Drug discovery: Doubling down on BET inhibition

November 15th, 2016 by Dafydd Owen

Nature Chemical Biology 12, 991 (2016). doi:10.1038/nchembio.2242

Author: Dafydd Owen

Through simultaneous binding to more than one site in a single protein, multivalent small molecules can achieve huge increases in potency. This 'avidity effect' has been demonstrated in BET bromodomain-containing proteins with bivalent probes that represent some of the most potent BET inhibitors to date.