Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains

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Abstract

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.

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Hay, D. A., Rogers, C. M., Fedorov, O., Tallant, C., Martin, S., Monteiro, O. P., … Brennan, P. E. (2015). Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains. MedChemComm, 6(7), 1381–1386. https://doi.org/10.1039/c5md00152h

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