Modulating the masters: chemical tools to dissect CBP and p300 function

被引:51
作者
Breen, Meghan E. [1 ]
Mapp, Anna K. [1 ]
机构
[1] Univ Michigan, Life Sci Inst, 210 Washtenaw Ave, Ann Arbor, MI 48109 USA
关键词
SMALL-MOLECULE INHIBITOR; ELEMENT-BINDING PROTEIN; ALLOSTERIC REGULATION; DIFFERENTIAL ROLES; COACTIVATORS CBP; KIX DOMAIN; DISCOVERY; CBP/P300; BROMODOMAINS; TARGETS;
D O I
10.1016/j.cbpa.2018.06.005
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Dysregulation of transcription is found in nearly every human disease, and as a result there has been intense interest in developing new therapeutics that target regulators of transcription. CREB binding protein (CBP) and its paralogue p300 are attractive targets due to their function as 'master coactivators'. Although inhibitors of several CBP/p300 domains have been identified, the selectivity of many of these compounds has remained underexplored. Here, we review recent successes in the development of chemical tools targeting several CBP/p300 domains with selectivity acceptable for use as chemical probes. Additionally, we highlight recent studies which have used these probes to expand our understanding of interdomain interactions and differential coactivator usage.
引用
收藏
页码:195 / 203
页数:9
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