Modulating the Masters: Chemical Tools to Dissect CBP and p300 Function
ACS Citation
Breen, M.E.; Mapp, A.K. "Modulating the masters: chemical tools to dissect CBP and p300 function", Current Opinion in Chemical Biology, 2018, 45, 195-203.
Version of Record
Abstract
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.
Source Name
Current Opinion in Chemical Biology
Publication Date
2018
Volume
45
Page(s)
195-203
Document Type
Article
Citation Type
Article