Evidence for exchange of inhibitors which bind to the active site of trypsin

F.S. Steven, M.M. Griffin
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引用次数: 5

Abstract

Two classes of inhibitors of trypsin (EC 3.4.21.4) have been studied, viz. active site-directed agents such as ovomucoid and active site titrants such as 4-methylumbelliferyl-4-guanidinobenzoate. The kinetics of β-naphthylamidase inhibition by an active site-directed agent were markedly different from simultaneous assays of the availability of the active site towards active site titrants in the presence of the active site-directed agents. Analysis of these data indicated an exchange of active site-directed agent by subsequent addition of active site titrant. One class of trypsin inhibitor could be displaced by another from the trypsin active centre. Competitive chase experiments were designed to measure this exchange in which the active site-directed agent was first equilibrated with trypsin, then partially displaced by incremental additions of an active site titrant; the degree of active sites occupied by these two agents was then determined by active site titration with a second reagent.

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与胰蛋白酶活性位点结合的抑制剂交换的证据
已经研究了两类胰蛋白酶抑制剂(EC 3.4.21.4),即活性位点导向剂,如卵泡样蛋白和活性位点滴定剂,如4-甲基伞状细胞酰-4-胍基苯甲酸酯。活性位点导向剂抑制β-萘酰胺酶的动力学与活性位点导向剂存在时活性位点对活性位点滴定剂的可用性的同时测定明显不同。对这些数据的分析表明,通过随后添加活性位点滴定剂来交换活性位点导向剂。一类胰蛋白酶抑制剂可以被另一类胰蛋白酶活性中心取代。竞争性追逐实验旨在测量这种交换,其中活性位点导向剂首先与胰蛋白酶平衡,然后通过活性位点滴定剂的增量添加部分取代;然后用第二种试剂进行活性位点滴定来测定这两种试剂占据的活性位点的程度。
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