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ID: ALA1156943
Journal: Bioorg Med Chem Lett
Title: Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases.
Authors: Dowden J, Hong W, Parry RV, Pike RA, Ward SG.
Abstract: Prototype inhibitors of protein arginine methyltransferases (PRMTs) have been constructed by attaching guanidine functionality via a variable linker to non-reactive amine analogues of the cellular co-factor (S)-adenosyl methionine (AdoMet). Potent inhibition of PRMT1 (IC(50) of approximately 3-6 microM) combined with weak inhibition of the lysine methyltransferase SET7 (approximately 50% of activity at 100 microM) was observed for two such compounds.
CiteXplore: 20219369