MS4322 / Icahn School of Medicine at Mount Sinai - LARVOL DELTA

MS4322 is a selective protein arginine methyltransferase 5 degrader with antitumor effects in cervical cancer cells. (PubMed, Oncol Rep) - "Mechanistically, MS4322 downregulated the expression of PRMT5, β‑catenin, Wnt‑3a, and c‑myc, while upregulating GSK‑3β, thereby inactivating the Wnt/β‑catenin pathway. These findings indicated that MS4322 exerted anti‑tumor effects via regulating the PRMT5/Wnt/β‑catenin pathway and may serve as a promising candidate agent for cervical cancer treatment."

Journal • Cervical Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • MYC • PRMT5

Discovery of a Potent and Selective Protein Arginine Methyltransferase 5 (PRMT5) PROTAC Degrader. (PubMed, J Med Chem) - "It displayed much improved PRMT5/MEP50 degradation potency over MS4322, which translated to better antiproliferative effect in both breast and prostate cancer cells. Overall, we discovered a highly potent and selective PRMT5/MEP50 complex degrader, which is an invaluable chemical biology tool and a potential cancer therapeutic."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • Targeted Protein Degradation • Von Hippel-Lindau Syndrome • PRMT5