Identification of a peptoid inhibitor of the proteasome 19S regulatory particle

被引：90

作者：

Lim, Hyun-Suk

Archer, Chase T.

Kodadek, Thomas

机构：

[1] Univ Texas, SW Med Ctr, Div Translat Res, Dept Internal Med, Dallas, TX 75390 USA

[2] Univ Texas, SW Med Ctr, Div Translat Res, Dept Mol Biol, Dallas, TX 75390 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2007年 / 129卷 / 25期

关键词：

D O I：

10.1021/ja072027p

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The first chemical inhibitor of the 19S regulatory particle (RP) of the proteasome is described. The molecule was identified by screening a library of nucleoside-capped peptoids for binding to the yeast 26S proteasome in a crude extract. The hit was resynthesized and shown to block 19S RP-mediated protein unfolding in vitro and proteasome-mediated turnover of p27 in HeLa cells.

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页码：7750 / +

页数：3

相关论文

共 15 条

[1] The development of proteasome inhibitors as anticancer drugs [J].

Adams, J .

CANCER CELL, 2004, 5 (05) :417-421

[2] Isolation of protein ligands from large peptoid libraries [J].

Alluri, PG ;

Reddy, MM ;

Bachhawat-Sikder, K ;

Olivos, HJ ;

Kodadek, T .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2003, 125 (46) :13995-14004

[3] The proteasome:: Paradigm of a self-compartmentalizing protease [J].

Baumeister, W ;

Walz, J ;

Zühl, F ;

Seemuller, E .

CELL, 1998, 92 (03) :367-380

[4] A robust small-molecule microarray platform for screening cell lysates [J].

Bradner, James E. ;

McPherson, Olivia M. ;

Mazitschek, Ralph ;

Barnes-Seeman, David ;

Shen, John P. ;

Dhaliwal, Jasmeet ;

Stevenson, Kristen E. ;

Duffner, Jay L. ;

Park, Seung Bum ;

Neuberg, Donna S. ;

Nghiem, Paul ;

Schreiber, Stuart L. ;

Koehler, Angela N. .

CHEMISTRY & BIOLOGY, 2006, 13 (05) :493-504

[5] The proteasome: a utility tool for transcription? [J].

Collins, GA ;

Tansey, WP .

CURRENT OPINION IN GENETICS & DEVELOPMENT, 2006, 16 (02) :197-202

[6] The proteasome, a novel protease regulated by multiple mechanisms [J].

DeMartino, GN ;

Slaughter, CA .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (32) :22123-22126

[7] The Role of p27Kip1 in Proteasome Inhibitor Induced Apoptosis [J].

Drexler, Hannes C. A. .

CELL CYCLE, 2003, 2 (05) :438-441

[8] Proteasomal ATPases link ubiquitylation of histone H2B to methylation of histone H3 [J].

Ezhkova, E ;

Tansey, WP .

MOLECULAR CELL, 2004, 13 (03) :435-442

[9] The 19S regulatory particle of the proteasome is required for efficient transcription elongation by RNA polymerase II [J].

Ferdous, A ;

Gonzalez, F ;

Sun, LP ;

Kodadek, T ;

Johnston, SA .

MOLECULAR CELL, 2001, 7 (05) :981-991

[10] The role of the proteasomal ATPases and activator monoubiquitylation in regulating Gal4 binding to promoters [J].

Ferdous, Anwarul ;

Sikder, Devanjan ;

Gillette, Thomas ;

Nalley, Kip ;

Kodadek, Thomas ;

Johnston, Stephen Albert .

GENES & DEVELOPMENT, 2007, 21 (01) :112-123