New Case Study: Discovery of GALNT3 Inhibitors Using a Universal Glycosyltransferase Assay and Orthogonal Pooled Screening

Glycosyltransferase (GT) enzymes participate in diverse metabolic and regulatory roles by catalyzing the transfer of sugars to protein, lipid and carbohydrate acceptors as well as to other molecules. Within the GT family, there are over 20 distinct polypeptide N-acetylgalactosaminyltransferases (GALNTs) that catalyze the initial step of O-glycosylation. GALNT3 overexpression and dysregulation has been directly linked to multiple cancers, making it a compelling target for drug discovery, and the one we chose for development of an HTS workflow with the Transcreener^® UDP² Assay and Orthogonal Pooled Screening technology.

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In this case study, learn how to:

• Develop an HTS workflow for GTs with an optimized Transcreener^® UDP² Assay (FP and TR-FRET formats)
• Use the assay to measure GT activity and determine K_m values
• Run a pilot screen for specific enzyme inhibitors on 8,000 compounds using Orthogonal Pooled Screening (OPS™) technology
• Confirm, validate, and characterize hits

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Transcreener is the only HTS-compatible glycosyltransferase assay method allows direct detection of reaction products without the use of coupling enzymes.