Novel Drugs Targeting the Epigenome

Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors

“…PRMT5 has been a drug target for many pharmaceutical and biotechnology companies, as well as academic research institutions, due to its critical function in cancer. − Before the disclosure of LLY-283 and JNJ64619178, − a major concern among scientists in the field was whether it was possible to obtain SAM mimetic nucleoside analogues with selectivity versus different PRMTs. Neither of the SAM analogues, SAH ( S -adenosyl- l -homocysteine) or sinefungin, is a selective methyltransferase inhibitor.…”