囊泡中磷脂酶A2的竞争性抑制作用。
Competitive inhibition of phospholipase A2 in vesicles.
作者信息
Jain M K, Yuan W, Gelb M H
机构信息
Department of Chemistry and Biochemistry, University of Delaware, Newark 19716.
出版信息
Biochemistry. 1989 May 16;28(10):4135-9. doi: 10.1021/bi00436a002.
Abstract
Kinetic studies with phospholipase A2 are complicated by the fact that binding of the enzyme to the interface precedes catalytic turnover. This difficulty can be overcome by monitoring interfacial catalysis in the scooting mode where the enzyme does not leave the interface. The kinetics of inhibition by transition-state analogues shows that specific competitive inhibition is the result of competition between inhibitor and substrate for the binding to the active site of the enzyme in the interface. Several lipophilic compounds, including alkanols, substituted butyrophenones, aristolochic acid, and mepacrine apparently reduce the rate of lipolysis by promoting the desorption of phospholipase A2 from the interface.
摘要
磷脂酶A2的动力学研究因酶与界面的结合先于催化周转这一事实而变得复杂。通过在“滑动”模式下监测界面催化可以克服这一困难，在该模式下酶不会离开界面。过渡态类似物的抑制动力学表明，特异性竞争性抑制是抑制剂与底物竞争结合界面处酶活性位点的结果。几种亲脂性化合物，包括链烷醇、取代丁酰苯、马兜铃酸和米帕林，显然通过促进磷脂酶A2从界面解吸来降低脂解速率。
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