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7-Fluorosialyl Glycosides Are Hydrolysis Resistant but Readily Assembled by Sialyltransferases Providing Easy Access to More Metabolically Stable Glycoproteins

Andreas Geissner, Lars Baumann, Thomas Morley, Andrew K. Wong, Lyann Sim, Jamie R. Rich, Pauline Pl So, Edie Dullaghan, Étienne Lessard, Umar Iqbal, María Moreno, Warren W. Wakarchuk, Stephen G. Withers

2021ACS Central Science28 citationsDOIOpen Access PDF

Abstract

pharmacokinetic studies reveal enhanced half-life of the protein decorated with 7-fluorosialic acid relative to unmodified sialic acid in the murine circulatory system. 7-Fluorosialylation therefore offers considerable promise as a means of prolonging circulatory half-lives of glycoproteins and may pave the way toward biobetters for therapeutic use.

Topics & Concepts

Sialic acidGlycoproteinBiochemistryGlycanChemistrySialyltransferaseSialidaseHydrolysisN-Acetylneuraminic acidNeuraminidaseEnzymeGlycosylation and Glycoproteins ResearchMonoclonal and Polyclonal Antibodies ResearchViral Infectious Diseases and Gene Expression in Insects
7-Fluorosialyl Glycosides Are Hydrolysis Resistant but Readily Assembled by Sialyltransferases Providing Easy Access to More Metabolically Stable Glycoproteins | Litcius