文摘
Epigenetic drug discovery has now witnessed the emergence of a new target class of proteins, the bromodomains. In their Communication on <a href="https://doi.org/10.1002/anie.201610816" rel="references:https://doi.org/10.1002/anie.201610816">page 827 ff.,a> 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, <em>Lem>-Moses, for use as a chemical tool for this epigenetic target to interrogate its role in associated diseases.