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TROGLITAZONE Drug Record

  • Summary
  • Interactions
  • Claims
  • TROGLITAZONE chembl:CHEMBL408

    Alternate Names:

    TROGLITAZONE
    ROMOZIN
    GR92132X
    PRELAY
    REZULIN
    CS-045
    GR-92132X
    CI-991
    REZULIN®
    REZULIN (TN)
    ROMGLIZONE
    5-(4-(6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMAN-2-YLMETHOXY)BENZYL)THIAZOLIDINE-2,4-DIONE
    (+-)-ALL-RAC-5-(P-((6-HYDROXY-2,5,7,8-TETRAMETHYL-2-CHROMANYL)METHOXY)BENZYL)-2,4-THIAZOLIDINEDIONE
    rxcui:72610
    chembl:CHEMBL408
    drugbank:00197
    pubchem.compound:5591
    chemidplus:97322-87-7

    Drug Info:

    Drug Categories ugt1a6 inhibitors
    Drug Categories thiazolidinediones
    Drug Categories cytochrome p-450 cyp2c19 inhibitors
    Drug Groups approved
    Drug Groups investigational
    Drug Categories blood glucose lowering agents
    Drug Categories chromans
    Drug Categories cytochrome p-450 cyp2b6 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2c9 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp3a5 inhibitors
    Drug Categories cytochrome p-450 cyp3a5 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a7 inhibitors
    Drug Categories cytochrome p-450 cyp3a7 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories oatp1b1/slco1b1 inhibitors
    Drug Categories ugt1a1 substrates
    Drug Categories ugt1a3 substrates
    Drug Categories ugt1a4 substrates
    Drug Categories ugt1a6 substrate
    Drug Categories ugt1a9 substrates
    Drug Categories ugt2b7 substrates
    (4 More Sources)

    Publications:

    Cominacini et al., 1999, The expression of adhesion molecules on endothelial cells is inhibited by troglitazone through its antioxidant activity., Cell Adhes. Commun.
    Hoang MH et al., 2012, Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells., Bioorg Med Chem Lett
    Kitamura et al., 1999, Peroxisome proliferator-activated receptor gamma induces growth arrest and differentiation markers of human colon cancer cells., Jpn. J. Cancer Res.
    Satoh et al., 1999, Prostaglandin J2 and its metabolites promote neurite outgrowth induced by nerve growth factor in PC12 cells., Biochem. Biophys. Res. Commun.
    Hong SS et al., 2012, Acetylenic acid analogues from the edible mushroom Chanterelle (Cantharellus cibarius) and their effects on the gene expression of peroxisome proliferator-activated receptor-gamma target genes., Bioorg Med Chem Lett
    Hiep NT et al., 2012, Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma., J Nat Prod
    Petrova et al., 1999, Cyclopentenone prostaglandins suppress activation of microglia: down-regulation of inducible nitric-oxide synthase by 15-deoxy-Delta12,14-prostaglandin J2., Proc. Natl. Acad. Sci. U.S.A.
    Baek et al., 2003, Troglitazone, a peroxisome proliferator-activated receptor gamma (PPAR gamma ) ligand, selectively induces the early growth response-1 gene independently of PPAR gamma. A novel mechanism for its anti-tumorigenic activity., J. Biol. Chem.
    Demetri et al., 1999, Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma., Proc. Natl. Acad. Sci. U.S.A.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Camp et al., 1999, PPARgamma activators down-regulate the expression of PPARgamma in 3T3-L1 adipocytes., FEBS Lett.
    MacDonald ML et al., 2006, Identifying off-target effects and hidden phenotypes of drugs in human cells., Nat Chem Biol
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Furuta et al., 2002, Troglitazone improves GLUT4 expression in adipose tissue in an animal model of obese type 2 diabetes mellitus., Diabetes Res. Clin. Pract.
    Sharma et al., 2004, Peroxisome proliferator-activated receptor gamma activation modulates cyclin D1 transcription via beta-catenin-independent and cAMP-response element-binding protein-dependent pathways in mouse hepatocytes., J. Biol. Chem.
    Watanabe et al., 2003, A study to survey susceptible genetic factors responsible for troglitazone-associated hepatotoxicity in Japanese patients with type 2 diabetes mellitus., Clin. Pharmacol. Ther.
    Nozawa et al., 2004, Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity., Drug Metab. Dispos.
    Kruszynska et al., 2000, Effects of troglitazone on blood concentrations of plasminogen activator inhibitor 1 in patients with type 2 diabetes and in lean and obese normal subjects., Diabetes
    Sobel, 1999, Insulin resistance and thrombosis: a cardiologist's view., Am. J. Cardiol.
    Nordt et al., 2000, Differential regulation by troglitazone of plasminogen activator inhibitor type 1 in human hepatic and vascular cells., J. Clin. Endocrinol. Metab.
    Kato et al., 2000, Improvement by the insulin-sensitizing agent, troglitazone, of abnormal fibrinolysis in type 2 diabetes mellitus., Metab. Clin. Exp.
    Gottschling-Zeller et al., 2000, Troglitazone reduces plasminogen activator inhibitor-1 expression and secretion in cultured human adipocytes., Diabetologia
    Wang et al., 2010, Troglitazone is an estrogen-related receptor alpha and gamma inverse agonist., Biochem. Pharmacol.
    Lewin et al., 2002, Rat liver acyl-CoA synthetase 4 is a peripheral-membrane protein located in two distinct subcellular organelles, peroxisomes, and mitochondrial-associated membrane., Arch. Biochem. Biophys.
    Lewin et al., 2001, Acyl-CoA synthetase isoforms 1, 4, and 5 are present in different subcellular membranes in rat liver and can be inhibited independently., J. Biol. Chem.
    Kim et al., 2001, Expression and characterization of recombinant rat Acyl-CoA synthetases 1, 4, and 5. Selective inhibition by triacsin C and thiazolidinediones., J. Biol. Chem.
    Yoshioka et al., 2001, Troglitazone enhances glucose uptake induced by alpha-adrenoceptor stimulation via phosphatidylinositol 3-kinase in rat heart., Clin. Exp. Pharmacol. Physiol.
    Ohta et al., 2001, Ligands for peroxisome proliferator-activated receptor gamma inhibit growth and induce apoptosis of human papillary thyroid carcinoma cells., J. Clin. Endocrinol. Metab.
    Yamanaka et al., 2007, Comparison of the antidiabetic effects of brain-derived neurotrophic factor and thiazolidinediones in obese diabetic mice., Diabetes Obes Metab
    Lappas et al., 2002, Regulation of proinflammatory cytokines in human gestational tissues by peroxisome proliferator-activated receptor-gamma: effect of 15-deoxy-Delta(12,14)-PGJ(2) and troglitazone., J. Clin. Endocrinol. Metab.
    Leung et al., 2005, Effect of thiazolidinediones on equilibrative nucleoside transporter-1 in human aortic smooth muscle cells., Biochem. Pharmacol.
    Watanabe et al., 2002, Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10., Drug Metab. Dispos.
    Yin et al., 2004, Signaling pathways involved in induction of GADD45 gene expression and apoptosis by troglitazone in human MCF-7 breast carcinoma cells., Oncogene
    Murata et al., 2000, Stimulation by eicosapentaenoic acids of leptin mRNA expression and its secretion in mouse 3T3-L1 adipocytes in vitro., Biochem. Biophys. Res. Commun.
    Piva et al., 2005, 15-Deoxy-delta 12,14-prostaglandin J2 induces apoptosis in human malignant B cells: an effect associated with inhibition of NF-kappa B activity and down-regulation of antiapoptotic proteins., Blood
    Cefalu et al., 2004, Effects of insulin sensitizers on plaque vulnerability associated with elevated lipid content in atheroma in ApoE-knockout mice., Acta Diabetol
    Patel et al., 2005, Differential modulation of COX-2 expression in A549 airway epithelial cells by structurally distinct PPAR(gamma) agonists: evidence for disparate functional effects which are independent of NF-(kappa)B and PPAR(gamma)., Cell. Signal.
    Inoue et al., 2002, Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB., Biochem. Biophys. Res. Commun.
    Boerma JS et al., 2011, Application of CYP102A1M11H as a tool for the generation of protein adducts of reactive drug metabolites., Chem Res Toxicol
  • TROGLITAZONE   ACSL4

    Interaction Score: 2.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    12147264 11319232 11319222


    Sources:
    DrugBank

  • TROGLITAZONE   GADD45A

    Interaction Score: 0.67

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15064713


    Sources:
    NCI

  • TROGLITAZONE   VCAM1

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10626906


    Sources:
    NCI

  • TROGLITAZONE   SERPINE1

    Interaction Score: 0.37

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    10871202 10418858 10770198 10831180 10768100


    Sources:
    DrugBank

  • TROGLITAZONE   UGT1A10

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12433820


    Sources:
    NCI

  • TROGLITAZONE   GSTT1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12732844


    Sources:
    PharmGKB

  • TROGLITAZONE   ESRRG

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:

    PMIDs:
    20298676


    Sources:
    DrugBank

  • TROGLITAZONE   ESRRA

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inverse agonist (inhibitory)

    Interaction Info:

    PMIDs:
    20298676


    Sources:
    DrugBank

  • TROGLITAZONE   LEP

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10753628


    Sources:
    NCI

  • TROGLITAZONE   SLC29A1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    15963471


    Sources:
    DrugBank

  • TROGLITAZONE   APOE

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15057551


    Sources:
    NCI

  • TROGLITAZONE   CCND1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14764597


    Sources:
    NCI

  • TROGLITAZONE   TRPM3

    Interaction Score: 0.15

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TROGLITAZONE   PPARG

    Interaction Score: 0.15

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    22579484 10076568 10222233 22342624 22424300 10200320 12475986 10097144 11752352 10214942 16680159


    Sources:
    DTC TTD DrugBank GuideToPharmacology ChemblInteractions

  • TROGLITAZONE   XIAP

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15498850


    Sources:
    NCI

  • TROGLITAZONE   GSTM1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12732844


    Sources:
    NCI

  • TROGLITAZONE   SLCO1B1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14977862


    Sources:
    NCI PharmGKB

  • TROGLITAZONE   MYC

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11344222


    Sources:
    NCI

  • TROGLITAZONE   SLC2A4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11947963


    Sources:
    NCI

  • TROGLITAZONE   GSTP1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21639118


    Sources:
    DrugBank

  • TROGLITAZONE   CXCL8

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12364456


    Sources:
    NCI

  • TROGLITAZONE   PIK3CB

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11553036


    Sources:
    NCI

  • TROGLITAZONE   BDNF

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17924870


    Sources:
    NCI

  • TROGLITAZONE   PPARA

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11779144


    Sources:
    DrugBank

  • TROGLITAZONE   PIK3CG

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15993751


    Sources:
    NCI

  • TROGLITAZONE   ALOX15B

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TROGLITAZONE   PPARD

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11779144


    Sources:
    DrugBank

  • TROGLITAZONE   NR1I2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TROGLITAZONE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TROGLITAZONE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TROGLITAZONE   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TROGLITAZONE   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TROGLITAZONE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TROGLITAZONE   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB00197

    • Version: 5.1.7

    Alternate Names:
    TROGLITAZONE DrugBank Drug Name
    97322-87-7 CAS Number
    Noscal Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Wang et al., 2010, Troglitazone is an estrogen-related receptor alpha and gamma inverse agonist., Biochem. Pharmacol.
    Kruszynska et al., 2000, Effects of troglitazone on blood concentrations of plasminogen activator inhibitor 1 in patients with type 2 diabetes and in lean and obese normal subjects., Diabetes
    Sobel, 1999, Insulin resistance and thrombosis: a cardiologist's view., Am. J. Cardiol.

  • NCI: TROGLITAZONE

    • Version: 14-September-2017

    Alternate Names:
    C1522 NCI drug code

    Drug Info:

    Publications:
    Cominacini et al., 1999, The expression of adhesion molecules on endothelial cells is inhibited by troglitazone through its antioxidant activity., Cell Adhes. Commun.
    Furuta et al., 2002, Troglitazone improves GLUT4 expression in adipose tissue in an animal model of obese type 2 diabetes mellitus., Diabetes Res. Clin. Pract.
    Piva et al., 2005, 15-Deoxy-delta 12,14-prostaglandin J2 induces apoptosis in human malignant B cells: an effect associated with inhibition of NF-kappa B activity and down-regulation of antiapoptotic proteins., Blood

  • DTC: TROGLITAZONE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL408 ChEMBL Drug ID

    Drug Info:

    Publications:
    Hoang MH et al., 2012, Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells., Bioorg Med Chem Lett
    Hong SS et al., 2012, Acetylenic acid analogues from the edible mushroom Chanterelle (Cantharellus cibarius) and their effects on the gene expression of peroxisome proliferator-activated receptor-gamma target genes., Bioorg Med Chem Lett
    Hiep NT et al., 2012, Polyhydroxylated macrolides from Seimatosporium discosioides and their effects on the activation of peroxisome proliferator-activated receptor gamma., J Nat Prod

  • PharmGKB: troglitazone

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Watanabe et al., 2003, A study to survey susceptible genetic factors responsible for troglitazone-associated hepatotoxicity in Japanese patients with type 2 diabetes mellitus., Clin. Pharmacol. Ther.
    Nozawa et al., 2004, Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity., Drug Metab. Dispos.

  • TTD: Troglitazone

    • Version: 2020.06.01

    Alternate Names:
    D06XZW TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 135651283

    • Version: 29-September-2020

    Alternate Names:
    TROGLITAZONE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL408

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL408

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21