Chemistry in living cells: Detection of active proteasomes by a two-step labeling strategy

被引：131

作者：

Ovaa, H

van Swieten, PF

Kessler, BM

Leeuwenburgh, MA

Fiebiger, E

van den Nieuwendijk, AMCH

Galardy, PJ

van der Marel, GA

Ploegh, HL

Overkleeft, HS

机构：

[1] Leiden State Univ, Gorlaeus Labs, NL-2300 RA Leiden, Netherlands

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

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 31期

关键词：

bioorganic chemistry; inhibitors; peptides; proteomics; solid-phase synthesis;

D O I：

10.1002/anie.200351314

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In vivo targeting of the proteasome: Probe 1 is a cell-permeable irreversible inhibitor that alkylates the active-site residues of the proteasome in a Michael fashion. After cell lysis, a biotin moiety is introduced by Staudinger ligation to yield construct 2. This strategy allows activity profiling of the catalytic activities of the proteasome in vivo.

引用

收藏

页码：3626 / 3629

页数：4

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