Ontology highlight
ABSTRACT:
SUBMITTER: Liu F
PROVIDER: S-EPMC3171737 | biostudies-literature | 2011 Sep
REPOSITORIES: biostudies-literature
Liu Feng F Barsyte-Lovejoy Dalia D Allali-Hassani Abdellah A He Yunlong Y Herold J Martin JM Chen Xin X Yates Christopher M CM Frye Stephen V SV Brown Peter J PJ Huang Jing J Vedadi Masoud M Arrowsmith Cheryl H CH Jin Jian J
Journal of medicinal chemistry 20110805 17
Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histone H3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53. We previously reported the discovery of UNC0321 (3), the most potent G9a inhibitor to date, via structure-based design and structure-activity relationship (SAR) exploration of the quinazoline scaffold represented by BIX01294 (1). Despite its ve ...[more]