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The glycosyltransferase, N-acetylglucosaminyltransferase V (GnT-V) is a newly discovered single-flippase enzyme that is known to play a critical role in GnT-V-mediated biosynthesis of the complex glycans that are present on the cell surface. Recent studies have shown that GnT-V is a promising therapeutic target for development of anti-inflammatory agents and anti-cancer therapies. This review highlights the applications of such target-specific GnT-V inhibitors and sets forth the new approaches for the development of GnT-V inhibitors that interfere with the endogenous activity of this enzyme.The Other Side of the Story

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