Lysine methyltransferase inhibitors: where we are now.

Protein lysine methyltransferases constitute a large family of epigenetic writers which catalyse the transfer of a methyl group from the cofactor S-adenosyl-L-methionine to histone and non-histone specific substrates. Alterations in the expression and activity of these proteins have been linked to the insurgence and progress of several diseases, including cancer, neurological disorders, and growing defects, hence they represent interesting targets for new therapeutical approaches. Over the past two decades, the identification of modulators of lysine methyltransferases has increased tremendously, clarifying the role of these proteins in different physio-pathological states. The aim of this review is to furnish an updated outlook about the protein lysine methyltransferases disclosed modulators, reporting their potency, the mechanism of action and their eventual use in clinical and preclinical studies.