Cytochromes P450 (CYPs)
Cytochromes P450 (CYPs) are proteins of the superfamily containing heme as a cofactor and, therefore, are hemoproteins. CYPs use a variety of small and large molecules as substrates in enzymatic reactions. They are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term P450 is derived from the spectrophotometric peak at the wavelength of the absorption maximum of the enzyme (450 nm) when it is in the reduced state and complexed with carbon monoxide.Cytochrome P450, family 3, subfamily A, also known as CYP3A, is a human gene. The CYP3A locus includes all the known members of the 3A subfamily of the cytochrome P450 superfamily of genes. These genes encode monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. The CYP3A cluster consists of four genes:CYP3A4,CYP3A5,CYP3A7, and CYP3A43.
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Fluconazole是抗真菌化合物，可用于表面和全身性的真菌感染。
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PF-4981517是一种有效的，选择性的CYP3A4(P450)抑制剂，IC50为0.03 μM，比作用于CYP3A5和CYP3A7选择性高500倍以上。
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Ketoconazole (酮康唑)是咪唑类抗真菌剂，是经典的CYP3A4抑制剂。
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TAK-700 (Orteronel)是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。Phase 3。
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Piperine是一种生物碱，是造成黑胡椒和长胡椒辛辣的原因，也用于一些传统医学领域，且作为杀虫剂。
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