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

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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Bibliographic Details
Main Author: Yong Ju (1404961) (author)
Other Authors: Huizhu Song (18279722) (author), Yuelan He (21567958) (author), Yingtung Lo (19359617) (author), Zhipeng Fan (110971) (author), Jianzhong Lu (480003) (author)
Published: 2025
Subjects:
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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