MS4322 is a First-in-Class PRMT5 PROTAC Degrader
PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...
MRTX9768 is an Orally Active PRMT5 Inhibitor
PRMT5 is the main type II enzyme. It catalyzes symmetric dimethylarginine of histone proteins to induce gene silencing by generating repressive histone marks. PRMT5 can also methylate nonhistone proteins such as the transcription factors p53 and p65. Modifications of these proteins by PRMT5 have relations with diverse cellular processes....