Title : Evaluation of 89 compounds for identification of substrates for cynomolgus monkey CYP2C76, a new bupropion/nifedipine oxidase.

Pub. Date : 2015 Jan

PMID : 25318994






5 Functional Relationships(s)
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1 Among them, bupropion and nifedipine showed high selectivity to CYP2C76. Nifedipine cytochrome P450 family 2 subfamily C member 76 Macaca fascicularis
2 As for nifedipine, CYP2C76 formed methylhydroxylated nifedipine, which was not produced by monkey CYP2C9, CYP2C19, or CYP3A4, as identified by mass spectrometry and estimated by a molecular docking simulation. Nifedipine cytochrome P450 family 2 subfamily C member 76 Macaca fascicularis
3 As for nifedipine, CYP2C76 formed methylhydroxylated nifedipine, which was not produced by monkey CYP2C9, CYP2C19, or CYP3A4, as identified by mass spectrometry and estimated by a molecular docking simulation. Nifedipine cytochrome P450 family 2 subfamily C member 76 Macaca fascicularis
4 This unique oxidative metabolite formation of nifedipine could be one of the selective marker reactions of CYP2C76 among the major CYP2Cs and CYP3As tested. Nifedipine cytochrome P450 family 2 subfamily C member 76 Macaca fascicularis
5 These results suggest that monkey CYP2C76 contributes to bupropion hydroxylation and formation of different nifedipine oxidative metabolites as a result of its relatively large substrate cavity. Nifedipine cytochrome P450 family 2 subfamily C member 76 Macaca fascicularis