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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.

Original publication

DOI

10.1021/acs.jmedchem.5b01719

Type

Journal article

Journal

J Med Chem

Publication Date

25/02/2016

Volume

59

Pages

1648 - 1653

Keywords

Drug Discovery, Humans, Ligands, Models, Molecular, Molecular Docking Simulation, Protein Binding, Protein Structure, Tertiary, Small Molecule Libraries, p300-CBP Transcription Factors