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Heparanase is an endoglycosidase enzyme that cleaves heparan sulfate (HS) chains found on heparan sulfate proteoglycans (HSPGs) in the extracellular matrix and at cell surfaces. It plays a key role in ECM remodeling, growth factor release, and cell migration, and is overexpressed in many cancers, promoting tumor growth, angiogenesis, and metastasis. It is also implicated in inflammation, fibrosis, diabetic nephropathy and bone osteolysis, making it a potential therapeutic target.
Heparanase inhibitors block the enzymatic activity of heparanase, preventing the degradation of heparan sulfate and subsequent release of growth factors and remodeling of the extracellular matrix. Monoclonal antibodies targeting heparanase inhibit its activity and block its interaction with the tumor microenvironment.
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