Discovery of Inhibitors of GALNT3 by Orthogonal Pooled Screening with a Universal Glycosyltransferase Assay

Glycosyltransferase (GTs) are enzymes that participate in diverse metabolic and regulatory roles. Of more than 200 GTs, there are over 20 distinct polypeptide N-acetylgalactosaminyltransferases (GALNTs) that catalyze the initial step of O-glycosylation. Over expression of one of these GTs, GALNT3, has been directly linked to multiple cancers, making it a compelling target for drug discovery. Development of an HTS workflow for GALNT3 is described here.