BET BROMODOMAIN INHIBITORS

The BET sub-family of bromodomains recognises acetyl-lysine histone marks in the chromatin, and thereby facilitates regulation of gene expression and thus ultimately synthesis of specific proteins. The BET family is considered an exciting new biological disease target class offering new mode of action for treatment of cancer and inflammatory diseases.

Common to all BET bromodomain proteins is the presence of tandem acetyl binding domains. Emerging data point to differentiated biological functions of the individual domains and it may be of therapeutic importance selectively inhibit only individual domains of the BET family thereby reducing toxicity associated with non-selective BET inhibition.

Nuevolution is developing compound classes exhibiting BET subdomain selectivity, and we are currently exploring the use of such compounds in various disease settings, including inflammation.