Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5

被引：130

作者：

Biel, M

Kretsovali, A

Karatzali, E

Papamatheakis, J

Giannis, A

机构：

[1] FORTH, Vassilika Vouton, Inst Mol Biol & Biotechnol, Iraklion, Greece

[2] Univ Leipzig, Inst Organ Chem, D-04103 Leipzig, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 30期

关键词：

biological activity; epigenetics; histone acetyltransferase; histone code; inhibitors;

D O I：

10.1002/anie.200453879

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

HATs off! The development of the first cell-permeable small-molecule inhibitor of the human histone acetyltransferase (HAT) Gcn5 opens up new possibilities for understanding the histone code. Based on kinetic data and the proposed mechanism of the acetylation by Gcn5, the relatively simple butyrolactone structure of the inhibitor was identified.

引用

页码：3974 / 3976

页数：3

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[21] Signaling network model of chromatin [J].