title: Chromatin proteins and modifications as drug targets.
abstract: A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.
authors.affiliation: 1] Biotech Research and Innovation Centre, University of Copenhagen, Ole Maaløes Vej 5, 2200 Copenhagen, Denmark. [2] Centre for Epigenetics, University of Copenhagen, Ole Maaløes Vej 5, 2200 Copenhagen, Denmark. [3] The Danish Stem Cell Center, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark.
authors.forename: Kristian
authors.initials: K
authors.lastname: Helin
authors.forename: Dashyant
authors.initials: D
authors.lastname: Dhanak
mesh_terms: D000818:Animals; D002843:Chromatin / Q000737:chemistry / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000076983:Histone Methyltransferases; D011495:Histone-Lysine N-Methyltransferase / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000235:genetics / Q000378:metabolism; D017434:Protein Structure, Tertiary / Q000187:drug effects
chemical_list: D002843:Chromatin; D056466:Histone Demethylases; C495195:KDM1A protein, human; D000076983:Histone Methyltransferases; D011495:Histone-Lysine N-Methyltransferase