title: Bromodomains: pockets with therapeutic potential.
abstract: Intense interest in the complex biology of the bromodomain (BRD) protein modules has fueled the development of novel small molecule inhibitors that target the acetyl-lysine (KAc) binding pocket of the BRD. BRD inhibition has revealed exciting opportunities for treating a variety of maladies such as cancer, inflammation, obesity, cardiovascular disease, and neurological disorders. With five BRD inhibitors already in clinical trials, the BRD field seems to be rising to success.
authors.affiliation: Department of Biological Chemistry, University of Athens Medical School, 11527 Athens, Greece.
authors.forename: Kostas A
authors.initials: KA
authors.lastname: Papavassiliou
authors.affiliation: Department of Biological Chemistry, University of Athens Medical School, 11527 Athens, Greece. Electronic address: papavas@med.uoa.gr.
authors.forename: Athanasios G
authors.initials: AG
authors.lastname: Papavassiliou
mesh_terms: D001569:Benzodiazepines / Q000494:pharmacology / Q000627:therapeutic use; D001665:Binding Sites; D002986:Clinical Trials as Topic; D006801:Humans; D058990:Molecular Targeted Therapy; D011485:Protein Binding / Q000187:drug effects; D054730:Protein Interaction Domains and Motifs / Q000187:drug effects; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use; D052999:Quinazolinones; D054852:Small Molecule Libraries / Q000494:pharmacology*
chemical_list: D011799:Quinazolines; D052999:Quinazolinones; D054852:Small Molecule Libraries; D001569:Benzodiazepines; C554645:molibresib; C000628794:apabetalone
keywords: bromodomain inhibitor; bromodomain pocket; therapeutic target; transcriptional regulation