Novel approaches to targeting BRD4

Publication date: Available online 28 October 2017 Source:Drug Discovery Today: Technologies Author(s): Olesya A. Kharenko, Henrik C. Hansen Inhibition of bromo and extra-terminal (BET) bromodomains, including BRD4, has emerged as a new exciting epigenetic target for oncology, in particular. Recently, novel alternatives to the traditional use of reversible small molecules have emerged, including proteolytic targeting BET agents and irreversible binding inhibitors. These alternatives to reversible inhibitors may offer some advantage and can be used as tools to further decipher the underlying biology. Supportive pre-clinical data have these novel approaches bound for clinical development in the near future.
Source: Drug Discovery Today: Technologies - Category: Drugs & Pharmacology Source Type: research