脊椎动物胶原酶抑制剂。I. 三肽基异羟肟酸。

Vertebrate collagenase inhibitor. I. Tripeptidyl hydroxamic acids.

作者信息

Odake S, Okayama T, Obata M, Morikawa T, Hattori S, Hori H, Nagai Y

机构信息

Research Institute, Fuji Chemical Industries, Ltd., Toyama, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Apr;38(4):1007-11. doi: 10.1248/cpb.38.1007.

DOI:10.1248/cpb.38.1007

PMID:2165873

Abstract

A series of tripeptidyl analogues carrying hydroxamic acid residue at the C-terminus of the molecule were synthesized, and their inhibitory activities against vertebrate collagenase and other metalloenzymes including bacterial collagenase were examined. Both Z-Pro-Leu-Ala-NHOH and Z-Pro-D-Leu-D-Ala-NHOH showed highly specific and potent inhibitory activity against tadpole and human skin collagenases with an IC50 of 10(-6) M order.

摘要

合成了一系列在分子C末端带有异羟肟酸残基的三肽基类似物，并检测了它们对脊椎动物胶原酶和包括细菌胶原酶在内的其他金属酶的抑制活性。Z-Pro-Leu-Ala-NHOH和Z-Pro-D-Leu-D-Ala-NHOH对蝌蚪和人皮肤胶原酶均表现出高度特异性和强效的抑制活性，IC50为10^(-6)M数量级。