Hit Finding & Assay Enablement for MGAT1, a Novel Glycosyl Transferase Involved in Cancer Cell Immune Evasion
- Identification of novel MGAT1 binders and inhibitors using two orthogonal discovery strategies: a UDPGlo™–based highthroughput enzymatic screen to identify functional inhibitors, and a DNAencoded library (DEL) screen to uncover compounds that bind MGAT1
- Mechanistic characterization of compound binding through the implementation of SPR competition assays, enabling direct interrogation of binding mode and target engagement
- Structural elucidation of ligand–MGAT1 interactions via highresolution crystal structures, revealing a welldefined binding site distinct from the active site and providing strong structural support for the proposed mechanism of action