The human protein
methyltransferases (PMTs) constitute a large enzyme class composed of two
families, the protein lysine methyltransferases (PKMTs) and the protein
arginine methyltransferases (PRMTs). Examples have been reported of both PKMTs
and PRMTs that are genetically altered in specific human cancers, and in
several cases these alterations have been demonstrated to confer a unique
dependence of the cancer cells on PMT enzymatic activity for the tumorigenic
phenotype. Examples of such driver alterations in PMTs will be presented
together with a review of current efforts towards the discovery and development
of small-molecule inhibitors of these enzymes as personalized cancer therapeutics.
Source: Targeting
genetic alterations in protein methyltransferases for personalized cancer
therapeutics. Copeland RA (RCopeland@Epizyme.com),
Moyer MP, Richon VM. Oncogene. 2012 Nov 19.
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