Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomainsElectronic supplementary information (ESI) available. See DOI: 10.1039/c5md00152h

Emerging evidence suggests bromodomain-containing proteins 7 and 9 (BRD7 and BRD9) have roles in the regulation of human transcription and disease including cancer. We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as tools to elucidate the biological rol...

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Main Authors: Hay, Duncan A, Rogers, Catherine M, Fedorov, Oleg, Tallant, Cynthia, Martin, Sarah, Monteiro, Octovia P, Müller, Susanne, Knapp, Stefan, Schofield, Christopher J, Brennan, Paul E
Format: Article
Language:English
Online Access:Get full text
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Summary:Emerging evidence suggests bromodomain-containing proteins 7 and 9 (BRD7 and BRD9) have roles in the regulation of human transcription and disease including cancer. We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as tools to elucidate the biological roles of BRD7 and BRD9 in healthy and diseased cells. We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as chemical probes to elucidate the biological roles of BRD7 and BRD9 in cells.
ISSN:2040-2503
2040-2511
DOI:10.1039/c5md00152h