arachidonic acid signal in response to the cholinergic muscarinic agonist, arecoline, in awake rats., Neurochem. Res.
van Haeringen et al., 2000, Constitutive cyclooxygenase-1 and induced cyclooxygenase-2 in isolated human iris inhibited by S(+) flurbiprofen., J Ocul Pharmacol Ther
Nivsarkar et al., Cyclooxygenase inhibitors: a novel direction for Alzheimer's management., Pharmacol Rep
Hewett et al., 2000, Cyclooxygenase-2 contributes to N-methyl-D-aspartate-mediated neuronal cell death in primary cortical cell culture., J. Pharmacol. Exp. Ther.
Kim JG et al., 2009, Prostaglandin synthase 2/cyclooxygenase 2 (PTGS2/COX2) 8473T>C polymorphism associated with prognosis for patients with colorectal cancer treated with capecitabine and oxaliplatin., Cancer Chemother Pharmacol
Lu et al., 2002, Cyclooxygenase-2 inhibitor celecoxib inhibits promotion of mammary tumorigenesis in rats fed a high fat diet rich in n-6 polyunsaturated fatty acids., Cancer Lett.
Sigthorsson et al., 2002, COX-1 and 2, intestinal integrity, and pathogenesis of nonsteroidal anti-inflammatory drug enteropathy in mice., Gastroenterology
Scheiman, 2002, Outcomes studies of the gastrointestinal safety of cyclooxygenase-2 inhibitors., Cleve Clin J Med
Reddy et al., 2002, Novel approaches for colon cancer prevention by cyclooxygenase-2 inhibitors., J. Environ. Pathol. Toxicol. Oncol.
Ahmad et al., 2002, Renal failure associated with the use of celecoxib and rofecoxib., Drug Saf
Gong L et al., 2012, Celecoxib pathways: pharmacokinetics and pharmacodynamics., Pharmacogenet Genomics
Narlawar et al., 2006, Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators., J. Med. Chem.
Brideau et al., 2001, In vitro effects of cyclooxygenase inhibitors in whole blood of horses, dogs, and cats., Am. J. Vet. Res.
Distrutti et al., 2006, 5-Amino-2-hydroxybenzoic acid 4-(5-thioxo-5H-[1,2]dithiol-3yl)-phenyl ester (ATB-429), a hydrogen sulfide-releasing derivative of mesalamine, exerts antinociceptive effects in a model of postinflammatory hypersensitivity., J. Pharmacol. Exp. Ther.
Mifflin et al., 2004, Aspirin-mediated COX-2 transcript stabilization via sustained p38 activation in human intestinal myofibroblasts., Mol. Pharmacol.
Generini et al., Therapy of spondylarthropathy in inflammatory bowel disease., Clin. Exp. Rheumatol.
Pruzanski et al., 1997, Inhibition of extracellular release of proinflammatory secretory phospholipase A2 (sPLA2) by sulfasalazine: a novel mechanism of anti-inflammatory activity., Biochem. Pharmacol.
Cipolla et al., 2002, Nonsteroidal anti-inflammatory drugs and inflammatory bowel disease: current perspectives., Pharmacol. Res.
FitzGerald, 2007, COX-2 in play at the AHA and the FDA., Trends Pharmacol. Sci.
Yuan et al., 2007, Global gastrointestinal safety profile of etoricoxib and lumiracoxib., Curr. Pharm. Des.
Capone et al., 2007, Pharmacodynamic of cyclooxygenase inhibitors in humans., Prostaglandins Other Lipid Mediat.
Smith et al., 1994, Interactions of PGH synthase isozymes-1 and -2 with NSAIDs., Ann. N. Y. Acad. Sci.
Traupe et al., 2002, Obesity increases prostanoid-mediated vasoconstriction and vascular thromboxane receptor gene expression., J. Hypertens.
Narsinghani et al., 2006, QSAR analysis of meclofenamic acid analogues as selective COX-2 inhibitors., Bioorg. Med. Chem. Lett.
Kalgutkar et al., 2000, Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors., Proc. Natl. Acad. Sci. U.S.A.
Moore et al., 2001, Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice., J Am Dent Assoc
Young et al., 1996, Human whole blood assays for inhibition of prostaglandin G/H synthases-1 and -2 using A23187 and lipopolysaccharide stimulation of thromboxane B2 production., Inflamm. Res.
Jeske, 1999, COX-2 inhibitors and dental pain control., J Gt Houst Dent Soc
Mao et al., 2001, Rational design of diflunisal analogues with reduced affinity for human serum albumin., J. Am. Chem. Soc.
Cappon et al., 2003, Relationship between cyclooxygenase 1 and 2 selective inhibitors and fetal development when administered to rats and rabbits during the sensitive periods for heart development and midline closure., Birth Defects Res. B Dev. Reprod. Toxicol.
Vidal et al., 2007, Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis., J. Pharmacol. Exp. Ther.
Yeh JR et al., 2009, Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation., Nat Chem Biol
Su B et al., 2006, Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition., J Med Chem
Zhang L et al., 2011, Effects of β-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro., Bioorg Med Chem
Park JB, 2014, Synthesis and characterization of norbelladine, a precursor of Amaryllidaceae alkaloid, as an anti-inflammatory/anti-COX compound., Bioorg Med Chem Lett
Poggi et al., 2006, Pharmacodynamics, chiral pharmacokinetics, and pharmacokinetic-pharmacodynamic modeling of fenoprofen in patients with diabetes mellitus., J Clin Pharmacol
Tacconelli et al., 2002, The biochemical selectivity of novel COX-2 inhibitors in whole blood assays of COX-isozyme activity., Curr Med Res Opin
Jain, 2000, Evaluation of intravenous parecoxib for the relief of acute post-surgical pain., Expert Opin Investig Drugs
Yuan et al., 2002, Disposition of a specific cyclooxygenase-2 inhibitor, valdecoxib, in human., Drug Metab. Dispos.
Gierse et al., 2005, Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity., J. Pharmacol. Exp. Ther.
Talley et al., 2000, 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2., J. Med. Chem.
Hood et al., 2003, Characterization of celecoxib and valdecoxib binding to cyclooxygenase., Mol. Pharmacol.
Onnis V et al., 2010, Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors., J Med Chem
Sanchez-Matienzo et al., 2006, Hepatic disorders in patients treated with COX-2 selective inhibitors or nonselective NSAIDs: a case/noncase analysis of spontaneous reports., Clin Ther
Chitturi et al., 2002, Hepatotoxicity of commonly used drugs: nonsteroidal anti-inflammatory drugs, antihypertensives, antidiabetic agents, anticonvulsants, lipid-lowering agents, psychotropic drugs., Semin. Liver Dis.
Waterbury et al., 2006, Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium., Curr Med Res Opin
Yamada et al., 1997, Prostaglandin E2 production dependent upon cyclooxygenase-1 and cyclooxygenase-2 and its contradictory modulation by auranofin in rat peritoneal macrophages., J. Pharmacol. Exp. Ther.
Yilmaz et al., 2005, The use and safety profile of non-steroidal antiinflammatory drugs among Turkish patients with osteoarthritis., Turk J Gastroenterol
Kothekar et al., Recognition of cyclooxygenase-2 (COX-2) active site by NSAIDs: a computer modelling study., Indian J. Biochem. Biophys.
Ozgocmen et al., 2005, In vivo effect of celecoxib and tenoxicam on oxidant/ anti-oxidant status of patients with knee osteoarthritis., Ann. Clin. Lab. Sci.
Galvão et al., 2005, Tenoxicam exerts a neuroprotective action after cerebral ischemia in rats., Neurochem. Res.
Ben-Chetrit et al., 2005, The effects of colchicine and hydroxychloroquine on the cyclo-oxygenases COX-1 and COX-2., Rheumatol. Int.
Wang H et al., 1999, Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries., J Nat Prod
Brandt et al., 1990, Effects of tiaprofenic acid on the concentration and metabolism of proteoglycans in normal and degenerating canine articular cartilage., J Clin Pharmacol
Elliott et al., 1995, A nitric oxide-releasing nonsteroidal anti-inflammatory drug accelerates gastric ulcer healing in rats., Gastroenterology
Roy et al., 2001, Distal bowel selectivity in the chemoprevention of experimental colon carcinogenesis by the non-steroidal anti-inflammatory drug nabumetone., Int. J. Cancer
van Kraaij et al., 2002, A comparison of the effects of nabumetone vs meloxicam on serum thromboxane B2 and platelet function in healthy volunteers., Br J Clin Pharmacol
Hedner et al., 2004, Nabumetone: therapeutic use and safety profile in the management of osteoarthritis and rheumatoid arthritis., Drugs
Blomme et al., 2003, Selective cyclooxygenase-2 inhibition does not affect the healing of cutaneous full-thickness incisional wounds in SKH-1 mice., Br. J. Dermatol.
Beubler, 2003, [Pharmacology of cyclooxygenase 2 inhibition]., Wien Med Wochenschr
Kirchheiner et al., 2003, Pharmacokinetics of diclofenac and inhibition of cyclooxygenases 1 and 2: no relationship to the CYP2C9 genetic polymorphism in humans., Br J Clin Pharmacol
Rowlinson et al., 2003, A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385., J. Biol. Chem.
Esser et al., 2005, Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2., Br. J. Pharmacol.
Atherton et al., 2004, Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2 selective inhibitor: An integrated study., Clin. Gastroenterol. Hepatol.
Capone et al., Clinical pharmacology of selective COX-2 inhibitors., Int J Immunopathol Pharmacol
Kalbag et al., 2004, No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor., Pharmacol. Res.
Tacconelli et al., 2004, Clinical pharmacology of novel selective COX-2 inhibitors., Curr. Pharm. Des.
Zeldis et al., 2003, Potential new therapeutics for Waldenstrom's macroglobulinemia., Semin. Oncol.
Brune et al., Pharmacokinetic and pharmacodynamic aspects of the ideal COX-2 inhibitor: a pharmacologist's perspective., Clin. Exp. Rheumatol.
Ashok et al., 2011, Selective cyclooxygenase-2 (COX-2) inhibitors and breast cancer risk., Breast
Langman et al., 1999, Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs., JAMA
Malmstrom et al., 1999, Comparison of rofecoxib and celecoxib, two cyclooxygenase-2 inhibitors, in postoperative dental pain: a randomized, placebo- and active-comparator-controlled clinical trial., Clin Ther
Chakraborti et al., 2010, Progress in COX-2 inhibitors: a journey so far., Curr. Med. Chem.
Pascucci, 1999, COX-2-specific inhibition: implications for clinical practice., J Am Osteopath Assoc
Matheson et al., 2001, Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis., Drugs
Hawkey et al., 2000, Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: a randomized, double-blind, placebo-controlled trial. The Rofecoxib Osteoarthritis Endoscopy Multinational Study Group., Arthritis Rheum.
Baron et al., 2008, Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial., Lancet
Ehrich et al., 1999, Effect of specific COX-2 inhibition in osteoarthritis of the knee: a 6 week double blind, placebo controlled pilot study of rofecoxib. Rofecoxib Osteoarthritis Pilot Study Group., J. Rheumatol.
Christ AN et al., 2010, Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases., J Med Chem
Hanna MM, 2012, New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies., Eur J Med Chem
Pergola C et al., 2014, Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase., J Med Chem
Armstrong et al., 2005, Suppression of experimental aortic aneurysms: comparison of inducible nitric oxide synthase and cyclooxygenase inhibitors., Ann Vasc Surg
Jerde et al., 2005, Celecoxib inhibits ureteral contractility and prostanoid release., Urology
Zhang et al., 2004, [Proliferation inhibition effect of indomethacin on CML cells associated with down-regulation of phosphorylated STAT1/STAT5 and inhibition of COX-2 expression]., Zhonghua Xue Ye Xue Za Zhi
Yokota et al., 2005, Rofecoxib produces intestinal but not gastric damage in the presence of a low dose of indomethacin in rats., J. Pharmacol. Exp. Ther.
Pilane et al., 2005, Nitric oxide stimulated vascular smooth muscle cells undergo apoptosis induced in part by arachidonic acid derived eicosanoids., J. Cell. Physiol.
Ashraf Z et al., 2016, Synthesis, Bioevaluation and Molecular Dynamic Simulation Studies of Dexibuprofen-Antioxidant Mutual Prodrugs., Int J Mol Sci
Chan et al., 2007, Aspirin and the risk of colorectal cancer in relation to the expression of COX-2., N. Engl. J. Med.
Ma et al., 2003, Cyclooxygenase 2 in infiltrating inflammatory cells in injured nerve is universally up-regulated following various types of peripheral nerve injury., Neuroscience
Höcherl et al., 2002, Role of prostanoids in regulation of the renin-angiotensin-aldosterone system by salt intake., Am. J. Physiol. Renal Physiol.
Padi et al., 2004, Pharmacological profile of parecoxib: a novel, potent injectable selective cyclooxygenase-2 inhibitor., Eur. J. Pharmacol.
Blais et al., 2002, In altering the release of glucocorticoids, ketorolac exacerbates the effects of systemic immune stimuli on expression of proinflammatory genes in the brain., Endocrinology
Ma et al., 2003, Intraplantar injection of a cyclooxygenase inhibitor ketorolac reduces immunoreactivities of substance P, calcitonin gene-related peptide, and dynorphin in the dorsal horn of rats with nerve injury or inflammation., Neuroscience
Dionne et al., Analgesia and COX-2 inhibition., Clin. Exp. Rheumatol.
Albertini et al., 2007, COX-2 mRNA expression decreases in the subplantar muscle of rat paw subjected to carrageenan-induced inflammation after low level laser therapy., Inflamm. Res.
Kumar et al., 2007, Cyclooxygenase inhibition attenuates 3-nitropropionic acid-induced neurotoxicity in rats: possible antioxidant mechanisms., Fundam Clin Pharmacol
Dhir et al., 2007, Neuroprotective effect of nimesulide, a preferential COX-2 inhibitor, against pentylenetetrazol (PTZ)-induced chemical kindling and associated biochemical parameters in mice., Seizure
White, 2007, Cardiovascular effects of the selective cyclooxygenase-2 inhibitors., Subcell. Biochem.
Hassan-Alin et al., 2005, Lack of Pharmacokinetic Interaction between Esomeprazole and the Nonsteroidal Anti-Inflammatory Drugs Naproxen and Rofecoxib in Healthy Subjects., Clin Drug Investig
Brutzkus JC et al., 2020, Naproxen,
Schaefer et al., 2003, Interaction of rofecoxib and celecoxib with warfarin., Am J Health Syst Pharm
Motsko et al., 2006, Temporal relationship between use of NSAIDs, including selective COX-2 inhibitors, and cardiovascular risk., Drug Saf
Josephs et al., 1999, Products of cyclooxygenase-2 catalysis regulate postoperative bowel motility., J. Surg. Res.
Stichtenoth et al., 1998, [New non-steroidal anti-rheumatic drugs: selective inhibitors of inducible cyclooxygenase]., Med. Klin. (Munich)
Talley et al., 2000, N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration., J. Med. Chem.
Bhat et al., 2007, Interaction between inhibitors of inducible nitric oxide synthase and cyclooxygenase in adjuvant-induced arthritis in female albino rats: an isobolographic study., Eur. J. Pharmacol.
Bhat et al., 2005, Interaction between inhibitors of inducible nitric oxide synthase and cyclooxygenase in Brewer's yeast induced pyrexia in mice: an isobolographic study., Eur. J. Pharmacol.
Cryer et al., 1998, Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs., Am. J. Med.
Gierse et al., 1995, Expression and selective inhibition of the constitutive and inducible forms of human cyclo-oxygenase., Biochem. J.
Walton et al., 1999, Inhibition of prostaglandin E2 synthesis in abdominal aortic aneurysms: implications for smooth muscle cell viability, inflammatory processes, and the expansion of abdominal aortic aneurysms., Circulation
Bianchi et al., 2002, Effects of lornoxicam, piroxicam, and meloxicam in a model of thermal hindpaw hyperalgesia induced by formalin injection in rat tail., Pharmacol. Res.
Berg et al., 1999, The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro., Inflamm. Res.
Renner et al., 2010, Pain control in first-trimester surgical abortion: a systematic review of randomized controlled trials., Contraception
Rose et al., 2004, Comparison of Lornoxicam and Rofecoxib in Patients with Activated Osteoarthritis (COLOR Study)., Clin Drug Investig
Cui PH et al., 2012, Antiproliferative and antimigratory actions of synthetic long chain n-3 monounsaturated fatty acids in breast cancer cells that overexpress cyclooxygenase-2., J Med Chem
Lee et al., 2003, Differential modulation of Toll-like receptors by fatty acids: preferential inhibition by n-3 polyunsaturated fatty acids., J. Lipid Res.
Ait-Said et al., 2003, Inhibition by eicosapentaenoic acid of IL-1beta-induced PGHS-2 expression in human microvascular endothelial cells: involvement of lipoxygenase-derived metabolites and p38 MAPK pathway., Biochim. Biophys. Acta
Machida et al., 2005, Docosahexaenoic acid enhances cyclooxygenase-2 induction by facilitating p44/42, but not p38, mitogen-activated protein kinase activation in rat vascular smooth muscle cells., J. Pharmacol. Sci.
Chêne et al., 2007, n-3 and n-6 polyunsaturated fatty acids induce the expression of COX-2 via PPARgamma activation in human keratinocyte HaCaT cells., Biochim. Biophys. Acta
Vecchio et al., 2010, Structural basis of fatty acid substrate binding to cyclooxygenase-2., J. Biol. Chem.
Cantarella et al., 2005, Adrenomedullin modulates COX-2 and HGF expression in reserpine-injuried gastric mucosa in the rat., Eur. J. Pharmacol.
Jabeen et al., 2005, Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution., Acta Crystallogr. D Biol. Crystallogr.
Diao et al., 2007, Rat ovulation, implantation and decidualization are severely compromised by COX-2 inhibitors., Front. Biosci.
Alpert et al., 2007, Selective cyclooxygenase-2 inhibitors stimulate glucose transport in L6 myotubes in a protein kinase Cdelta-dependent manner., Biochem. Pharmacol.
Robida et al., 2000, Cyclosporin A selectively inhibits mitogen-induced cyclooxygenase-2 gene transcription in vascular smooth muscle cells., Mol. Pharmacol.
Ferguson et al., 2007, Immunomodulatory drug CC-4047 is a cell-type and stimulus-selective transcriptional inhibitor of cyclooxygenase 2., J. Clin. Immunol.
Ringbom T et al., 1998, Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis., J Nat Prod
Oviedo et al., Raloxifene increases the capacity of serum to promote prostacyclin release in human endothelial cells: implication of COX-1 and COX-2., Menopause
Thomas GM et al., 1975, Simultaneous pharmacokinetics of alclofenace in plasma and synovial fluid in patients with rheumatoid arthritis., Curr Med Res Opin
Esteve J et al., 1988, Pharmacological profile of droxicam., Gen Pharmacol
Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
Tokola RA et al., 1984, Effects of migraine attack and metoclopramide on the absorption of tolfenamic acid., Br J Clin Pharmacol
Lees P et al., 1998, Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation., Vet J
McKellar QA et al., 1994, Pharmacodynamics of tolfenamic acid in dogs. Evaluation of dose response relationships., Eur J Pharmacol
Brogden RN et al., 1975, Bufexamac: a review of its pharmacological properties and therapeutic efficacy in inflammatory dermatoses., Drugs
Visioli F et al., 2012, Molecular targets of omega 3 and conjugated linoleic Fatty acids - "micromanaging" cellular response., Front Physiol
Legrand E, 2004, Aceclofenac in the management of inflammatory pain., Expert Opin Pharmacother
Chae et al., 2004, Salicylate regulates COX-2 expression through ERK and subsequent NF-kappaB activation in osteoblasts., Immunopharmacol Immunotoxicol
Wu, 2003, Aspirin and other cyclooxygenase inhibitors: new therapeutic insights., Semin Vasc Med
Elvira et al., 2001, Incorporation of salicylic acid derivatives to hydrophilic copolymer systems with biomedical applications., J Mater Sci Mater Med
Graham et al., 2003, Mechanisms of action of paracetamol and related analgesics., Inflammopharmacology
Fiebich et al., 2004, Effects of an ethanolic salix extract on the release of selected inflammatory mediators in vitro., Phytomedicine
Riendeau D et al., 2004, Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2., Bioorg Med Chem Lett
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Levy G, 1980, Clinical pharmacokinetics of salicylates: a re-assessment., Br J Clin Pharmacol
Ouellet et al., 1995, Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms., Biochem. J.

RESVERATROL PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

PHENYLBUTAZONE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

Publications:

Arifah et al., 2002, Pharmacodynamics and pharmacokinetics of phenylbutazone in calves., J. Vet. Pharmacol. Ther.

Beretta et al., 2005, COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis., Pharmacol. Res.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

NEPAFENAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name -

Publications:

Gamache et al., 2000, Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy., Inflammation

KETOPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of COX2 in human whole blood.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

Sommerauer et al., 2001, Ketoprofen-induced cyclooxygenase inhibition in renal medulla and platelets of rats treated with caffeine., Pharmacology

Kay-Mugford et al., 2000, In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs., Am. J. Vet. Res.

Zúñiga et al., 2003, Effects of steroidal and non steroidal drugs on the neovascularization response induced by tumoral TA3 supernatant on CAM from chick embryo., Biol. Res.

SUPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Llorens et al., 2002, Differential binding mode of diverse cyclooxygenase inhibitors., J. Mol. Graph. Model.

SULINDAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Giuliano et al., 1999, Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs., Br. J. Pharmacol.

Yip-Schneider et al., 2000, Cyclooxygenase-2 expression in human pancreatic adenocarcinomas., Carcinogenesis

Fosslien, 2000, Biochemistry of cyclooxygenase (COX)-2 inhibitors and molecular pathology of COX-2 in neoplasia., Crit Rev Clin Lab Sci

ACETAMINOPHEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Lee et al., 2007, Acetaminophen selectively suppresses peripheral prostaglandin E2 release and increases COX-2 gene expression in a clinical model of acute inflammation., Pain

Hinz et al., 2008, Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man., FASEB J.

Weinheimer et al., 2007, Resistance exercise and cyclooxygenase (COX) expression in human skeletal muscle: implications for COX-inhibiting drugs and protein synthesis., Am. J. Physiol. Regul. Integr. Comp. Physiol.

ETODOLAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Details of the Assay for Interaction Measured as LPS-induced PGE<sub>2</sub> production in COX-1-inhibited human monocytes.

Specific Action of the Ligand Inhibition

Publications:

Chen et al., 2001, Tumor invasiveness and liver metastasis of colon cancer cells correlated with cyclooxygenase-2 (COX-2) expression and inhibited by a COX-2-selective inhibitor, etodolac., Int. J. Cancer

Wilson et al., 2004, Determination of expression of cyclooxygenase-1 and -2 isozymes in canine tissues and their differential sensitivity to nonsteroidal anti-inflammatory drugs., Am. J. Vet. Res.

Svendsen et al., 2000, A comparison of the effects of etodolac and ibuprofen on renal haemodynamics, tubular function, renin, vasopressin and urinary excretion of albumin and alpha-glutathione-S-transferase in healthy subjects: a placebo-controlled cross-over study., Eur. J. Clin. Pharmacol.

CARPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

Publications:

Narlawar et al., 2006, Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators., J. Med. Chem.

Beretta et al., 2005, COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis., Pharmacol. Res.

Brideau et al., 2001, In vitro effects of cyclooxygenase inhibitors in whole blood of horses, dogs, and cats., Am. J. Vet. Res.

DICLOFENAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Blomme et al., 2003, Selective cyclooxygenase-2 inhibition does not affect the healing of cutaneous full-thickness incisional wounds in SKH-1 mice., Br. J. Dermatol.

Beubler, 2003, [Pharmacology of cyclooxygenase 2 inhibition]., Wien Med Wochenschr

Kirchheiner et al., 2003, Pharmacokinetics of diclofenac and inhibition of cyclooxygenases 1 and 2: no relationship to the CYP2C9 genetic polymorphism in humans., Br J Clin Pharmacol

ASPIRIN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Chan et al., 2007, Aspirin and the risk of colorectal cancer in relation to the expression of COX-2., N. Engl. J. Med.

KETOROLAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name intranasal ketorolac tromethamine, ROX-888,Sprix

Novel drug target Established target

Trial Name ketorolac tromethamine ophthalmic solution,Acuvail

Publications:

Ma et al., 2003, Cyclooxygenase 2 in infiltrating inflammatory cells in injured nerve is universally up-regulated following various types of peripheral nerve injury., Neuroscience

Höcherl et al., 2002, Role of prostanoids in regulation of the renin-angiotensin-aldosterone system by salt intake., Am. J. Physiol. Renal Physiol.

Padi et al., 2004, Pharmacological profile of parecoxib: a novel, potent injectable selective cyclooxygenase-2 inhibitor., Eur. J. Pharmacol.

NAPROXEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name MT 100

Novel drug target Established target

Trial Name MT 400,Treximet

Publications:

Albertini et al., 2007, COX-2 mRNA expression decreases in the subplantar muscle of rat paw subjected to carrageenan-induced inflammation after low level laser therapy., Inflamm. Res.

Kumar et al., 2007, Cyclooxygenase inhibition attenuates 3-nitropropionic acid-induced neurotoxicity in rats: possible antioxidant mechanisms., Fundam Clin Pharmacol

Dhir et al., 2007, Neuroprotective effect of nimesulide, a preferential COX-2 inhibitor, against pentylenetetrazol (PTZ)-induced chemical kindling and associated biochemical parameters in mice., Seizure

MECLOFENAMATE SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
NAPROXEN ETEMESIL PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
OXYPHENBUTAZONE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
BROMFENAC SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
IBUPROFEN LYSINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
AMINOSALICYLATE POTASSIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
NAPROXCINOD PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
DICLOFENAC SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
SC-560 PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
FENOPROFEN CALCIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
DICLOFENAC EPOLAMINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
ESFLURBIPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of COX-2 in human blood.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
OLSALAZINE SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
BISMUTH SUBSALICYLATE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
NAPROXEN SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
KETOROLAC TROMETHAMINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
TOLMETIN SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
FLURBIPROFEN SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
OXAPROZIN POTASSIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
POLMACOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Trial Name CG100649

Publications:
APRICOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name apricoxib, TG01,Capoxigem

Publications:
DICLOFENAC POTASSIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:
IBUPROFEN SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
BENZQUINAMIDE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
GW-406381 PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
BALSALAZIDE DISODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:
AMINOSALICYLATE SODIUM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:

IBUPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name HZT-501, ibuprofen + famotidine,Duexa

Novel drug target Established target

Specific Action of the Ligand Inhibition

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: ibuprofen pathways., Pharmacogenet Genomics

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Lee YS et al., 2006, Genetically mediated interindividual variation in analgesic responses to cyclooxygenase inhibitory drugs., Clin Pharmacol Ther

MELOXICAM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Gross et al., 1999, Natriuretic response to increased pressure is preserved with COX-2 inhibitors., Hypertension

Blanco et al., 1999, Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes., J. Rheumatol.

NIMESULIDE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Rainsford et al., 2006, Nimesulide -- a multifactorial approach to inflammation and pain: scientific and clinical consensus., Curr Med Res Opin

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

CHOLINE MAGNESIUM TRISALICYLATE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Simon, 2004, Adverse respiratory reactions to aspirin and nonsteroidal anti-inflammatory drugs., Curr Allergy Asthma Rep

Brzozowski et al., 2006, Interaction of nonsteroidal anti-inflammatory drugs (NSAID) with Helicobacter pylori in the stomach of humans and experimental animals., J. Physiol. Pharmacol.

Shen et al., 2006, Genetic polymorphisms in the cyclooxygenase-2 gene, use of nonsteroidal anti-inflammatory drugs, and breast cancer risk., Breast Cancer Res.

OXAPROZIN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Yamazaki et al., 2002, Nonsteroidal anti-inflammatory drugs induce apoptosis in association with activation of peroxisome proliferator-activated receptor gamma in rheumatoid synovial cells., J. Pharmacol. Exp. Ther.

Zhou et al., 2009, Design, synthesis, and in-vivo evaluation of 4,5-diaryloxazole as novel nonsteroidal anti-inflammatory drug., Biol. Pharm. Bull.

Kawai et al., 1998, Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells., Eur. J. Pharmacol.

GINSENG PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Yim et al., 2005, Cyclooxygenase-2 inhibits novel ginseng metabolite-mediated apoptosis., Cancer Res.

Kim et al., 2007, Transgenic Panax ginseng inhibits the production of TNF-alpha, IL-6, and IL-8 as well as COX-2 expression in human mast cells., Am. J. Chin. Med.

Seo et al., 2005, Effect of a fermented ginseng extract, BST204, on the expression of cyclooxygenase-2 in murine macrophages., Int. Immunopharmacol.

PIROXICAM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

Publications:

Fackovcova et al., 2000, Renal damage induced by the treatment with non-opioid analgesics--theoretical assumption or clinical significance., Bratisl Lek Listy

Blanco et al., 1999, Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes., J. Rheumatol.

Veiga et al., 2004, Prevention by celecoxib of secondary hyperalgesia induced by formalin in rats., Life Sci.

THALIDOMIDE PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Thalomid

Novel drug target Established target

Publications:

Wiedmann et al., 2005, Molecularly targeted therapy for gastrointestinal cancer., Curr Cancer Drug Targets

Hada et al., 2004, [A case report of metastatic pancreatic cancer that responded remarkably to the combination of thalidomide, celecoxib and irinotecan]., Gan To Kagaku Ryoho

Payvandi et al., 2004, Immunomodulatory drugs inhibit expression of cyclooxygenase-2 from TNF-alpha, IL-1beta, and LPS-stimulated human PBMC in a partially IL-10-dependent manner., Cell. Immunol.

BALSALAZIDE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name balsalazide disodium,Colazal, Giazo

Publications:

Stolfi et al., 2008, Cyclooxygenase-2-dependent and -independent inhibition of proliferation of colon cancer cells by 5-aminosalicylic acid., Biochem. Pharmacol.

Wiggins et al., 2009, Balsalazide: a novel 5-aminosalicylate prodrug for the treatment of active ulcerative colitis., Expert Opin Drug Metab Toxicol

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

TOLMETIN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Capasso et al., 1997, Arachidonic acid and its metabolites are involved in the expression of morphine dependence in guinea-pig isolated ileum., Eur. J. Pharmacol.

Burdan et al., 2004, Gastrointestinal and hepatic toxicity of selective and non-selective cyclooxygenase-2 inhibitors in pregnant and non-pregnant rats., Pharmacol. Res.

Kirkova et al., 2007, In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs., Auton Autacoid Pharmacol

FLURBIPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name HCT 1026, NO-flurbiprofen

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Smith et al., 2000, Arachidonic acid and nonsteroidal anti-inflammatory drugs induce conformational changes in the human prostaglandin endoperoxide H2 synthase-2 (cyclooxygenase-2)., J. Biol. Chem.

Bayly et al., 1999, Structure-based design of COX-2 selectivity into flurbiprofen., Bioorg. Med. Chem. Lett.

Hinz et al., 2001, Flurbiprofen enantiomers inhibit inducible nitric oxide synthase expression in RAW 264.7 macrophages., Pharm. Res.

CELECOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Novel drug target Established target

Trial Name celecoxib,Celebrex, Celecox

Publications:

Lu et al., 2002, Cyclooxygenase-2 inhibitor celecoxib inhibits promotion of mammary tumorigenesis in rats fed a high fat diet rich in n-6 polyunsaturated fatty acids., Cancer Lett.

Sigthorsson et al., 2002, COX-1 and 2, intestinal integrity, and pathogenesis of nonsteroidal anti-inflammatory drug enteropathy in mice., Gastroenterology

Scheiman, 2002, Outcomes studies of the gastrointestinal safety of cyclooxygenase-2 inhibitors., Cleve Clin J Med

MESALAMINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name MAX-002

Novel drug target Established target

Trial Name mesalamine,Pentasa, Canasa, Asacol

Publications:

Distrutti et al., 2006, 5-Amino-2-hydroxybenzoic acid 4-(5-thioxo-5H-[1,2]dithiol-3yl)-phenyl ester (ATB-429), a hydrogen sulfide-releasing derivative of mesalamine, exerts antinociceptive effects in a model of postinflammatory hypersensitivity., J. Pharmacol. Exp. Ther.

Mifflin et al., 2004, Aspirin-mediated COX-2 transcript stabilization via sustained p38 activation in human intestinal myofibroblasts., Mol. Pharmacol.

Generini et al., Therapy of spondylarthropathy in inflammatory bowel disease., Clin. Exp. Rheumatol.

ETORICOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name etoricoxib, MK-663,Arcoxia

Novel drug target Established target

Specific Action of the Ligand Inhibition

Publications:

FitzGerald, 2007, COX-2 in play at the AHA and the FDA., Trends Pharmacol. Sci.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Yuan et al., 2007, Global gastrointestinal safety profile of etoricoxib and lumiracoxib., Curr. Pharm. Des.

MECLOFENAMIC ACID PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Wilson et al., 2004, Determination of expression of cyclooxygenase-1 and -2 isozymes in canine tissues and their differential sensitivity to nonsteroidal anti-inflammatory drugs., Am. J. Vet. Res.

Smith et al., 1994, Interactions of PGH synthase isozymes-1 and -2 with NSAIDs., Ann. N. Y. Acad. Sci.

Traupe et al., 2002, Obesity increases prostanoid-mediated vasoconstriction and vascular thromboxane receptor gene expression., J. Hypertens.

DIFLUNISAL PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Trial Name CRx-401

Publications:

Moore et al., 2001, Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice., J Am Dent Assoc

Young et al., 1996, Human whole blood assays for inhibition of prostaglandin G/H synthases-1 and -2 using A23187 and lipopolysaccharide stimulation of thromboxane B2 production., Inflamm. Res.

Jeske, 1999, COX-2 inhibitors and dental pain control., J Gt Houst Dent Soc

SULFASALAZINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name sulfasalazine,Azulfidine, Salazopyrin

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Distrutti et al., 2006, 5-Amino-2-hydroxybenzoic acid 4-(5-thioxo-5H-[1,2]dithiol-3yl)-phenyl ester (ATB-429), a hydrogen sulfide-releasing derivative of mesalamine, exerts antinociceptive effects in a model of postinflammatory hypersensitivity., J. Pharmacol. Exp. Ther.

Mifflin et al., 2004, Aspirin-mediated COX-2 transcript stabilization via sustained p38 activation in human intestinal myofibroblasts., Mol. Pharmacol.

Generini et al., Therapy of spondylarthropathy in inflammatory bowel disease., Clin. Exp. Rheumatol.

NS-398 PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

Yeh JR et al., 2009, Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation., Nat Chem Biol

Su B et al., 2006, Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition., J Med Chem

Zhang L et al., 2011, Effects of β-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro., Bioorg Med Chem

FENOPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Poggi et al., 2006, Pharmacodynamics, chiral pharmacokinetics, and pharmacokinetic-pharmacodynamic modeling of fenoprofen in patients with diabetes mellitus., J Clin Pharmacol

VALDECOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Tacconelli et al., 2002, The biochemical selectivity of novel COX-2 inhibitors in whole blood assays of COX-isozyme activity., Curr Med Res Opin

Jain, 2000, Evaluation of intravenous parecoxib for the relief of acute post-surgical pain., Expert Opin Investig Drugs

BROMFENAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Bromfenac

Novel drug target Established target

Trial Name ISV-101

Publications:

Sanchez-Matienzo et al., 2006, Hepatic disorders in patients treated with COX-2 selective inhibitors or nonselective NSAIDs: a case/noncase analysis of spontaneous reports., Clin Ther

Chitturi et al., 2002, Hepatotoxicity of commonly used drugs: nonsteroidal anti-inflammatory drugs, antihypertensives, antidiabetic agents, anticonvulsants, lipid-lowering agents, psychotropic drugs., Semin. Liver Dis.

Waterbury et al., 2006, Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium., Curr Med Res Opin

TENOXICAM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamada et al., 1997, Prostaglandin E2 production dependent upon cyclooxygenase-1 and cyclooxygenase-2 and its contradictory modulation by auranofin in rat peritoneal macrophages., J. Pharmacol. Exp. Ther.

Yilmaz et al., 2005, The use and safety profile of non-steroidal antiinflammatory drugs among Turkish patients with osteoarthritis., Turk J Gastroenterol

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

TIAPROFENIC ACID PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

NABUMETONE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name -

Publications:

Fackovcova et al., 2000, Renal damage induced by the treatment with non-opioid analgesics--theoretical assumption or clinical significance., Bratisl Lek Listy

Elliott et al., 1995, A nitric oxide-releasing nonsteroidal anti-inflammatory drug accelerates gastric ulcer healing in rats., Gastroenterology

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

LUMIRACOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Esser et al., 2005, Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2., Br. J. Pharmacol.

Atherton et al., 2004, Pharmacology and gastrointestinal safety of lumiracoxib, a novel cyclooxygenase-2 selective inhibitor: An integrated study., Clin. Gastroenterol. Hepatol.

LENALIDOMIDE PTGS2

Interaction Types & Directionality:

negative modulator (inhibitory)

Interaction Info:

Publications:

Zeldis et al., 2003, Potential new therapeutics for Waldenstrom's macroglobulinemia., Semin. Oncol.

Payvandi et al., 2004, Immunomodulatory drugs inhibit expression of cyclooxygenase-2 from TNF-alpha, IL-1beta, and LPS-stimulated human PBMC in a partially IL-10-dependent manner., Cell. Immunol.

ANTIPYRINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Brune et al., Pharmacokinetic and pharmacodynamic aspects of the ideal COX-2 inhibitor: a pharmacologist's perspective., Clin. Exp. Rheumatol.

ROFECOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name rofecoxib,Vioxx

Novel drug target Established target

Specific Action of the Ligand Inhibition

Publications:

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Lee YS et al., 2006, Genetically mediated interindividual variation in analgesic responses to cyclooxygenase inhibitory drugs., Clin Pharmacol Ther

Ashok et al., 2011, Selective cyclooxygenase-2 (COX-2) inhibitors and breast cancer risk., Breast

INDOMETHACIN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Specific Action of the Ligand Inhibition

Publications:

Christ AN et al., 2010, Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases., J Med Chem

Hanna MM, 2012, New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies., Eur J Med Chem

Pergola C et al., 2014, Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase., J Med Chem

DEXIBUPROFEN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Onnis V et al., 2010, Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors., J Med Chem

Ashraf Z et al., 2016, Synthesis, Bioevaluation and Molecular Dynamic Simulation Studies of Dexibuprofen-Antioxidant Mutual Prodrugs., Int J Mol Sci

SALSALATE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Schaefer et al., 2003, Interaction of rofecoxib and celecoxib with warfarin., Am J Health Syst Pharm

Motsko et al., 2006, Temporal relationship between use of NSAIDs, including selective COX-2 inhibitors, and cardiovascular risk., Drug Saf

Josephs et al., 1999, Products of cyclooxygenase-2 catalysis regulate postoperative bowel motility., J. Surg. Res.

PARECOXIB PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name parecoxib sodium,Dynastat

Novel drug target Established target

Publications:

Talley et al., 2000, N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration., J. Med. Chem.

MEFENAMIC ACID PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Publications:

Bhat et al., 2007, Interaction between inhibitors of inducible nitric oxide synthase and cyclooxygenase in adjuvant-induced arthritis in female albino rats: an isobolographic study., Eur. J. Pharmacol.

Bhat et al., 2005, Interaction between inhibitors of inducible nitric oxide synthase and cyclooxygenase in Brewer's yeast induced pyrexia in mice: an isobolographic study., Eur. J. Pharmacol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

LORNOXICAM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Bianchi et al., 2002, Effects of lornoxicam, piroxicam, and meloxicam in a model of thermal hindpaw hyperalgesia induced by formalin injection in rat tail., Pharmacol. Res.

Berg et al., 1999, The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro., Inflamm. Res.

Renner et al., 2010, Pain control in first-trimester surgical abortion: a systematic review of randomized controlled trials., Contraception

ANTRAFENINE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Albertini et al., 2007, COX-2 mRNA expression decreases in the subplantar muscle of rat paw subjected to carrageenan-induced inflammation after low level laser therapy., Inflamm. Res.

Kumar et al., 2007, Cyclooxygenase inhibition attenuates 3-nitropropionic acid-induced neurotoxicity in rats: possible antioxidant mechanisms., Fundam Clin Pharmacol

Dhir et al., 2007, Neuroprotective effect of nimesulide, a preferential COX-2 inhibitor, against pentylenetetrazol (PTZ)-induced chemical kindling and associated biochemical parameters in mice., Seizure

ICOSAPENT PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Das, 2005, Can COX-2 inhibitor-induced increase in cardiovascular disease risk be modified by essential fatty acids?, J Assoc Physicians India

Lee et al., 2003, Differential modulation of Toll-like receptors by fatty acids: preferential inhibition by n-3 polyunsaturated fatty acids., J. Lipid Res.

Ait-Said et al., 2003, Inhibition by eicosapentaenoic acid of IL-1beta-induced PGHS-2 expression in human microvascular endothelial cells: involvement of lipoxygenase-derived metabolites and p38 MAPK pathway., Biochim. Biophys. Acta

NIFLUMIC ACID PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Jabeen et al., 2005, Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution., Acta Crystallogr. D Biol. Crystallogr.

Diao et al., 2007, Rat ovulation, implantation and decidualization are severely compromised by COX-2 inhibitors., Front. Biosci.

Alpert et al., 2007, Selective cyclooxygenase-2 inhibitors stimulate glucose transport in L6 myotubes in a protein kinase Cdelta-dependent manner., Biochem. Pharmacol.

POMALIDOMIDE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Ferguson et al., 2007, Immunomodulatory drug CC-4047 is a cell-type and stimulus-selective transcriptional inhibitor of cyclooxygenase 2., J. Clin. Immunol.
ALCLOFENAC PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Thomas GM et al., 1975, Simultaneous pharmacokinetics of alclofenace in plasma and synovial fluid in patients with rheumatoid arthritis., Curr Med Res Opin
DROXICAM PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Esteve J et al., 1988, Pharmacological profile of droxicam., Gen Pharmacol
NABIXIMOLS PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics

TOLFENAMIC ACID PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Tokola RA et al., 1984, Effects of migraine attack and metoclopramide on the absorption of tolfenamic acid., Br J Clin Pharmacol

Lees P et al., 1998, Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation., Vet J

McKellar QA et al., 1994, Pharmacodynamics of tolfenamic acid in dogs. Evaluation of dose response relationships., Eur J Pharmacol

CANNABIDIOL PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
BUFEXAMAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Brogden RN et al., 1975, Bufexamac: a review of its pharmacological properties and therapeutic efficacy in inflammatory dermatoses., Drugs
FISH OIL TRIGLYCERIDES PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Visioli F et al., 2012, Molecular targets of omega 3 and conjugated linoleic Fatty acids - "micromanaging" cellular response., Front Physiol
ACECLOFENAC PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Legrand E, 2004, Aceclofenac in the management of inflammatory pain., Expert Opin Pharmacother

MAGNESIUM SALICYLATE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Chae et al., 2004, Salicylate regulates COX-2 expression through ERK and subsequent NF-kappaB activation in osteoblasts., Immunopharmacol Immunotoxicol

Wu, 2003, Aspirin and other cyclooxygenase inhibitors: new therapeutic insights., Semin Vasc Med

Elvira et al., 2001, Incorporation of salicylic acid derivatives to hydrophilic copolymer systems with biomedical applications., J Mater Sci Mater Med

LOXOPROFEN PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Riendeau D et al., 2004, Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2., Bioorg Med Chem Lett
CHEMBL173562 PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Levy G, 1980, Clinical pharmacokinetics of salicylates: a re-assessment., Br J Clin Pharmacol
TALNIFLUMATE PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
DEXKETOPROFEN PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
PROPACETAMOL PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
ACEMETACIN PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
TROLAMINE SALICYLATE PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
PHENYL SALICYLATE PTGS2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:
CIMICOXIB PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Cimicoxib

Publications:

Almansa et al., 2004, New water-soluble sulfonylphosphoramidic acid derivatives of the COX-2 selective inhibitor cimicoxib. A novel approach to sulfonamide prodrugs., J. Med. Chem.
LICOFELONE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name licofelone, ML3000

Publications:

Vidal et al., 2007, Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis., J. Pharmacol. Exp. Ther.
VB-201 PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name VB-201

Publications:
DERSALAZINE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name dersalazine sodium

Novel drug target Established target

Publications:
FIROCOXIB PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

McCann et al., 2004, In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in dogs with experimentally induced synovitis., Am. J. Vet. Res.

CURCUMIN PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Koeberle A et al., 2014, SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase., J Med Chem

DIHOMO-GAMMA-LINOLENIC ACID PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Das, 2005, Can COX-2 inhibitor-induced increase in cardiovascular disease risk be modified by essential fatty acids?, J Assoc Physicians India

Thuresson et al., 2001, Mutational and X-ray crystallographic analysis of the interaction of dihomo-gamma -linolenic acid with prostaglandin endoperoxide H synthases., J. Biol. Chem.

Levin et al., 2002, Differential metabolism of dihomo-gamma-linolenic acid and arachidonic acid by cyclo-oxygenase-1 and cyclo-oxygenase-2: implications for cellular synthesis of prostaglandin E1 and prostaglandin E2., Biochem. J.

CAPECITABINE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kim JG et al., 2009, Prostaglandin synthase 2/cyclooxygenase 2 (PTGS2/COX2) 8473T>C polymorphism associated with prognosis for patients with colorectal cancer treated with capecitabine and oxaliplatin., Cancer Chemother Pharmacol

HYDROXYCHLOROQUINE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ben-Chetrit et al., 2005, The effects of colchicine and hydroxychloroquine on the cyclo-oxygenases COX-1 and COX-2., Rheumatol. Int.
E163 PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Wang H et al., 1999, Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries., J Nat Prod
(R)-IBUPROPHEN PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Onnis V et al., 2010, Synthesis and evaluation of paracetamol esters as novel fatty acid amide hydrolase inhibitors., J Med Chem

CURCUMIN PYRAZOLE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Koeberle A et al., 2014, SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase., J Med Chem

OXALIPLATIN PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kim JG et al., 2009, Prostaglandin synthase 2/cyclooxygenase 2 (PTGS2/COX2) 8473T>C polymorphism associated with prognosis for patients with colorectal cancer treated with capecitabine and oxaliplatin., Cancer Chemother Pharmacol

CHEMBL2171117 PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Cui PH et al., 2012, Antiproliferative and antimigratory actions of synthetic long chain n-3 monounsaturated fatty acids in breast cancer cells that overexpress cyclooxygenase-2., J Med Chem
RESERPINE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Cantarella et al., 2005, Adrenomedullin modulates COX-2 and HGF expression in reserpine-injuried gastric mucosa in the rat., Eur. J. Pharmacol.
CYCLOSPORINE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Robida et al., 2000, Cyclosporin A selectively inhibits mitogen-induced cyclooxygenase-2 gene transcription in vascular smooth muscle cells., Mol. Pharmacol.
URSOLIC ACID PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ringbom T et al., 1998, Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis., J Nat Prod
RALOXIFENE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Oviedo et al., Raloxifene increases the capacity of serum to promote prostacyclin release in human endothelial cells: implication of COX-1 and COX-2., Menopause
CHEMBL1235806 PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
FLUFENAMIC ACID PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ouellet et al., 1995, Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms., Biochem. J.
ATENOLOL PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
FENBUFEN PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RWJ-67657 PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
IMRECOXIB PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DARBUFELONE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MORNIFLUMATE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BENDAZAC PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DIPYRITHIONE PTGS2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000073756
- Version: 101_38
Alternate Names:

PTGS2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P35354
- Version: 11-September-2012
Alternate Names:

PGH2_HUMAN Uniprot Id

PROSTAGLANDIN G/H SYNTHASE 2 Uniprot Protein Name

5743 Entrez Gene Id

Gene Info:

Uniprot Status Swiss-Prot

Interpro Type Family

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

RussLampel: ENSG00000073756

Version: 26-July-2011

Alternate Names:

PROSTAGLANDIN G/H SYNTHASE 2 PRECURSOR (EC 1.14.99.1) (CYCLOOXYGENASE- 2) (COX-2) (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE 2) (PROSTAGLANDIN H2 SYNTHASE 2) (PGH SYNTHASE 2) (PGHS-2) (PHS II). [SOURCE:UNIPROT/SWISSPROT;ACC:P35354] Description

ENSG00000073756 Ensembl Gene Id

PTGS2 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TdgClinicalTrial: P35354
- Version: January-2014
Alternate Names:

PTGS2 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:1.14.99.1

Publications:
TEND: P35354
- Version: 01-August-2011
Alternate Names:

PGH2_HUMAN Uniprot Id

5743 Entrez Gene Id

P35354 Uniprot Accession

Gene Info:

Target Subclass 1.14.99.1

Target Main Class Enzymes

Publications:
GuideToPharmacology: 5743
- Version: 29-September-2020
Alternate Names:

9605 HUGO Gene ID

9605 HUGO Gene Symbol

prostaglandin-endoperoxide synthase 2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Cyclooxygenase

GuideToPharmacology Gene Category ID 269

Gene Categories:

ENZYME

Publications:

PharmGKB: PTGS2

Version: 18-August-2020

Alternate Names:

PA293 PharmGKB ID

Gene Info:

Publications:

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

Gong L et al., 2012, Celecoxib pathways: pharmacokinetics and pharmacodynamics., Pharmacogenet Genomics

Roberts RL et al., 2015, Pharmacogenetic considerations in the treatment of gout., Pharmacogenomics

CIViC: PTGS2
- Version: 14-September-2020
Alternate Names:

5743 Entrez Gene ID

4659 CIViC Gene ID

Gene Info:

Publications:

Chan et al., 2007, Aspirin and the risk of colorectal cancer in relation to the expression of COX-2., N. Engl. J. Med.

DrugBank: BE0000262

Version: 5.1.7

Alternate Names:

PTGS2 DrugBank Gene Name

P35354 UniProt Accession

5743 Entrez Gene Id

Gene Info:

Publications:

Das, 2005, Can COX-2 inhibitor-induced increase in cardiovascular disease risk be modified by essential fatty acids?, J Assoc Physicians India

Levin et al., 2002, Differential metabolism of dihomo-gamma-linolenic acid and arachidonic acid by cyclo-oxygenase-1 and cyclo-oxygenase-2: implications for cellular synthesis of prostaglandin E1 and prostaglandin E2., Biochem. J.

Thuresson et al., 2001, Mutational and X-ray crystallographic analysis of the interaction of dihomo-gamma -linolenic acid with prostaglandin endoperoxide H synthases., J. Biol. Chem.

NCI: PTGS2

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Robida et al., 2000, Cyclosporin A selectively inhibits mitogen-induced cyclooxygenase-2 gene transcription in vascular smooth muscle cells., Mol. Pharmacol.

Inoue et al., 2007, Cyclooxygenase-2 inhibition promotes enhancement of antitumor responses by transcutaneous vaccination with cytosine-phosphate-guanosine-oligodeoxynucleotides and model tumor antigen., J. Invest. Dermatol.

Ben-Chetrit et al., 2005, The effects of colchicine and hydroxychloroquine on the cyclo-oxygenases COX-1 and COX-2., Rheumatol. Int.

DTC: PTGS2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Park JB, 2014, Synthesis and characterization of norbelladine, a precursor of Amaryllidaceae alkaloid, as an anti-inflammatory/anti-COX compound., Bioorg Med Chem Lett

Zhang L et al., 2011, Effects of β-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro., Bioorg Med Chem

Su B et al., 2006, Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition., J Med Chem

HingoraniCasas: ENSG00000073756
- Version: 31-May-2017
Alternate Names:

ENSG00000073756 Gene Symbol

PTGS2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: PTGS2
- Version: 12-May-2016
Alternate Names:

PTGS2 Gene Symbol

Gene Info:

Publications:
TALC: COX-2
- Version: 12-May-2016
Alternate Names:

COX-2 Gene Symbol

Gene Info:

Publications:
ChemblInteractions: COX2
- Version: chembl_23
Alternate Names:

COX2 GENE_SYMBOL

PTGS2 GENE_SYMBOL

Prostaglandin G/H synthase 2 UNIPROT

Gene Info:

Publications:
Pharos: PTGS2
- Version: 03-September-2020
Alternate Names:

Prostaglandin G/H synthase 2 Gene Name

P35354 UniProt ID

Gene Info:

Gene Categories:

ENZYME

Publications:
GO: PTGS2
- Version: 05-September-2020
Alternate Names:

COX2 GO Gene Synonym

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:
TTD: Prostaglandin G/H synthase 2
- Version: 2020.06.01
Alternate Names:

COX-2 TTD Gene Abbreviation

T66665 TTD Target ID

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: PTGS2
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Novel drug target	Established target
Trial Name	-
Specific Action of the Ligand	Inhibition

Mechanism of Interaction	Cyclooxygenase inhibitor
Direct Interaction	yes
Trial Name	-

Details of the Assay for Interaction	Inhibition of COX2 in human whole blood.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Direct Interaction?	True
Details of the Assay for Interaction	Measured as LPS-induced PGE<sub>2</sub> production in COX-1-inhibited human monocytes.
Specific Action of the Ligand	Inhibition

Trial Name	intranasal ketorolac tromethamine, ROX-888,Sprix
Novel drug target	Established target
Trial Name	ketorolac tromethamine ophthalmic solution,Acuvail

Trial Name	MT 100
Novel drug target	Established target
Trial Name	MT 400,Treximet

Details of the Assay for Interaction	Inhibition of COX-2 in human blood.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	Cyclooxygenase-2 inhibitor
Trial Name	CG100649

Trial Name	HZT-501, ibuprofen + famotidine,Duexa
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Notes
Novel drug target	Established target
Trial Name	celecoxib,Celebrex, Celecox

Trial Name	MAX-002
Novel drug target	Established target
Trial Name	mesalamine,Pentasa, Canasa, Asacol

Trial Name	etoricoxib, MK-663,Arcoxia
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Trial Name	sulfasalazine,Azulfidine, Salazopyrin
Novel drug target	Established target
Mechanism of Interaction	Cyclooxygenase inhibitor

Trial Name	Bromfenac
Novel drug target	Established target
Trial Name	ISV-101

Trial Name	rofecoxib,Vioxx
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Trial Name	parecoxib sodium,Dynastat
Novel drug target	Established target

Trial Name	dersalazine sodium
Novel drug target	Established target

PGH2_HUMAN	Uniprot Id
PROSTAGLANDIN G/H SYNTHASE 2	Uniprot Protein Name
5743	Entrez Gene Id

PROSTAGLANDIN G/H SYNTHASE 2 PRECURSOR (EC 1.14.99.1) (CYCLOOXYGENASE- 2) (COX-2) (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASE 2) (PROSTAGLANDIN H2 SYNTHASE 2) (PGH SYNTHASE 2) (PGHS-2) (PHS II). [SOURCE:UNIPROT/SWISSPROT;ACC:P35354]	Description
ENSG00000073756	Ensembl Gene Id
PTGS2	Display Id

PTGS2 Gene Record

PTGS2 5743 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications: Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes Trial Name -

Publications: Gamache et al., 2000, Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy., Inflammation

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of COX2 in human whole blood. Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Details of the Assay for Interaction Measured as LPS-induced PGE<sub>2</sub> production in COX-1-inhibited human monocytes. Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Direct Interaction yes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Publications: Chan et al., 2007, Aspirin and the risk of colorectal cancer in relation to the expression of COX-2., N. Engl. J. Med.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name intranasal ketorolac tromethamine, ROX-888,Sprix Novel drug target Established target Trial Name ketorolac tromethamine ophthalmic solution,Acuvail

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name MT 100 Novel drug target Established target Trial Name MT 400,Treximet

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Inhibition of COX-2 in human blood. Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name -

Publications:

Gamache et al., 2000, Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy., Inflammation

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of COX2 in human whole blood.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Details of the Assay for Interaction Measured as LPS-induced PGE<sub>2</sub> production in COX-1-inhibited human monocytes.

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Chan et al., 2007, Aspirin and the risk of colorectal cancer in relation to the expression of COX-2., N. Engl. J. Med.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name intranasal ketorolac tromethamine, ROX-888,Sprix

Novel drug target Established target

Trial Name ketorolac tromethamine ophthalmic solution,Acuvail

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name MT 100

Novel drug target Established target

Trial Name MT 400,Treximet

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Inhibition of COX-2 in human blood.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Trial Name CG100649

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name apricoxib, TG01,Capoxigem

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

9605	HUGO Gene ID
9605	HUGO Gene Symbol
prostaglandin-endoperoxide synthase 2	HUGO Gene Name

PTGS2	DrugBank Gene Name
P35354	UniProt Accession
5743	Entrez Gene Id

COX2	GENE_SYMBOL
PTGS2	GENE_SYMBOL
Prostaglandin G/H synthase 2	UNIPROT