Journal
FUTURE MEDICINAL CHEMISTRY
Volume 8, Issue 6, Pages 647-680Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0012
Keywords
angiogenesis; cancer and metastasis; endo-beta-D-glucuronidase; heparanase; heparanase structure; heparanase inhibitors; heparanase in vitro assays; inflammation; modified heparins; rare diseases
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Funding
- Sigma-Tau Research Switzerland S.A. (Mendrisio, CH)
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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-beta-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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