A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

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Science  31 Oct 2014:
Vol. 346, Issue 6209, pp. 638-641
DOI: 10.1126/science.1249830

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Epigenetics: It's all about the individual

The bromodomain and extraterminal domain (BET) proteins are a family of epigenetic regulators that affect transcription through interactions with acetylated chromatin. These proteins have attracted interest as drug targets because of their roles in human diseases, including cancer. Parsing out the biological functions of individual family members is important for drug development but has been challenging because of the proteins' shared structural domains. In a proof-of-concept study, Baud et al. used a chemical genetics strategy to design a highly selective small-molecule probe that inhibits the chromatin binding activity of one family member. Extension of this approach may help elucidate the function of individual BET proteins and prioritize them as drug targets.

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