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Discovery of the First-in-Class Protein Arginine Methyltransferase 1 PROTAC Degrader.
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ID: paper-41830641
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Discovery of the First-in-Class Protein Arginine Methyltransferase 1 PROTAC Degrader.
Guo S, Li J, Lin J, Chen Y, Liu C, Liu H, He Z, Zhu Y, Wang L, Yang F, Luo C, Li Z, Jin J, Ye F
Abstract
Protein arginine methyltransferase 1 (PRMT1) plays a critical role in cancer, yet current PRMT1 modulators lack selectivity and rely on enzymatic inhibition. Here, we developed first-in-class PRMT1-targeting PROTAC degrader compound 4, designed based on the pharmacophore of our previously developed PRMT1 inhibitor. Compound 4 potently induces PRMT1 degradation in a concentration-, time-, and proteasome-dependent manner and exhibits high selectivity, with no detectable degradation of other common...
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