Development of a Selective and Potent PRMT4 PROTAC Degrader with Efficacy against Multiple Myeloma in Vitro and in Vivo

Protein arginine methyltransferase 4 (PRMT4) is highly expressed in relapsed or refractory multiple myeloma (MM) and is associated with poor prognosis. Conventional PRMT4 inhibitors face challenges including inadequate efficacy, acquired resistance, and inability to inhibit nonenzymatic functions. I...

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מחבר ראשי:	Yong Ju (1404961) (author)
מחברים אחרים:	Huizhu Song (18279722) (author), Yuelan He (21567958) (author), Yingtung Lo (19359617) (author), Zhipeng Fan (110971) (author), Jianzhong Lu (480003) (author)
יצא לאור:	2025
נושאים:	Biophysics Biochemistry Genetics Molecular Biology Pharmacology Biotechnology Cancer Science Policy Hematology Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified relatively long half protein arginine methyltransferases inhibit nonenzymatic functions exhibit therapeutic effects e3 ligase ligand showed high selectivity proteolysis targeting chimera vivo studies showed targeted protac degrader refractory multiple myeloma max </ sub 50 </ sub c199 </ b prmt4 inhibitor ezm2302 multiple myeloma targeting prmt4 high doses >< sub von hippel versus 49 poor prognosis highly expressed first evidence findings provide acquired resistance 89 h 106 nm 1 %)
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Development of a Selective and Potent PRMT4 PROTAC Degrader with Efficacy against Multiple Myeloma in Vitro and in Vivo

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