Targets in Epigenetics: Inhibiting the Methyl Writers of the Histone Code
Julianne M Yost#, Ilia Korboukh#, Feng Liu#, Cen Gao#, Jian Jin*
Identifiers and Pagination:Year: 2011
Issue: Suppl 1
First Page: 72
Last Page: 84
Publisher Id: CCGTM-5-72
Article History:Received Date: 1/2/2011
Revision Received Date: 11/7/2011
Acceptance Date: 18/7/2011
Electronic publication date: 22/8/2011
Collection year: 2011
open-access license: This is an open access article licensed under the terms of the Creative Commons Attribution Non-Commercial License (http: //creativecommons.org/licenses/by-nc/3.0/ which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
Growing evidence suggests that protein lysine methyltransferases (PKMTs) and protein arginine methyltransferases (PRMTs) are associated with the development of various human diseases, including cancer, inflammation, and psychiatric disorders. Given the significant role of these proteins in human disease, efforts to discover selective small-molecule inhibitors of these enzymes are quickly gaining momentum. In this review, we focus on the recent progress in the discovery of selective PKMT and PRMT inhibitors. A future perspective on developing methyltransferase inhibitors is also offered.