Current Chemical Genomics and Translational Medicine

2011, 5 : 72-84
Published online 2011 August 22. DOI: 10.2174/1875397301005010072
Publisher ID: CCGTM-5-72

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

Julianne M Yost , Ilia Korboukh , Feng Liu , Cen Gao and 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

* 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

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.