TY  - JOUR
A1  - Chaikuad, Apirat
A1  - Lang, Steffen
A1  - Brennan, Paul E.
A1  - Temperini, Claudia
A1  - Fedorov, Oleg
A1  - Hollander, Johan
A1  - Nachane, Ruta
A1  - Abell, Chris
A1  - Müller, Susanne
A1  - Siegal, Gregg
A1  - Knapp, Stefan
T1  - Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain
T2  - Journal of medicinal chemistry
N2  - The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.
Y1  - 2016
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/41894
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-418944
SN  - 1520-4804
N1  - This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
VL  - 59
IS  - 4
SP  - 1648
EP  - 1653
PB  - American Chemical Society
CY  - Washington, DC
ER  -