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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Methoxyresorufin是荧光CYP450底物(fluorometric CYP450 substrate)。
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Mephenytoin是CYP2C19 底物。 抗惊厥剂。
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Itraconazole 是一种三唑类抗真菌药物。
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Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
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Abiraterone是一种有效的类固醇细胞色素P450 17alpha-羟化酶-17, 20-裂解酶(CYP17)抑制剂,IC50为2 nM;对前列腺癌有活性。
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