General Information of Drug-Metabolizing Enzyme (DME ID: DME0018)
DME Name Cytochrome P450 2C8 (CYP2C8), Homo sapiens DME Info
UniProt ID
CP2C8_HUMAN
EC Number    EC: 1.14.14.1     (Click to Show/Hide the Complete EC Tree)
Oxidoreductase
Oxygen paired donor oxidoreductase
Flavin/flavoprotein donor oxidoreductase
EC: 1.14.14.1
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Interactome
Interactions between Xenobiotics and DME (XEOTIC)
      Fungicide(s), Herbicide(s) or Insecticide(s)
                  Herbicide Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Clofibric acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01257   XEOTIC Info Gene Form Protein
                                 Classification Herbicide
                                 DME Modulation Clofibric acid induces the drug-metabolizing activity of DME CYP2C8 [1]
                  Pesticide/Insecticide Click to Show/Hide the Full List of Xenobiotics:        4 Xenobiotics
                              Cypermethrin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01046   XEOTIC Info Gene Form mRNA
                                 Classification Pesticide/Insecticide
                                 DME Modulation Cypermethrin up-regulates the expression of DME CYP2C8 [2]
                              Decamethrin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01047   XEOTIC Info Gene Form mRNA
                                 Classification Pesticide/Insecticide
                                 DME Modulation Decamethrin up-regulates the expression of DME CYP2C8 [2]
                              Fenitrothion Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01052   XEOTIC Info Gene Form Protein
                                 Classification Pesticide/Insecticide
                                 DME Modulation Fenitrothion inhibits the drug-metabolizing activity of DME CYP2C8 [3]
                              Fenvalerate Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01053   XEOTIC Info Gene Form mRNA
                                 Classification Pesticide/Insecticide
                                 DME Modulation Fenvalerate up-regulates the expression of DME CYP2C8 [2]
      Health or Environmental Toxicant(s)
                  Acute Toxic Substance Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Fipronil Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01302   XEOTIC Info Gene Form mRNA
                                 Classification Acute Toxic Substance
                                 DME Modulation Fipronil up-regulates the expression of DME CYP2C8 [4]
                  Biotoxin Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Cylindrospermopsin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00905   XEOTIC Info Gene Form mRNA
                                 Classification Cyanotoxin
                                 DME Modulation Cylindrospermopsin inhibits the expression of DME CYP2C8 [5]
                  Carcinogen Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Aflatoxin B1 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00806   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen-mycotoxin
                                 DME Modulation Aflatoxin B1 inhibits the expression of DME CYP2C8 [6], [7]
                  Health Hazard/Toxicant Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Perfluorooctane sulfonic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00921   XEOTIC Info Gene Form mRNA
                                 Classification Health and Environmental Toxicant
                                 DME Modulation Perfluorooctane sulfonic acid up-regulates the expression of DME CYP2C8 [8]
      Natural Product(s), Extract(s) or Medicine(s)
                  Natural Product Click to Show/Hide the Full List of Xenobiotics:        5 Xenobiotics
                              15,16-dihydrotanshinone I Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01517   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation 15,16-dihydrotanshinone I inhibits the drug-metabolizing activity of DME CYP2C8 [9]
                              Diosmetin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01281   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Diosmetin inhibits the drug-metabolizing activity of DME CYP2C8 [10]
                              Puag-haad Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01442   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Puag-haad inhibits the drug-metabolizing activity of DME CYP2C8 [11]
                              Salvianolic acid C Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00861   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Salvianolic acid C inhibits the drug-metabolizing activity of DME CYP2C8 [12]
                              Walrycin A Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01498   XEOTIC Info Gene Form mRNA
                                 Classification Natural Product
                                 DME Modulation Walrycin A up-regulates the expression of DME CYP2C8 [13]
      Pharmaceutical Agent(s)
                  Approved/Marketed Drug Click to Show/Hide the Full List of Xenobiotics:      45 Xenobiotics
                              Acetaminophen Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00217   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Acetaminophen inhibits the expression of DME CYP2C8 [14]
                              Amiodarone hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00277   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Amiodarone hydrochloride inhibits the drug-metabolizing activity of DME CYP2C8 (Ki = 1.5 microM) [15]
                              Amoxicillin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00246   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Amoxicillin inhibits the drug-metabolizing activity of DME CYP2C8 [16]
                              Candesartan cilexetil Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00236   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Candesartan cilexetil inhibits the drug-metabolizing activity of DME CYP2C8 [17]
                              Carbamazepine Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00011   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Carbamazepine up-regulates the expression of DME CYP2C8 [18]
                              Clotrimazole Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00017   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Clotrimazole inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 0.803 microM) [19]
                              Cocaine hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00751   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Cocaine hydrochloride inhibits the drug-metabolizing activity of DME CYP2C8 [20]
                              Cyclosporine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00241   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Cyclosporine inhibits the expression of DME CYP2C8 [21]
                              Dexamethasone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00088   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Dexamethasone up-regulates the expression of DME CYP2C8 [22], [23]
                              Estradiol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00090   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Estradiol inhibits the expression of DME CYP2C8 [21]
                              Ethinyl estradiol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00267   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Ethinyl estradiol inhibits the drug-metabolizing activity of DME CYP2C8 [17]
                              Felodipine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00245   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Felodipine inhibits the drug-metabolizing activity of DME CYP2C8 [17], [24]
                              Fenofibrate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00035   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Fenof DMEibrate inhibits the drug-metabolizing activity of DME CYP2C8 [17]
                              Fenofibric acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00138   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Fenofibric acid induces the drug-metabolizing activity of DME CYP2C8 [1]
                              Fluoxetine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00358   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Fluoxetine inhibits the drug-metabolizing activity of DME CYP2C8 (Ki = 294 microM) [15]
                              Gemfibrozil Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00042   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Gemfibrozil inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 4.1 microM) [25]
                              Irbesartan Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00249   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Irbesartan inhibits the drug-metabolizing activity of DME CYP2C8 [17]
                              Isoniazid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00224   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Isoniazid inhibits the drug-metabolizing activity of DME CYP2C8 (Ki = 170 microM) [15]
                              Ketoconazole Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00251   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Ketoconazole inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 2.45 microM) [19]
                              Loratadine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00055   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Loratadine inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 2.95 microM) [19]
                              Lovastatin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00262   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Lovastatin inhibits the drug-metabolizing activity of DME CYP2C8 [26], [27]
                              Medroxyprogesterone acetate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00743   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Medroxyprogesterone acetate inhibits the drug-metabolizing activity of DME CYP2C8 [28]
                              Mometasone furoate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00162   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Mometasone furoate inhibits the drug-metabolizing activity of DME CYP2C8 [29]
                              Montelukast Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00368   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Montelukast inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 1 microM) [30]
                              Nicardipine hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00311   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Nicardipine hydrochloride inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 1.56 microM) [19]
                              Nortriptyline hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00313   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Nortriptyline hydrochloride inhibits the drug-metabolizing activity of DME CYP2C8 (Ki = 49.9 microM) [15]
                              Pazopanib Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00374   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Pazopanib up-regulates the expression of DME CYP2C8 [31]
                              Phenelzine sulfate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00318   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Phenelzine sulfate inhibits the drug-metabolizing activity of DME CYP2C8 (Ki = 1.2 microM) [15]
                              Phenobarbital Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00410   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Phenobarbital induces the drug-metabolizing activity of DME CYP2C8 [32]
                              Pioglitazone hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00319   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Pioglitazone hydrochloride inhibits the expression of DME CYP2C8 [33]
                              Piperacillin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00375   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Piperacillin inhibits the drug-metabolizing activity of DME CYP2C8 [34]
                              Raloxifene hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00126   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Raloxifene hydrochloride inhibits the expression of DME CYP2C8 [35]
                              Rifampin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00223   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Rifampin up-regulates the expression of DME CYP2C8 and leads to increasing the drug-metabolizing activity of this enzyme [36], [37]
                              Salmeterol xinafoate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00128   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Salmeterol xinafoate inhibits the drug-metabolizing activity of DME CYP2C8 [38]
                              Simvastatin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00125   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Simvastatin inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 3.7 microM) [19]
                              Spironolactone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00266   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Spironolactone inhibits the expression of DME CYP2C8 [39]
                              Sulfinpyrazone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00081   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Sulfinpyrazone inhibits the drug-metabolizing activity of DME CYP2C8 [40]
                              Tamoxifen Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00383   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Tamoxifen inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 14.3 microM) [19]
                              Trimethoprim Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00263   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Trimethoprim inhibits the expression of DME CYP2C8 [41], [33]
                              Troglitazone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00086   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Troglitazone up-regulates the expression of DME CYP2C8 [42]
                              Valproic acid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00029   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Valproic acid inhibits the expression of DME CYP2C8 [43]
                              Verapamil Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00387   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Verapamil inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 > 30 microM) [19]
                              Zafirlukast Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00087   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Zafirlukast inhibits the expression of DME CYP2C8 [44]
                              Bezafibrate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00493   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Bezafibrate inhibits the drug-metabolizing activity of DME CYP2C8 [45]
                              Cinnamic acid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01252   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Cinnamic acid inhibits the drug-metabolizing activity of DME CYP2C8 [38]
                  Drug in Phase 3 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        4 Xenobiotics
                              Afimoxifene Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00610   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Afimoxifene inhibits the drug-metabolizing activity of DME CYP2C8 [46]
                              Diethyltoluamide Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00582   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Diethyltoluamide up-regulates the expression of DME CYP2C8 [4]
                              Endoxifen Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00671   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Endoxifen inhibits the drug-metabolizing activity of DME CYP2C8 [46]
                              Satraplatin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00663   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Satraplatin inhibits the expression of DME CYP2C8 [47]
                  Drug in Phase 2 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        5 Xenobiotics
                              Butyric acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01230   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2/3
                                 DME Modulation Butyric acid up-regulates the expression of DME CYP2C8 [48]
                              Bisphenol A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01226   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Bisphenol A inhibits the drug-metabolizing activity of DME CYP2C8 [49]
                              Camptothecin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00597   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Camptothecin inhibits the expression of DME CYP2C8 [50]
                              MeIQx Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00609   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation MeIQx inhibits the expression of DME CYP2C8 [51]
                              Silibinin B Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00686   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation Silibinin B inhibits the drug-metabolizing activity of DME CYP2C8 [52]
                  Drug in Phase 1 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Licochalcone A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01365   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 1
                                 DME Modulation Licochalcone A inhibits the drug-metabolizing activity of DME CYP2C8 [53]
                              Quercetin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00538   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 1
                                 DME Modulation Quercetin inhibits the drug-metabolizing activity of DME CYP2C8 (IC50 = 1.2 microM) [54]
                  Preclinical/Patented Drug Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              CP-778875 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01156   XEOTIC Info Gene Form Protein
                                 Classification Drug in Preclinical Study
                                 DME Modulation CP-778875 inhibits the drug-metabolizing activity of DME CYP2C8 [55]
                  Investigative Agent Click to Show/Hide the Full List of Xenobiotics:        3 Xenobiotics
                              5-fluorotryptamine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01159   XEOTIC Info Gene Form Protein
                                 Classification Investigative Agent
                                 DME Modulation 5-fluorotryptamine inhibits the drug-metabolizing activity of DME CYP2C8 [56]
                              CITCO Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01165   XEOTIC Info Gene Form mRNA
                                 Classification Investigative Agent
                                 DME Modulation CITCO up-regulates the expression of DME CYP2C8 [22]
                              DY-9760e Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01130   XEOTIC Info Gene Form Protein
                                 Classification Investigative Agent
                                 DME Modulation DY-9760e inhibits the drug-metabolizing activity of DME CYP2C8 [57]
References
1 Comparative effects of fibrates on drug metabolizing enzymes in human hepatocytes. Pharm Res. 2005 Jan;22(1):71-8.
2 Characterization of human cytochrome P450 induction by pesticides. Toxicology. 2012 Mar 29;294(1):17-26.
3 An evaluation of the cytochrome P450 inhibition potential of selected pesticides in human hepatic microsomes. J Environ Sci Health B. 2009 Aug;44(6):553-63.
4 Impact of environmental chemicals on the transcriptome of primary human hepatocytes: potential for health effects. J Biochem Mol Toxicol. 2016 Aug;30(8):375-95.
5 Identification of key pathways involved in the toxic response of the cyanobacterial toxin cylindrospermopsin in human hepatic HepaRG cells. Toxicol In Vitro. 2019 Aug;58:69-77.
6 Identification of early target genes of aflatoxin B1 in human hepatocytes, inter-individual variability and comparison with other genotoxic compounds. Toxicol Appl Pharmacol. 2012 Jan 15;258(2):176-87.
7 Aflatoxin B1 induces persistent epigenomic effects in primary human hepatocytes associated with hepatocellular carcinoma. Toxicology. 2016 Mar 28;350-352:31-9.
8 Cytotoxicity and gene expression profiling of two hydroxylated polybrominated diphenyl ethers in human H295R adrenocortical carcinoma cells. Toxicol Lett. 2009 Feb 25;185(1):23-31.
9 Inhibitory effects of Danshen components on CYP2C8 and CYP2J2. Chem Biol Interact. 2018 Jun 1;289:15-22.
10 Effects of diosmetin on nine cytochrome P450 isoforms, UGTs and three drug transporters in vitro. Toxicol Appl Pharmacol. 2017 Nov 1;334:1-7.
11 Effect of the interaction between lipoxygenase pathway and progesterone on the regulation of hydroxysteroid 11-Beta dehydrogenase 2 in cultured human term placental trophoblasts. Biol Reprod. 2008 Mar;78(3):514-20.
12 Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs. ACS Med Chem Lett. 2011 Oct 15;3(1):39-42.
13 Gene expression changes in human lung cells exposed to arsenic, chromium, nickel or vanadium indicate the first steps in cancer. Metallomics. 2012 Aug;4(8):784-93.
14 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
15 Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr Drug Metab. 2005 Oct;6(5):413-54.
16 Effect of penicillin-based antibiotics, amoxicillin, ampicillin, and piperacillin, on drug-metabolizing activities of human hepatic cytochromes P450. J Toxicol Sci. 2016 Feb;41(1):143-6.
17 Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78.
18 Transcriptional profiling of genes induced in the livers of patients treated with carbamazepine. Clin Pharmacol Ther. 2006 Nov;80(5):440-456.
19 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.
20 Down-regulation of astroglial CYP2C, glucocorticoid receptor and constitutive androstane receptor genes in response to cocaine in human U373 MG astrocytoma cells. Toxicol Lett. 2005 Dec 15;159(3):203-11.
21 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
22 Human CYP2C8 is transcriptionally regulated by the nuclear receptors constitutive androstane receptor, pregnane X receptor, glucocorticoid receptor, and hepatic nuclear factor 4alpha. Mol Pharmacol. 2005 Sep;68(3):747-57.
23 Use of mRNA expression to detect the induction of drug metabolising enzymes in rat and human hepatocytes. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):86-96.
24 In vitro toxicological evaluation of NCS-382, a high-affinity antagonist of gama-hydroxybutyrate (GHB) binding. Toxicol In Vitro. 2017 Apr;40:196-202.
25 Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. J Med Chem. 2012 Jun 14;55(11):4896-933.
26 Retinaldehyde is a substrate for human aldo-keto reductases of the 1C subfamily. Biochem J. 2011 Dec 15;440(3):335-44.
27 Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone. Chem Biol Interact. 2003 Feb 1;143-144:503-13.
28 Interaction of bispyridinium compounds with the orthosteric binding site of human alpha7 and Torpedo californica nicotinic acetylcholine receptors (nAChRs). Toxicol Lett. 2011 Sep 25;206(1):100-4.
29 Mitotane alters mitochondrial respiratory chain activity by inducing cytochrome c oxidase defect in human adrenocortical cells. Endocr Relat Cancer. 2013 May 21;20(3):371-81.
30 Novel terminal bipheny-based diapophytoene desaturases (CrtN) inhibitors as anti-MRSA/VISR/LRSA agents with reduced hERG activity. J Med Chem. 2018 Jan 11;61(1):224-250.
31 Environmental pollutants parathion, paraquat and bisphenol A show distinct effects towards nuclear receptors-mediated induction of xenobiotics-metabolizing cytochromes P450 in human hepatocytes. Toxicol Lett. 2015 Oct 1;238(1):43-53.
32 High perfluorooctanoic acid exposure induces autophagy blockage and disturbs intracellular vesicle fusion in the liver. Arch Toxicol. 2017 Jan;91(1):247-258.
33 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
34 Inhibition of monoamine oxidase activity by phenylpropanolamine, an anorectic agent. Res Commun Chem Pathol Pharmacol. 1986 Feb;51(2):163-71.
35 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
36 Induction of quinone reductase NQO1 by resveratrol in human K562 cells involves the antioxidant response element ARE and is accompanied by nuclear translocation of transcription factor Nrf2. Med Chem. 2006 May;2(3):275-85.
37 Prevention of estrogen-DNA adduct formation in MCF-10F cells by resveratrol. Free Radic Biol Med. 2008 Jul 15;45(2):136-45.
38 Cinnamic acid based thiazolidinediones inhibit human P450c17 and 3beta-hydroxysteroid dehydrogenase and improve insulin sensitivity independent of PPARgamma agonist activity. J Mol Endocrinol. 2004 Apr;32(2):425-36.
39 Identification of human cell responses to hexavalent chromium. Environ Mol Mutagen. 2007 Oct;48(8):650-7.
40 The oximes HI-6 and MMB-4 fail to reactivate soman-inhibited human and guinea pig AChE: a kinetic in vitro study. Toxicol Lett. 2018 Sep 1;293:216-221.
41 From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
42 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
43 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
44 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
45 Expression of cytochrome P450 epoxygenases and soluble epoxide hydrolase is regulated by hypolipidemic drugs in dose-dependent manner. Toxicol Appl Pharmacol. 2018 Sep 15;355:156-163.
46 The formation of estrogen-like tamoxifen metabolites and their influence on enzyme activity and gene expression of ADME genes. Arch Toxicol. 2018 Mar;92(3):1099-1112.
47 Toxicity, recovery, and resilience in a 3D dopaminergic neuronal in vitro model exposed to rotenone. Arch Toxicol. 2018 Aug;92(8):2587-2606.
48 Butyrate interacts with benzo[a]pyrene to alter expression and activities of xenobiotic metabolizing enzymes involved in metabolism of carcinogens within colon epithelial cell models. Toxicology. 2019 Jan 15;412:1-11.
49 Inhibition of drug-metabolizing enzyme activity in human hepatic cytochrome P450s by bisphenol A. Biol Pharm Bull. 2000 Apr;23(4):498-501.
50 Identification of approved drugs as potent inhibitors of pregnane X receptor activation with differential receptor interaction profiles. Arch Toxicol. 2018 Apr;92(4):1435-1451.
51 Preferential induction of the AhR gene battery in HepaRG cells after a single or repeated exposure to heterocyclic aromatic amines. Toxicol Appl Pharmacol. 2010 Nov 15;249(1):91-100.
52 The effect of milk thistle (Silybum marianum) and its main flavonolignans on CYP2C8 enzyme activity in human liver microsomes. Chem Biol Interact. 2017 Jun 1;271:24-29.
53 Inhibition of human cytochrome P450 enzymes by licochalcone A, a naturally occurring constituent of licorice. Toxicol In Vitro. 2015 Oct;29(7):1569-76.
54 Discovery of GBT440, an orally bioavailable R-state stabilizer of sickle cell hemoglobin. ACS Med Chem Lett. 2017 Jan 23;8(3):321-326.
55 Elucidation of the biochemical basis for a clinical drug-drug interaction between atorvastatin and 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha. Xenobiotica. 2013 Nov;43(11):963-72.
56 Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class. Toxicol Lett. 2016 Jan 22;241:82-94.
57 In vitro metabolism of the calmodulin antagonist DY-9760e (3-[2-[4-(3-chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride 3.5 hydrate) by human liver microsomes: involvement of cytochromes p450 in atypical kinetics and potential drug interactions. Drug Metab Dispos. 2005 Nov;33(11):1628-36.

If you find any error in data or bug in web service, please kindly report it to Dr. Yin and Dr. Li.