RESEARCH ARTICLE


Targets in Epigenetics: Inhibiting the Methyl Writers of the Histone Code



Julianne M Yost#, Ilia Korboukh#, Feng Liu#, Cen Gao#, Jian Jin*
Center for Integrative Chemical Biology and Drug Discovery, Division of Medicinal Chemistry and Natural Products, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA


Article Metrics

CrossRef Citations:
0
Total Statistics:

Full-Text HTML Views: 893
Abstract HTML Views: 629
PDF Downloads: 255
Total Views/Downloads: 1777
Unique Statistics:

Full-Text HTML Views: 418
Abstract HTML Views: 330
PDF Downloads: 140
Total Views/Downloads: 888



© Yost et al.; Licensee Bentham Open.

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.

* Address correspondence to this author at the Center for Integrative Chemical Biology and Drug Discovery, Division of Medicinal Chemistry and Natural Products, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA; Tel: 919-843-8459; Fax: 919-843-8465; E-mail: jianjin@unc.edu
# These authors contributed equally to this review.


Abstract

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.

Keywords: PRMT inhibitors, PKMT inhibitors, HMT inhibitors, methyltransferase inhibitors, small molecule inhibitors, drug discovery, Epigenetics.