Fragment-Based Screening of the Bromodomain of ATAD2

被引：64

作者：

Harner, Mary J. ^{[1
]}

Chauder, Brian A. ^{[1
]}

Phan, Jason ^{[1
]}

Fesik, Stephen W. ^{[1
]}

机构：

[1] Vanderbilt Univ, Dept Biochem, Sch Med, Nashville, TN 37232 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 22期

基金：

美国国家卫生研究院;

关键词：

HIGH-AFFINITY LIGANDS; COREGULATOR ANCCA; PROTEIN; CANCER; NMR; COACTIVATOR; DESIGN; BREAST;

D O I：

10.1021/jm501035j

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.

引用

页码：9687 / 9692

页数：6

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