Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation

Abstract

With each newly disclosed resistance mechanism, management of cancer with previously established targets have become a "failure" oriented approach. Molecular targets such as kinases did initially provide a ray of hope against cancer but with decades of struggle between novel therapeutic agents and more sophisticated resistance mechanisms, they seem to have saturated as anti-cancer targets. Now, with more exhaustive molecular recognition techniques and approaches, epigenetic targets have accessed the centre stage as anti-cancer targets. Accordingly, several classes of epigenetic enzymes are being studied for this role and histone methyltransferases form one such class. They include a class of epigenetic enzymes which transfer methyl group from histone proteins and maintain genetic homeostasis. In cancer, several reports have deduced upregulation of different members of this family according to the tumor environment, establishing them as one of the novel anti-cancer targets. This compilation provides an updated information on several members of histone methyltransferases family as epigenetic targets for developing novel anti-cancer agents.

Keywords: Cancer; DOT1L; EHMT2; EZH2; LSDs; SETD; SMYD.