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

DRUG RESISTANCE
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.

ETORICOXIB PTGS2

Interaction Score: 6.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name etoricoxib, MK-663,Arcoxia

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
17573128 11752352 17691997 17164136 17016423 17139284 19602986

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
CARPROFEN PTGS2

Interaction Score: 2.77

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
17181139 15939622 11703020 10895904 15198222 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
SUPROFEN PTGS2

Interaction Score: 2.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17016423 17139284 11885959 10377455

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
CIMICOXIB PTGS2

Interaction Score: 1.85

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Cimicoxib

PMIDs:
15481993

Sources:
DrugBank TdgClinicalTrial TTD
VALDECOXIB PTGS2

Interaction Score: 1.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
19602986 12564662 11060833 12167567 15494548 10715145 11752352 12644588 20143779

Sources:
DTC DrugBank ChemblInteractions GuideToPharmacology PharmGKB TTD
OXAPROZIN PTGS2

Interaction Score: 1.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

PMIDs:
12065695 19952416 9650852 17024689 9831331 19338579

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
ANTRAFENINE PTGS2

Interaction Score: 1.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17607546 17521299 17604186 17612049 11752352 17532719

Sources:
DrugBank
SALSALATE PTGS2

Interaction Score: 1.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12901032 16808554 10452868 9711054

Sources:
DrugBank TdgClinicalTrial TEND
ETODOLAC PTGS2

Interaction Score: 1.62

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

PMIDs:
11275997 15198222 11009046 11752352 12824918 10594327 19602986

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
KETOROLAC PTGS2

Interaction Score: 1.54

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

PMIDs:
14568029 12110513 15102535 12446609 14568028 11695255

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology
TOLMETIN PTGS2

Interaction Score: 1.54

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9253954 15458776 17391279 11752352 14613550 10465690

Sources:
DrugBank TdgClinicalTrial TEND TTD
MELOXICAM PTGS2

Interaction Score: 1.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
19602986 10567199 10381057 10340919 10381787 10220944 11752352 16197363 30774225

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
MAGNESIUM SALICYLATE PTGS2

Interaction Score: 1.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15106733 15199473 15348270 15035793 15070163

Sources:
DrugBank
APRICOXIB PTGS2

Interaction Score: 1.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name apricoxib, TG01,Capoxigem

PMIDs:
None found

Sources:
TALC TdgClinicalTrial ChemblInteractions
BROMFENAC PTGS2

Interaction Score: 1.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Bromfenac

Novel drug target Established target

Trial Name ISV-101

PMIDs:
16982289 12016548 16846546

Sources:
DrugBank TdgClinicalTrial TEND
CHOLINE MAGNESIUM TRISALICYLATE PTGS2

Interaction Score: 1.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
14680616 17033106 17181859 17037745 17258197

Sources:
DrugBank
LUMIRACOXIB PTGS2

Interaction Score: 1.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19602986 15655513 15017615 14552704 11752352 15177307 14965322

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD
DIHOMO-GAMMA-LINOLENIC ACID PTGS2

Interaction Score: 1.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16190133 11121413 11939906 15990700

Sources:
DrugBank
NEPAFENAC PTGS2

Interaction Score: 1.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name -

PMIDs:
10850857

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND
FLURBIPROFEN PTGS2

Interaction Score: 1.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name HCT 1026, NO-flurbiprofen

Mechanism of Interaction Cyclooxygenase inhibitor

PMIDs:
11006278 10091674 11405284 17562170 10977131 19066416 10773011

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
ROFECOXIB PTGS2

Interaction Score: 1.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name rofecoxib,Vioxx

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19602986 16678543 20724158 10580458 10566562 20166930 10643177 11752352 11398914 10693877 18922570 10555907

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB TTD
DIFLUNISAL PTGS2

Interaction Score: 1.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Trial Name CRx-401

PMIDs:
11315375 8737748 10825891 11673972 12852483 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD
CHEMBL1235806 PTGS2

Interaction Score: 0.92

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL2171117 PTGS2

Interaction Score: 0.92

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22822908

Sources:
DTC
(R)-IBUPROPHEN PTGS2

Interaction Score: 0.92

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20143779

Sources:
DTC
TENOXICAM PTGS2

Interaction Score: 0.92

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9152412 16245223 11752352 11563332 15943176 15756931

Sources:
DrugBank TdgClinicalTrial TEND TTD
KETOPROFEN PTGS2

Interaction Score: 0.92

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

PMIDs:
11729362 10895904 14513718 15198222 11752352 11814865

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
FIROCOXIB PTGS2

Interaction Score: 0.92

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15077695

Sources:
DrugBank
BALSALAZIDE PTGS2

Interaction Score: 0.81

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name balsalazide disodium,Colazal, Giazo

PMIDs:
17981262 19743890 17016423 17139284 12950415

Sources:
DrugBank TdgClinicalTrial
TIAPROFENIC ACID PTGS2

Interaction Score: 0.77

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17016423 17139284 11752352 2277128

Sources:
DrugBank
NABUMETONE PTGS2

Interaction Score: 0.73

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name -

PMIDs:
11153163 7615202 11752352 11304699 12047490 15456329

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND TTD
PARECOXIB PTGS2

Interaction Score: 0.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name parecoxib sodium,Dynastat

Novel drug target Established target

PMIDs:
10794682

Sources:
DrugBank TdgClinicalTrial
GINSENG PTGS2

Interaction Score: 0.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15753395 17436372 15778128

Sources:
DrugBank
NAPROXEN PTGS2

Interaction Score: 0.58

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name MT 100

Novel drug target Established target

Trial Name MT 400,Treximet

PMIDs:
17607546 17521299 17604186 17612049 11752352 17532719 19602986 30247840

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD
MECLOFENAMIC ACID PTGS2

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15198222 7825862 12409963 16290292 10639181

Sources:
DrugBank
CHEMBL173562 PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
7437270

Sources:
DrugBank
LOXOPROFEN PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
14980665

Sources:
DrugBank
DROXICAM PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
3278945

Sources:
DrugBank
ALCLOFENAC PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
241595

Sources:
DrugBank
LORNOXICAM PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11846620 10450786 20399943 17516707

Sources:
DrugBank
POLMACOXIB PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Trial Name CG100649

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
ANTIPYRINE PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11695253

Sources:
DrugBank
E163 PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10075763

Sources:
DTC
NS-398 PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
19172146 16480277 21775152 25453792

Sources:
DTC GuideToPharmacology
LICOFELONE PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name licofelone, ML3000

PMIDs:
17015640

Sources:
DrugBank TdgClinicalTrial
NAPROXCINOD PTGS2

Interaction Score: 0.46

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology
PIROXICAM PTGS2

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

PMIDs:
11153163 10381057 15464832 11785774 11952155 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology
PHENYLBUTAZONE PTGS2

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Inhibition

PMIDs:
12213119 15939622 11752352 15489888

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
MEFENAMIC ACID PTGS2

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

PMIDs:
17150210 15792781 11752352 9626023 7832763 10393680

Sources:
DrugBank ChemblInteractions
FENOPROFEN PTGS2

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17050798

Sources:
DrugBank TdgClinicalTrial TEND
ACECLOFENAC PTGS2

Interaction Score: 0.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15163279

Sources:
DrugBank
ICOSAPENT PTGS2

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16190133 12562875 12573452 16141635 17459764 20463020

Sources:
DrugBank
TROLAMINE SALICYLATE PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
ACEMETACIN PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
BENDAZAC PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
AMINOSALICYLATE SODIUM PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GW-406381 PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
DARBUFELONE PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
IBUPROFEN SODIUM PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DICLOFENAC POTASSIUM PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CURCUMIN PYRAZOLE PTGS2

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

</

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

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

Mechanism of Interaction	Cyclooxygenase-2 inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

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	Bromfenac
Novel drug target	Established target
Trial Name	ISV-101

Mechanism of Interaction	Cyclooxygenase inhibitor
Direct Interaction	yes
Trial Name	-

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

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

Trial Name	parecoxib sodium,Dynastat
Novel drug target	Established target

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

PTGS2 Gene Record

PTGS2 5743 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 17573128 11752352 17691997 17164136 17016423 17139284 19602986

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 17181139 15939622 11703020 10895904 15198222 11752352

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 17016423 17139284 11885959 10377455

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name Cimicoxib

PMIDs: 15481993

Sources: DrugBank TdgClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase-2 inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: 19602986 12564662 11060833 12167567 15494548 10715145 11752352 12644588 20143779

Sources: DTC DrugBank ChemblInteractions GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 12065695 19952416 9650852 17024689 9831331 19338579

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17607546 17521299 17604186 17612049 11752352 17532719

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12901032 16808554 10452868 9711054

Sources: DrugBank TdgClinicalTrial TEND

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

PMIDs: 11275997 15198222 11009046 11752352 12824918 10594327 19602986

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

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

PMIDs: 14568029 12110513 15102535 12446609 14568028 11695255

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 9253954 15458776 17391279 11752352 14613550 10465690

Sources: DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase-2 inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

PMIDs: 19602986 10567199 10381057 10340919 10381787 10220944 11752352 16197363 30774225

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 15106733 15199473 15348270 15035793 15070163

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase-2 inhibitor Direct Interaction yes Trial Name apricoxib, TG01,Capoxigem

PMIDs: None found

Sources: TALC TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Bromfenac Novel drug target Established target Trial Name ISV-101

PMIDs: 16982289 12016548 16846546

Sources: DrugBank TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 14680616 17033106 17181859 17037745 17258197

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 19602986 15655513 15017615 14552704 11752352 15177307 14965322

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16190133 11121413 11939906 15990700

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name etoricoxib, MK-663,Arcoxia

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
17573128 11752352 17691997 17164136 17016423 17139284 19602986

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
17181139 15939622 11703020 10895904 15198222 11752352

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17016423 17139284 11885959 10377455

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Cimicoxib

PMIDs:
15481993

Sources:
DrugBank TdgClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
19602986 12564662 11060833 12167567 15494548 10715145 11752352 12644588 20143779

Sources:
DTC DrugBank ChemblInteractions GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction Cyclooxygenase inhibitor

PMIDs:
12065695 19952416 9650852 17024689 9831331 19338579

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17607546 17521299 17604186 17612049 11752352 17532719

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12901032 16808554 10452868 9711054

Sources:
DrugBank TdgClinicalTrial TEND

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

PMIDs:
11275997 15198222 11009046 11752352 12824918 10594327 19602986

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

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

PMIDs:
14568029 12110513 15102535 12446609 14568028 11695255

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9253954 15458776 17391279 11752352 14613550 10465690

Sources:
DrugBank TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
19602986 10567199 10381057 10340919 10381787 10220944 11752352 16197363 30774225

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
15106733 15199473 15348270 15035793 15070163

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase-2 inhibitor

Direct Interaction yes

Trial Name apricoxib, TG01,Capoxigem

PMIDs:
None found

Sources:
TALC TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Bromfenac

Novel drug target Established target

Trial Name ISV-101

PMIDs:
16982289 12016548 16846546

Sources:
DrugBank TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
14680616 17033106 17181859 17037745 17258197

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19602986 15655513 15017615 14552704 11752352 15177307 14965322

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

n/a

PMIDs:
16190133 11121413 11939906 15990700

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Trial Name -

PMIDs:
10850857

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name HCT 1026, NO-flurbiprofen

Mechanism of Interaction Cyclooxygenase inhibitor

PMIDs:
11006278 10091674 11405284 17562170 10977131 19066416 10773011

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name rofecoxib,Vioxx

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19602986 16678543 20724158 10580458 10566562 20166930 10643177 11752352 11398914 10693877 18922570 10555907

Sources:
DrugBank TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB TTD