Epigenetic drug discovery has now witnessed the emergence of a new target c
lass of proteins, the bromodomains. In their Communication on
l="references:https://doi.org/10.1002/anie.201610816">page 827 ff., D.
J.
Dixon, P. E. Brennan et a
l. report the first potent, se
lective, ce
ll-permeab
le, and ce
ll-active chemica
l probe for the p300/CBP associated factor (PCAF) bromodomain. A combination of computationa
l docking studies, inhibitor design, and asymmetric synthesis furnished their probe,
L-Moses, for use as a chemica
l too
l for this epigenetic target to interrogate its ro
le in associated diseases.