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首页> 外文期刊>Drug discovery today >Implications of the allosteric kinetics of cytochrome P450s.
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Implications of the allosteric kinetics of cytochrome P450s.

机译：细胞色素P450的变构动力学的影响。

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摘要

Drug metabolites can uniquely contribute to therapeutic efficacy, toxicity and drug-drug interactions. Therefore, the rates of formation and clearance of each metabolite are crucially important parameters in the net therapeutic profile of new drugs. However, the recent appreciation for the importance of drug metabolism has made it apparent that the understanding of the fundamental kinetic and biophysical properties of the enzymes that are responsible for catalyzing these reactions, the cytochrome P450s, is incomplete. The need to fully comprehend the complex allosteric behavior of these enzymes has fostered increased scrutiny of cytochrome P450s, which has subsequently resulted in major changes in the way that these enzymes are perceived at the molecular level.
机译：药物代谢产物可以独特地促进治疗功效，毒性和药物-药物相互作用。因此，每种代谢产物的形成和清除速率是新药净治疗谱中至关重要的重要参数。但是，最近对药物代谢重要性的认识使人们很清楚，对负责催化这些反应的酶（细胞色素P450s）的基本动力学和生物物理特性的理解还不完全。全面了解这些酶的复杂变构行为的需要促进了对细胞色素P450的严格审查，这随后导致在分子水平上感知这些酶的方式发生了重大变化。

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