用N-肽基-O-酰基羟胺对半胱氨酸蛋白酶进行有效且选择性的失活处理。
Potent and selective inactivation of cysteine proteinases with N-peptidyl-O-acyl hydroxylamines.
作者信息
Brömme D, Schierhorn A, Kirschke H, Wiederanders B, Barth A, Fittkau S, Demuth H U
机构信息
Institute of Biochemistry, Medical Faculty, Martin-Luther-University, Halle, German Democratic Republic.
出版信息
Biochem J. 1989 Nov 1;263(3):861-6. doi: 10.1042/bj2630861.
Abstract
A series of N-peptidyl-O-acyl hydroxylamines was synthesized and tested as inactivators of cysteine proteinases. Depending on the structure of the peptidyl residue of the inhibitors, rapid and complete irreversible inactivation of the lysosomal cathepsins, B, L and S, may be achieved. The most effective inhibitors display second-order rate constants of the inactivation in the range 10(5)-10(6) M-1.s-1. By contrast, the activity of the aminoendopeptidase cathepsin H is only negligibly affected by the N-terminal-protected peptidyl inhibitors.
摘要
合成了一系列N-肽基-O-酰基羟胺，并作为半胱氨酸蛋白酶的失活剂进行了测试。根据抑制剂肽基残基的结构，可以实现溶酶体组织蛋白酶B、L和S的快速、完全不可逆失活。最有效的抑制剂的失活二级速率常数在10(5)-10(6) M-1.s-1范围内。相比之下，氨基端肽酶组织蛋白酶H的活性仅受到N端保护的肽基抑制剂的轻微影响。
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