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Identification of Covalent Bromodomain Binders through DNA Display of Small Molecules

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Tallant, Cynthia
Published in Angewandte Chemie: International Edition. 2015, vol. 54, no. 20, p. 6057-6061
Abstract The regulation of transcriptional programs by epigenetic readers (bromodomains) has been linked to the development of several pathologies. Notably, it has been implicated in the regulation of cellular growth and evasion of apoptosis, in cancer as well as in inflammation. The discovery of small-molecule probes to dissect the role of bromodomains is thus important. We demonstrate that specific cysteine residues conserved across the bromodomains can be harnessed for covalent trapping. We report the discovery of two small molecules that form a covalent bond with cysteine residues conserved across the bromodomain family, analyze the subset of bromodomains that can be addressed through covalent binding, and show proteomic analyses enabled by the enrichment of bromodomains from native lysates.
Keywords Activity-based proteomic profilingBromodomainsCovalent inhibitorsMicroarrays
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Other version: http://doi.wiley.com/10.1002/anie.201412276
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DAGUER, Jean Pierre et al. Identification of Covalent Bromodomain Binders through DNA Display of Small Molecules. In: Angewandte Chemie: International Edition, 2015, vol. 54, n° 20, p. 6057-6061. https://archive-ouverte.unige.ch/unige:56105

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Deposited on : 2015-05-11

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