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Drug Discov Today Technol. 2016 Mar;19:3-15. doi: 10.1016/j.ddtec.2016.09.001. Epub 2016 Sep 22.

Structural features and inhibitors of bromodomains.

Author information

1
Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States. Electronic address: jamel.meslamani@mssm.edu.
2
Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States.

Abstract

Bromodomains are conserved structural modules responsible for recognizing acetylated-lysine residues on histone tails and other transcription-associated proteins, such as transcription factors and co-factors. Owing to their important functions in the regulation of ordered gene transcription in chromatin, bromodomains of the BET family proteins have recently been shown as druggable targets for a wide array of human diseases, including cancer and inflammation. Here we review the structural and functional features of the bromodomains and their small-molecule inhibitors. Additional new insights provided herein highlight the landscape of the ligand binding sites in the bromodomains that will hopefully facilitate further development of new inhibitors with optimal affinity and selectivity.

PMID:
27769355
PMCID:
PMC5325140
DOI:
10.1016/j.ddtec.2016.09.001
[Indexed for MEDLINE]
Free PMC Article

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