Title |
Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching
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Published in |
Epigenetics & Chromatin, July 2014
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DOI | 10.1186/1756-8935-7-14 |
Pubmed ID | |
Authors |
Martin Philpott, Catherine M Rogers, Clarence Yapp, Chris Wells, Jean-Philippe Lambert, Claire Strain-Damerell, Nicola A Burgess-Brown, Anne-Claude Gingras, Stefan Knapp, Susanne Müller |
Abstract |
Acetylation of lysine residues in histone tails plays an important role in the regulation of gene transcription. Bromdomains are the readers of acetylated histone marks, and, consequently, bromodomain-containing proteins have a variety of chromatin-related functions. Moreover, they are increasingly being recognised as important mediators of a wide range of diseases. The first potent and selective bromodomain inhibitors are beginning to be described, but the diverse or unknown functions of bromodomain-containing proteins present challenges to systematically demonstrating cellular efficacy and selectivity for these inhibitors. Here we assess the viability of fluorescence recovery after photobleaching (FRAP) assays as a target agnostic method for the direct visualisation of an on-target effect of bromodomain inhibitors in living cells. |
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