Development of a Potent and Selective HDAC8 Inhibitor

被引：62

作者：

Ingham, Oscar J. ^{[1
,2
]}

Paranal, Ronald M. ^{[3
]}

Smith, William B. ^{[3
]}

Escobar, Randolph A. ^{[1
,2
]}

Yueh, Han ^{[1
,2
]}

Snyder, Tracy ^{[1
,2
]}

Porco, John A., Jr. ^{[1
,2
]}

Bradner, James E. ^{[3
,4
]}

Beeler, Aaron B. ^{[1
,2
]}

机构：

[1] Boston Univ, Dept Chem, 590 Commonwealth Ave, Boston, MA 02215 USA

[2] Boston Univ, Ctr Mol Discovery BU CMD, 590 Commonwealth Ave, Boston, MA 02215 USA

[3] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA 02215 USA

[4] Harvard Med Sch, Dept Med, Boston, MA 02115 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2016年 / 7卷 / 10期

关键词：

Histone deacetylase; HDAC; histone deacetylase 8; HDAC8; triazole; epigenetic; DEACETYLASE INHIBITORS; HISTONE; CORNELIA; CYCLOADDITION; MUTATIONS; DISCOVERY; SPECTRUM; BINDING; DESIGN; CANCER;

D O I：

10.1021/acsmedchemlett.6b00239

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel, isoform-selective inhibitor of histone deacetylase 8 (HDAC8) has been discovered by the repurposing of a diverse compound collection. Medicinal chemistry optimization led to the identification of a highly potent (0.8 nM) and selective inhibitor of HDAC8.

引用

页码：929 / 932

页数：4

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