title: Histone lysine methyltransferases as anti-cancer targets for drug discovery.
abstract: Post-translational epigenetic modification of histones is controlled by a number of histone-modifying enzymes. Such modification regulates the accessibility of DNA and the subsequent expression or silencing of a gene. Human histone methyltransferases (HMTs)constitute a large family that includes histone lysine methyltransferases (HKMTs) and histone/protein arginine methyltransferases (PRMTs). There is increasing evidence showing a correlation between HKMTs and cancer pathogenesis. Here, we present an overview of representative HKMTs, including their biological and biochemical properties as well as the profiles of small molecule inhibitors for a comprehensive understanding of HKMTs in drug discovery.
authors.affiliation: The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.|The National Center for Drug Screening, Shanghai 201203, China.|School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Liu
authors.affiliation: The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.|The National Center for Drug Screening, Shanghai 201203, China.|School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Ming-Wei
authors.initials: MW
authors.lastname: Wang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D055808:Drug Discovery; D011495:Histone-Lysine N-Methyltransferase / Q000037:antagonists & inhibitors*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D011495:Histone-Lysine N-Methyltransferase