References: |
PRMT5 is a protein arginine methyltransferase (PRMT) that is reported to have a role in diverse cellular processes, including tumorigenesis. PRMT5 overexpression is observed in cell lines and primary patient samples derived from a number of cancers, including lymphomas, lung cancer, breast cancer and colorectal cancer. GSK3326595 (formerly EPZ015938), a highly selective and orally bioavailable small molecule, is the first PRMT5 inhibitor and the third epigenetic investigational therapy derived from Epizyme’s proprietary discovery platform to enter the clinic. |