title: Targets in epigenetics: inhibiting the methyl writers of the histone code.
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.
authors.affiliation: 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.
authors.forename: Julianne M
authors.initials: JM
authors.lastname: Yost
authors.forename: Ilia
authors.initials: I
authors.lastname: Korboukh
authors.forename: Feng
authors.initials: F
authors.lastname: Liu
authors.forename: Cen
authors.initials: C
authors.lastname: Gao
authors.forename: Jian
authors.initials: J
authors.lastname: Jin