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PST3.1a is a first-in-class small molecule inhibitor of N-acetylglucosaminyltransferase V (GnT-V), an enzyme encoded by the MGAT5 gene. Developed by Phost'In Therapeutics, this compound targets the aberrant N-glycosylation of proteins, a hallmark of cancer progression that facilitates metastasis and immune system evasion. By specifically inhibiting GnT-V, PST3.1a reduces the branching of N-glycans on the surface of tumor cells, which in turn stabilizes cell-cell adhesion and restores the visibility of the tumor to the immune system. The drug is currently being evaluated in Phase 1 clinical trials for patients with advanced solid tumors, including glioblastoma and colorectal cancer, where GnT-V is frequently overexpressed.
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