N-氨酰基-O-4-硝基苯甲酰异羟肟酸酯对氨肽酶的抑制作用。

Inhibition of aminopeptidases by N-aminoacyl-O-4-nitrobenzoyl hydroxamates.

作者信息

Demuth H U, Stöckel A, Schierhorn A, Fittkau S, Kirschke H, Brömme D

机构信息

Department of Biochemistry and Biotechnology, Martin-Luther-University, Halle, Germany.

出版信息

Biochim Biophys Acta. 1993 Oct 6;1202(2):265-70. doi: 10.1016/0167-4838(93)90014-i.

DOI:10.1016/0167-4838(93)90014-i

PMID:8399389

Abstract

10 N-aminoacyl-O-4-nitrobenzoyl hydroxamates were investigated as potential inhibitors of aminopeptidases. While the metal-depending enzymes aminopeptidase M, aminopeptidase P and leucine aminopeptidase were inhibited reversibly by the compounds, the thiol enzyme cathepsin H was inhibited efficiently in time-dependent reactions according to its substrate specificity. N-phenylalanyl-O-4-nitrobenzoyl hydroxamate was shown to be most effective, exhibiting a second-order-rate constant of inhibition of 31,766 M-1 s-1.

摘要

对10种N-氨酰基-O-4-硝基苯甲酰异羟肟酸酯作为氨肽酶潜在抑制剂进行了研究。虽然金属依赖性酶氨肽酶M、氨肽酶P和亮氨酸氨肽酶被这些化合物可逆抑制，但硫醇酶组织蛋白酶H根据其底物特异性在时间依赖性反应中被有效抑制。N-苯丙氨酰基-O-4-硝基苯甲酰异羟肟酸酯被证明是最有效的，其二级抑制速率常数为31,766 M-1 s-1。