Journal of Medicinal Chemistry p. 3087 - 3097 (2016)
Update date:2022-08-02
Topics:
Unzue, Andrea
Zhao, Hongtao
Lolli, Graziano
Dong, Jing
Zhu, Jian
Zechner, Melanie
Dolbois, Aymeric
Caflisch, Amedeo
Nevado, Cristina
Small-molecule hits for the bromodomains of CREBBP and BAZ2B have been identified by scaffold hopping followed by docking of a set of ~200 compounds containing the acetyl indole scaffold. Chemical synthesis of nearly 30 derivatives has resulted in ligands of representatives of three subfamilies of human bromodomains with favorable ligand efficiency. The X-ray crystal structures of three different bromodomains (CREBBP, BAZ2B, and BRPF1b) in complex with acetyl indole derivatives reveal the influence of the gatekeeper residue on the orientation of small-molecule ligands in the acetyl lysine binding site.
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