biostudies-literatureSmith SGNIDA NIH HHSNHGRI NIH HHSNCI NIH HHSNIGMS NIH HHS573-83https://www.ebi.ac.uk/biostudies/studies/S-EPMC4035449biostudies-literatureUnknown21(5)Chemical compounds built on a diazepine scaffold have recently emerged as potent inhibitors of the acetyl-lysine binding activity of bromodomain-containing proteins, which is required for gene transcriptional activation in cancer and inflammation. Not only have these chemical compounds validated bromodomains as attractive epigenetic drug targets, but they have also brought to the forefront another application of the diazepine, which had already been regarded as a versatile chemical scaffold in rational drug design. This article reviews the success of diazepine compounds as therapeutic agents and examines the unique chemical and geometric features of this privileged scaffold that make it an excellent template for developing potent and selective molecules that control bromodomain-related genChemistry & biologyPrivileged diazepine compounds and their emergence as bromodomain inhibitors.PMC4035449P01 CA080058T32 GM062754R33 DA029963R01 CA087658R01 HG004508Sanchez RZhou MMSmith SGfalsePrivileged diazepine compounds and their emergence as bromodomain inhibitors.Chemical compounds built on a diazepine scaffold have recently emerged as potent inhibitors of the acetyl-lysine binding activity of bromodomain-containing proteins, which is required for gene transcriptional activation in cancer and inflammation. Not only have these chemical compounds validated bromodomains as attractive epigenetic drug targets, but they have also brought to the forefront another application of the diazepine, which had already been regarded as a versatile chemical scaffold in rational drug design. This article reviews the success of diazepine compounds as therapeutic agents and examines the unique chemical and geometric features of this privileged scaffold that make it an excellent template for developing potent and selective molecules that control bromodomain-related gen2014-01-01T00:00:00Z2014 May2025-04-04T14:43:00.621Z2019-06-06T12:49:19ZS-EPMC40354492474655910.1016/j.chembiol.2014.03.004