Weifeng Mao

Discovery of GTA182, a Novel CNS-Active Tricyclic Amide MTA-Cooperative PRMT5 Inhibitor for MTAP -Deleted Cancers

Abstract Developing central nervous system (CNS) active, MTA-cooperative PRMT5 inhibitors for MTAP-deleted malignancies represents a formidable challenge. Here, we report the discovery of GTA182 via structure-based drug design. Multi-parameter optimization balanced single-digit n...