title: Protein arginine methyltransferases (PRMTs) as therapeutic targets.
abstract: BACKGROUND
  Protein arginine methyltransferases (PRMTs) add one or two monomethyl groups to the guanidino nitrogen atoms of arginine residues, resulting in epigenetic modification of histones or changes of protein-protein interactions, which in turn leads to the regulation of a variety of biological functions, including transcriptional activation/repression, signal transduction, cell differentiation, and embryonic development. As dysregulation of PRMTs has been observed in diverse types of cancers and modulation of their levels affects cancer cell growth, these enzymes are considered to be potential therapeutic targets.
  
  
  METHODS
  In this review, we examined recent advances in our understanding of the regulatory mechanisms of PRMT activity and the biological roles of PRMTs in embryonic stem cell, Wnt/β-catenin signaling, and cancer development.
  
  
  CONCLUSIONS
  The roles of PRMTs have been fairly well established, but further studies are required to determine how PRMTs are regulated by cellular signaling pathways in vivo. Since the usage of adult stem cells is under intense scrutiny by society, identification of the roles of PRMTs in adult stem cells is expected in the near future. Although small molecules specific to PRMTs with high potency in vitro have been identified, development of small molecules that can regulate the activity of PRMTs in vivo is urgently required for therapeutic purposes.
authors.affiliation: The University of Seoul, Department of Life Science, 90 Jeonnong-dong, Dongdaemun-gu, Seoul, 130-743, Republic of Korea.
authors.forename: Boksik
authors.initials: B
authors.lastname: Cha
authors.forename: Eek-Hoon
authors.initials: EH
authors.lastname: Jho
mesh_terms: D000818:Animals; D053595:Embryonic Stem Cells / Q000201:enzymology; D006801:Humans; D009369:Neoplasms / Q000201:enzymology*; D011484:Protein-Arginine N-Methyltransferases / Q000378:metabolism*; D051153:Wnt Proteins / Q000378:metabolism; D051176:beta Catenin / Q000378:metabolism
chemical_list: D051153:Wnt Proteins; D051176:beta Catenin; D011484:Protein-Arginine N-Methyltransferases