Heparanase: a rainbow pharmacological target associated to multiple pathologies including rare diseases

S Rivara, FM Milazzo, G Giannini - Future medicinal chemistry, 2016 - Future Science
S Rivara, FM Milazzo, G Giannini
Future medicinal chemistry, 2016Future Science
In recent years, heparanase has attracted considerable attention as a promising target for
innovative pharmacological applications. Heparanase is a multifaceted protein endowed
with enzymatic activity, as an endo-β-D-glucuronidase, and nonenzymatic functions. It is
responsible for the cleavage of heparan sulfate side chains of proteoglycans, resulting in
structural alterations of the extracellular matrix. Heparanase appears to be involved in major
human diseases, from the most studied tumors to chronic inflammation, diabetic …
In recent years, heparanase has attracted considerable attention as a promising target for innovative pharmacological applications. Heparanase is a multifaceted protein endowed with enzymatic activity, as an endo-β-D-glucuronidase, and nonenzymatic functions. It is responsible for the cleavage of heparan sulfate side chains of proteoglycans, resulting in structural alterations of the extracellular matrix. Heparanase appears to be involved in major human diseases, from the most studied tumors to chronic inflammation, diabetic nephropathy, bone osteolysis, thrombosis and atherosclerosis, in addition to more recent investigation in various rare diseases. The present review provides an overview on heparanase, its biological role, inhibitors and possible clinical applications, covering the latest findings in these areas.
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