Title : Interaction of Human Drug-Metabolizing CYP3A4 with Small Inhibitory Molecules.

Pub. Date : 2019 Feb 19

PMID : 30676743






3 Functional Relationships(s)
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1 This study investigated the interaction of recombinant CYP3A4 with a nonspecific inhibitor metyrapone, antifungal drug fluconazole, and protease inhibitor phenylmethanesulfonyl fluoride (PMSF). Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Metyrapone and fluconazole are classic type II ligands that inhibit CYP3A4 with medium strength by ligating to the heme iron, whereas PMSF, lacking the heme-ligating moiety, acts as a weak type I ligand and inhibitor of CYP3A4. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens