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Semin Thromb Hemost 2021; 47(03): 316-332
DOI: 10.1055/s-0041-1725067
Review Article

Development of Molecules Antagonizing Heparan Sulfate Proteoglycans

Tanja Gerlza
1   Karl-Franzens University Graz, Institute of Pharmaceutical Sciences, Graz, Austria
,
Christina Trojacher
1   Karl-Franzens University Graz, Institute of Pharmaceutical Sciences, Graz, Austria
,
Nikola Kitic
1   Karl-Franzens University Graz, Institute of Pharmaceutical Sciences, Graz, Austria
,
Tiziana Adage
2   Antagonis Biotherapeutics GmbH, Graz, Austria
,
Andreas J. Kungl
1   Karl-Franzens University Graz, Institute of Pharmaceutical Sciences, Graz, Austria
2   Antagonis Biotherapeutics GmbH, Graz, Austria
› Author Affiliations
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Abstract

Heparan sulfate proteoglycans (HSPGs) occur in almost every tissue of the human body and consist of a protein core, with covalently attached glycosaminoglycan polysaccharide chains. These glycosaminoglycans are characterized by their polyanionic nature, due to sulfate and carboxyl groups, which are distributed along the chain. These chains can be modified by different enzymes at varying positions, which leads to huge diversity of possible structures with the complexity further increased by varying chain lengths. According to their location, HSPGs are divided into different families, the membrane bound, the secreted extracellular matrix, and the secretory vesicle family. As members of the extracellular matrix, they take part in cell–cell communication processes on many levels and with different degrees of involvement. Of particular therapeutic interest is their role in cancer and inflammation as well as in infectious diseases. In this review, we give an overview of the current status of medical approaches to antagonize HSPG function in pathology.

Keywords

heparan sulfate proteoglycan glycosaminoglycans - glypicans - syndecans - antibodies - GAG mimetic - chemokines - inflammation - cancer


Publication History

Article published online:
01 April 2021

© 2021. Thieme. All rights reserved.

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