Document Report Card

ID: ALA1152272

Journal: J Med Chem

Title: Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Authors: Rose NR, Ng SS, Mecinović J, Liénard BM, Bello SH, Sun Z, McDonough MA, Oppermann U, Schofield CJ.

Abstract: The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.

CiteXplore: 18942826

DOI: 10.1021/jm800936s