Ontology highlight
ABSTRACT:
SUBMITTER: Vedadi M
PROVIDER: S-EPMC3184254 | biostudies-literature | 2011 Jul
REPOSITORIES: biostudies-literature
Vedadi Masoud M Barsyte-Lovejoy Dalia D Liu Feng F Rival-Gervier Sylvie S Allali-Hassani Abdellah A Labrie Viviane V Labrie Viviane V Wigle Tim J TJ Dimaggio Peter A PA Wasney Gregory A GA Siarheyeva Alena A Dong Aiping A Tempel Wolfram W Wang Sun-Chong SC Chen Xin X Chau Irene I Mangano Thomas J TJ Huang Xi-Ping XP Simpson Catherine D CD Pattenden Samantha G SG Norris Jacqueline L JL Kireev Dmitri B DB Tripathy Ashutosh A Edwards Aled A Roth Bryan L BL Janzen William P WP Garcia Benjamin A BA Petronis Arturas A Ellis James J Brown Peter J PJ Frye Stephen V SV Arrowsmith Cheryl H CH Jin Jian J
Nature chemical biology 20110710 8
Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as dimethylation of non-histone targets. Here we report the discovery of UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small ...[more]