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Curr Opin Biotechnol. 2009 Dec;20(6):678-84. doi: 10.1016/j.copbio.2009.10.009. Epub 2009 Nov 4.

Pharmacological significance of glycosylation in therapeutic proteins.

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GlycoFi, Inc., a wholly-owned subsidiary of Merck & Co., Inc. 21 Lafayette St., Suite 200, Lebanon, NH 03766, United States.


Glycoproteins represent the major share of marketed and clinical development phase therapeutic proteins. A thorough understanding of the nature and function of the carbohydrate moiety and its impact on pharmacology properties is essential in discovering and developing safe and efficacious glycoprotein biopharmaceuticals. This review summarizes the processes of N-linked and O-linked glycosylation and both established and emerging platforms for expression of recombinant glycoproteins. Recent or illustrative examples of N-linked and/or O-linked glycosylation impacting drug pharmacology properties (including activity, pharmacokinetics, clearance, and immunogenicity) of marketed and developing therapeutic proteins are presented.

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