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首页> 外文期刊>Catalysis science & technology >Engineering P450(LaMO) stereospecificity and product selectivity for selective C-H oxidation of tetralin-like alkylbenzenes
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Engineering P450(LaMO) stereospecificity and product selectivity for selective C-H oxidation of tetralin-like alkylbenzenes

机译：工程P450(拉莫)定向性产品选择性氧化碳氢键的选择性的tetralin-like烷基苯

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摘要

The P450-mediated asymmetric hydroxylation of inert C-H bonds is a chemically challenging reaction. Self-sufficient P450(LaMO) from the CYP116B subfamily could catalyze the transformation of 1,2,3,4-tetrahydronaphthalene to (S)-tetralol, despite its poor enantioselectivity (er 66:34) and product selectivity (the ratio of alcohol and ketone, ak, 76:24). To improve the selectivity, phenylalanine scanning and further protein engineering were performed to reshape the active pocket of P450(LaMO), resulting in a mutant (T121V/Y385F/M391L) with not only improved (S)-enantioselectivity (er 98:2) but also excellent product selectivity (ak 99:1), in contrast to another mutant L97F/T121F/E282V/T283Y with complementary (R)-enantioselectivity (er 23:77). Moreover, the enantiopure (S)-alcohols formed by the P450(LaMO)-catalyzed oxidation of a series of alkylbenzenes are potentially important building blocks in the pharmaceutical industry. This Phe-based enantioselectivity engineering used for reshaping the active pocket of P450s could provide a guide to the protein evolution of other CYP116B members.
机译：P450-mediated不对称羟基化的惰性碳氢键是一个化学具有挑战性的反应。CYP116B亚科可以催化转换的1、2、3,4-tetrahydronaphthalene(年代)-tetralol,尽管它贫穷选择性(er 66:34)和产品选择性(酒精和酮的比例、正义与发展党76:24)。扫描和进一步的蛋白质工程进行重塑的活性口袋P450(拉莫),导致突变(T121V / Y385F / M391L)不仅改善(S)选择性(er 98:2)也优秀的产品选择性(ak 99:1)对比另一个突变L97F / T121F / E282V / T283Y与互补(R)选择性(er23:77)。由P450(拉莫)的催化氧化一系列烷基苯是潜在的重要的构建块在制药行业。这Phe-based选择性工程用于重塑p450酶类的活性口袋可以提供一个指导蛋白质的进化其他CYP116B成员。

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