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1-硬脂酰基-2-硬脂酰氨基脱氧磷脂酰胆碱,一种有效的磷脂酶A2可逆抑制剂。

1-Stearyl,2-stearoylaminodeoxy phosphatidylcholine, a potent reversible inhibitor of phospholipase A2.

作者信息

Davidson F F, Hajdu J, Dennis E A

出版信息

Biochem Biophys Res Commun. 1986 Jun 13;137(2):587-92. doi: 10.1016/0006-291x(86)91118-6.

Abstract

1-stearyl, 2-stearoylaminodeoxy phosphatidylcholine, a structurally modified phospholipid substrate analog exhibits potent and reversible inhibition of phospholipase A2 from cobra venom (N. naja naja). The apparent KI values determined in two different assay systems employing phosphatidylcholine-surfactant mixed micelles are in reasonable agreement (40 microM and 16 microM) and indicate that the inhibitor binds to the enzyme as much as two orders of magnitude more tightly than does dipalmitoyl phosphatidylcholine. With phosphatidylethanolamine as substrate, the kinetics are more complicated as the analog also exhibits activation, presumably at a second binding site on the enzyme.

摘要

1-硬脂酰基-2-硬脂酰氨基脱氧磷脂酰胆碱,一种结构修饰的磷脂底物类似物,对眼镜蛇毒(印度眼镜蛇)中的磷脂酶A2表现出强效且可逆的抑制作用。在使用磷脂酰胆碱-表面活性剂混合胶束的两种不同测定系统中测定的表观抑制常数(KI)值相当一致(分别为40微摩尔和16微摩尔),这表明该抑制剂与酶的结合比二棕榈酰磷脂酰胆碱紧密约两个数量级。以磷脂酰乙醇胺作为底物时,动力学更为复杂,因为该类似物还表现出激活作用,推测是在酶的第二个结合位点上。

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