title: Design of small molecule epigenetic modulators.
abstract: The field of epigenetics has expanded rapidly to reveal multiple new targets for drug discovery. The functional elements of the epigenomic machinery can be categorized as writers, erasers and readers, and together these elements control cellular gene expression and homeostasis. It is increasingly clear that aberrations in the epigenome can underly a variety of diseases, and thus discovery of small molecules that modulate the epigenome in a specific manner is a viable approach to the discovery of new therapeutic agents. In this Digest, the components of epigenetic control of gene expression will be briefly summarized, and efforts to identify small molecules that modulate epigenetic processes will be described.
authors.affiliation: Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, 70 President St., Charleston, SC 29425, United States.
authors.forename: Boobalan
authors.initials: B
authors.lastname: Pachaiyappan
authors.affiliation: Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina, 70 President St., Charleston, SC 29425, United States. Electronic address: woster@musc.edu.
authors.forename: Patrick M
authors.initials: PM
authors.lastname: Woster
mesh_terms: D000818:Animals; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D044127:Epigenesis, Genetic / Q000187:drug effects*; D057890:Epigenomics; D056466:Histone Demethylases / Q000037:antagonists & inhibitors / Q000235:genetics* / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014166:Transferases / Q000037:antagonists & inhibitors / Q000235:genetics* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D056466:Histone Demethylases; D014166:Transferases
keywords: Acetyllysine; Epigenetic; Histone; Methylarginine; Methyllysine