Back Cover: Discovery of a PCAF Bromodomain Chemical Probe (Angew. Chem. Int. Ed. 3/2017)

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Abstract

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Epigenetic drug discovery has now witnessed the emergence of a new target class of proteins, the bromodomains. In their Communication on page 827 ff., D. J. Dixon, P. E. Brennan et al. report the first potent, selective, cell-permeable, and cell-active chemical probe for the p300/CBP associated factor (PCAF) bromodomain. A combination of computational docking studies, inhibitor design, and asymmetric synthesis furnished their probe, L-Moses, for use as a chemical tool for this epigenetic target to interrogate its role in associated diseases.

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