Novel pharmacological maps of protein lysine methyltransferases: key for target deorphanization.

ABSTRACT: Epigenetic therapies are being investigated for the treatment of cancer, cognitive disorders, metabolic alterations and autoinmune diseases. Among the different epigenetic target families, protein lysine methyltransferases (PKMTs), are especially interesting because it is believed that their inhibition may be highly specific at the functional level. Despite its relevance, there are currently known inhibitors against only 10 out of the 50 SET-domain containing members of the PKMT family. Accordingly, the identification of chemical probes for the validation of the therapeutic impact of epigenetic modulation is key. Moreover, little is known about the mechanisms that dictate their substrate specificity and ligand selectivity. Consequently, it is desirable to explore novel methods to character

SUBMITTER: Rabal O 

PROVIDER: S-EPMC6054832 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature