Small-molecule inhibitors and probes for ubiquitin- and ubiquitin-like-specific proteases

被引：65

作者：

Borodovsky, A ^{[1
]}

Ovaa, H ^{[1
]}

Meester, WJN ^{[1
]}

Venanzi, ES ^{[1
]}

Bogyo, MS ^{[1
]}

Hekking, BG ^{[1
]}

Ploegh, HL ^{[1
]}

Kessler, BM ^{[1
]}

Overkleeft, HS ^{[1
]}

机构：

[1] Harvard Univ, Sch Med, Dept Pathol, Boston, MA 02115 USA

来源：

CHEMBIOCHEM | 2005年 / 6卷 / 02期

关键词：

active-site-directed probe; enzymes; proteases; protein modifications; SUMO APG; ubiquitin; vinyl sulfones;

D O I：

10.1002/cbic.200400236

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

There's always a catch. The post-translational modification of proteins with ubiquitin (Ub) or ubiquitin-like (Ubl) modifiers is an important signal in the regulation of a variety of biological processes, such as degradation and regulation of gene expression. Here we report the synthesis of a panel of peptide vinyl sulfones (see scheme) harboring various portions of the Ub C terminus by using a safety-catch linker. Depending on their length, such compounds can efficiently target Ubl-specific proteases. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：287 / 291

页数：5

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