title: Structural features and inhibitors of bromodomains.
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.
authors: 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.
authors: Jamel
authors: J
authors: Meslamani
authors: Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States.
authors: Steven G
authors: SG
authors: Smith
authors: Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States.
authors: Roberto
authors: R
authors: Sanchez
authors: Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, 1425 Madison Avenue, New York, NY 10029, United States.
authors: Ming-Ming
authors: MM
authors: Zhou
mesh_terms: D000818:Animals; D006801:Humans; D009687:Nuclear Proteins / Q000737:chemistry*; D000072417:Protein Domains; D014157:Transcription Factors / Q000737:chemistry*
chemical_list: D009687:Nuclear Proteins; D014157:Transcription Factors