title: Functional Crosstalk Between Lysine Methyltransferases on Histone Substrates: The Case of G9A/GLP and Polycomb Repressive Complex 2.
abstract: CONCLUSIONS
  Methylation of histone H3 on lysine 9 and 27 (H3K9 and H3K27) are two epigenetic modifications that have been linked to several crucial biological processes, among which are transcriptional silencing and cell differentiation.
  
  
  BACKGROUND
  Deposition of these marks is catalyzed by H3K9 lysine methyltransferases (KMTs) and polycomb repressive complex 2, respectively. Increasing evidence is emerging in favor of a functional crosstalk between these two major KMT families.
  
  
  RESULTS
  Here, we review the current knowledge on the mechanisms of action and function of these enzymes, with particular emphasis on their interplay in the regulation of chromatin states and biological processes. We outline their crucial roles played in tissue homeostasis, by controlling the fate of embryonic and tissue-specific stem cells, highlighting how their deregulation is often linked to the emergence of a number of malignancies and neurological disorders.
  
  
  CONCLUSIONS
  Histone methyltransferases are starting to be tested as drug targets. A new generation of highly selective chemical inhibitors is starting to emerge. These hold great promise for a rapid translation of targeting epigenetic drugs into clinical practice for a number of aggressive cancers and neurological disorders.
authors.affiliation: Laboratoire Epigénétique et Destin Cellulaire, UMR7216, Centre National de la Recherche Scientifique CNRS, Université Paris Diderot , Sorbonne Paris Cité, Paris, France .
authors.forename: Chiara
authors.initials: C
authors.lastname: Mozzetta
authors.forename: Julien
authors.initials: J
authors.lastname: Pontis
authors.forename: Slimane
authors.initials: S
authors.lastname: Ait-Si-Ali
mesh_terms: D011495:Histone-Lysine N-Methyltransferase / Q000378:metabolism*; D006657:Histones / Q000378:metabolism*; D006801:Humans; D063151:Polycomb Repressive Complex 2 / Q000378:metabolism*; D013379:Substrate Specificity
chemical_list: D006657:Histones; C455847:EHMT1 protein, human; D011495:Histone-Lysine N-Methyltransferase; D063151:Polycomb Repressive Complex 2