Bromodomains: pockets with therapeutic potential

Kostas A Papavassiliou; Athanasios G Papavassiliou

doi:10.1016/j.molmed.2014.06.004

Bromodomains: pockets with therapeutic potential

Trends Mol Med. 2014 Sep;20(9):477-8. doi: 10.1016/j.molmed.2014.06.004. Epub 2014 Jun 28.

Authors

Kostas A Papavassiliou¹, Athanasios G Papavassiliou²

Affiliations

¹ Department of Biological Chemistry, University of Athens Medical School, 11527 Athens, Greece.
² Department of Biological Chemistry, University of Athens Medical School, 11527 Athens, Greece. Electronic address: papavas@med.uoa.gr.

PMID: 24986769
DOI: 10.1016/j.molmed.2014.06.004

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.

Keywords: bromodomain inhibitor; bromodomain pocket; therapeutic target; transcriptional regulation.

MeSH terms

Benzodiazepines / pharmacology
Benzodiazepines / therapeutic use
Binding Sites
Clinical Trials as Topic
Humans
Molecular Targeted Therapy
Protein Binding / drug effects
Protein Interaction Domains and Motifs* / drug effects
Quinazolines / pharmacology
Quinazolines / therapeutic use
Quinazolinones
Small Molecule Libraries / pharmacology*

Substances

Quinazolines
Quinazolinones
Small Molecule Libraries
Benzodiazepines
molibresib
apabetalone