title: Cancer drug discovery targeting histone methyltransferases: an update.
abstract: Epigenetic dysregulation has been recognized as an important contributor to cancer initiation and progression as most tumors harbor both genetic and epigenetic abnormalities. Inhibiting epigenetic proteins represents a novel approach in cancer drug discovery and more profound efficacy and less resistance are expected since multiple signaling pathways can be modulated as a result of inhibiting a single epigenetic target. Histone methyl transferases (HMTs) are an important component in epigenome and HMT inhibitors are being pursued intensely by both pharmaceutical industry and academic institutions. In this article we will provide an update on the drug discovery effort on several key HMTs.
authors: Research and Development, AbbVie Inc. 1 North Waukegan Road, North Chicago, IL60064, USA. hongyu.zhao@abbvie.com.
authors: Hongyu
authors: H
authors: Zhao
authors: Ying
authors: Y
authors: Wang
authors: Huanqiu
authors: H
authors: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D055808:Drug Discovery; D000076983:Histone Methyltransferases; D011495:Histone-Lysine N-Methyltransferase / Q000037:antagonists & inhibitors*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology
chemical_list: D000970:Antineoplastic Agents; D000076983:Histone Methyltransferases; D011495:Histone-Lysine N-Methyltransferase