Development of Molecules Antagonizing Heparan Sulfate Proteoglycans

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.

Hemostatic and Nonhemostatic Effects of Heparan Sulfate Proteoglycans

“…Gerlza et al then provide insights into the development of new drug compositions and methods targeting HSPGs and heparanase in cancer and inflammatory diseases. 9 These studies are ongoing and will hopefully pave the way to novel strategies in cancer and rheumatic treatment.…”