Histone methyltransferases (HMTs, also known as protein methyltransferases) have been increasingly pursued as potential therapeutic targets. High quality selective inhibitors of HMTs will permit biological and disease hypotheses concerning these enzymes to be tested in cell-based and/or animal models with high confidence. Our laboratory has made significant progress on discovering selective inhibitors of HMTs by pursuing multiple complementary structure-based inhibitor discovery approaches. Our progress on discovering selective inhibitors of GLP, SETD8 and type I PRMTs along with new utilities of our EZH2 inhibitors will be presented.

Discovery of selective inhibitors for histone methyltransferases

256th National Meeting (2018)

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