Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl α-keto aldehydes (glyoxals)

被引：65

作者：

Lynas, JF

Harriott, P

Healy, A

McKervey, MA

Walker, B

机构：

[1] Queens Univ Belfast, Sch Biol & Biochem, Ctr Peptide & Prot Engn, Belfast BT9 7BL, Antrim, North Ireland

[2] Queens Univ Belfast, Sch Chem, Belfast BT9 5AG, Antrim, North Ireland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(98)00030-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final K-i values of approximately 3.0 nM. These are among the lowest values so far reported for (tri)peptide-based aldehyde-releated inhibitors. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：373 / 378

页数：6

共 27 条

[1] Novel inhibitors of the proteasome and their therapeutic use in inflammation [J].