Abstract
Heparanase is an endo-β-glucuronidase that degrades the glycosaminoglycan heparan sulfate, a major component of the extracellular matrix and basement membranes, and has been implicated in such processes as inflammation, angiogenesis and metastasis. The identification of inhibitors of heparanase is an attractive approach towards developing new therapeutics for metastatic tumours and chronic inflammatory diseases. This review focuses on heparanase inhibitors that have been isolated or synthesised to date. More recent developments in the understanding of heparanase structure and function that may ultimately aid in the future design of inhibitors with improved potency and specificity, are also discussed.
Keywords: heparanase, glucuronidase, heparan sulfate, metastasis, angiogenesis, inflammation, inhibitors
Mini-Reviews in Medicinal Chemistry
Title: The Development of Inhibitors of Heparanase, a Key Enzyme Involved in Tumour Metastasis, Angiogenesis and Inflammation
Volume: 4 Issue: 6
Author(s): Vito Ferro, Edward Hammond and Jon K. Fairweather
Affiliation:
Keywords: heparanase, glucuronidase, heparan sulfate, metastasis, angiogenesis, inflammation, inhibitors
Abstract: Heparanase is an endo-β-glucuronidase that degrades the glycosaminoglycan heparan sulfate, a major component of the extracellular matrix and basement membranes, and has been implicated in such processes as inflammation, angiogenesis and metastasis. The identification of inhibitors of heparanase is an attractive approach towards developing new therapeutics for metastatic tumours and chronic inflammatory diseases. This review focuses on heparanase inhibitors that have been isolated or synthesised to date. More recent developments in the understanding of heparanase structure and function that may ultimately aid in the future design of inhibitors with improved potency and specificity, are also discussed.
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Cite this article as:
Ferro Vito, Hammond Edward and Fairweather K. Jon, The Development of Inhibitors of Heparanase, a Key Enzyme Involved in Tumour Metastasis, Angiogenesis and Inflammation, Mini-Reviews in Medicinal Chemistry 2004; 4 (6) . https://dx.doi.org/10.2174/1389557043403729
DOI https://dx.doi.org/10.2174/1389557043403729 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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