Pharmacological significance of glycosylation in therapeutic proteins.
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.
Li
Huijuan
H
GlycoFi, Inc., a wholly-owned subsidiary of Merck & Co., Inc. 21 Lafayette St., Suite 200, Lebanon, NH 03766, United States. Huijuan_li@merck.com
d'Anjou
Marc
M
D000818:Animals; D001688:Biological Products / Q000378:metabolism; D001702:Biopharmaceutics / Q000379:methods*; D001709:Biotechnology / Q000639:trends*; D002241:Carbohydrates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006023:Glycoproteins / Q000737:chemistry / Q000378:metabolism; D006031:Glycosylation; D006801:Humans; D007107:Immune System; D011485:Protein Binding; D011506:Proteins / Q000627:therapeutic use*; D011994:Recombinant Proteins / Q000737:chemistry
D001688:Biological Products; D002241:Carbohydrates; D006023:Glycoproteins; D011506:Proteins; D011994:Recombinant Proteins