底物特异性、监管和多态性的人类细胞色素P450 2 b6。

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莫SL,刘本段W,魏MQ, Kanwar JR,周科幻

底物特异性、监管和多态性的人类细胞色素P450 2 b6。

咕咕叫药物金属底座。2009年9月,10(7):730 - 53年。

PubMed ID

19702527 (在PubMed

]

文摘

CYP2B6主要表达在肝脏被认为历史上人类药物代谢中扮演微不足道的角色。然而,增加的兴趣已经激发了这种酶多态和种族差异的发现CYP2B6表达式,为CYP2B6识别额外的基质,对CYP3A4 co-regulation证据。本文更新我们的知识的结构、功能、调节和CYP2B6多态性。beplayappCYP2B6可以代谢大约8%的临床使用药物(n > 60岁),包括环磷酰胺、异环磷酰胺,三苯氧胺,氯胺酮,青蒿素,奈韦拉平,依法韦伦,安非他酮,西布曲明,异丙酚。CYP2B6是CYP酶bioactivate几个前致癌物和毒物。这种酶代谢花生四烯酸、月桂酸、17个beta雌二醇,雌素酮,乙炔雌二醇和睾酮。CYP2B6 non-planar分子的典型基质、中性或弱碱性,高度亲脂性的与一个或两个受体形成氢键。CYP2B6尚未解决的晶体结构,而一些药效团和同源性模型的人类CYP2B6报告。人类CYP2B6密切监管本构雄烷受体(汽车/ NR1I3)可以激活CYP2B6表达式在配体结合。孕烷X受体和糖皮质激素受体在CYP2B6的规定也扮演了一定的角色。 Induction of CYP2B6 may partially explain some clinical drug interactions observed. For example, coadministered carbamazepine decreases the systemic exposure of bupropion. There is a wide interindividual variability in the expression and activity of CYP2B6. Such a large variability is probably due to effects of genetic polymorphisms and exposure to drugs that are inducers or inhibitors of CYP2B6. To date, at least 28 allelic variants and some subvariants of CYP2B6 (*1B through *29) have been described and some of them have been shown to have important functional impact on drug clearance and drug response. For example, the efavirenz plasma levels in African-American subjects with the CYP2B6 homozygous 516T/T genotype are approximately 3-fold higher than individuals carrying the homozygous G/G genotype. The CYP2B6 516T/T genotype is associated with 1.7-fold greater plasma levels of nevirapine in HIV-infected patients. Smokers with the 1459C>T (R487C) variant of CYP2B6 may be more vulnerable to abstinence symptoms and relapse following treatment with bupropion as a smoking cessation agent. Further studies in the structure, function, regulation and polymorphism of CYP2B6 are warranted.

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药物酶

药物	酶	类	生物	药理作用	行动
雌激素酮	细胞色素P450 2 b6	蛋白质	人类	未知的	底物	细节