Abstract
Hepatocyte growth factor (HGF) plays a plethora of roles in the progression of many invasive and metastatic cancers. The interaction between tumour cells and their surrounding stromal environment remains a crucial factor governing tumour invasion and metastasis. HGF is primarily synthesised by stromal fibroblasts as an inactive precursor known as pro-HGF. A number of proteases have demonstrated the ability to convert pro-HGF into the biologically active form of HGF, although the two main factors responsible are HGF activator (HGFA) and matriptase. The HGF activation inhibitors (HAI-1 and HAI-2) are two novel Kunitz-type serine protease inhibitors that regulate HGFA and matriptase activity to govern the influence of HGF within the body. Deregulation of HAI expression can lead to shift in the HGF activation/inhibition balance ratio in favour of enhanced HGF production. Therefore, these HGF activation inhibitors may have a direct bearing on cancer invasion and metastasis. This review examines the accumulating evidence on the emerging role and therapeutic potential of HAI-1 and HAI-2 in cancer.
Keywords: Hepatocyte growth factor, matriptase, HGF activator, HGF inhibitor, HAI-1, HAI-2, prognosis
Anti-Cancer Agents in Medicinal Chemistry
Title: Hepatocyte Growth Factor Activation Inhibitors – Therapeutic Potential in Cancer
Volume: 10 Issue: 1
Author(s): Christian Parr, Andrew J. Sanders and Wen G. Jiang
Affiliation:
Keywords: Hepatocyte growth factor, matriptase, HGF activator, HGF inhibitor, HAI-1, HAI-2, prognosis
Abstract: Hepatocyte growth factor (HGF) plays a plethora of roles in the progression of many invasive and metastatic cancers. The interaction between tumour cells and their surrounding stromal environment remains a crucial factor governing tumour invasion and metastasis. HGF is primarily synthesised by stromal fibroblasts as an inactive precursor known as pro-HGF. A number of proteases have demonstrated the ability to convert pro-HGF into the biologically active form of HGF, although the two main factors responsible are HGF activator (HGFA) and matriptase. The HGF activation inhibitors (HAI-1 and HAI-2) are two novel Kunitz-type serine protease inhibitors that regulate HGFA and matriptase activity to govern the influence of HGF within the body. Deregulation of HAI expression can lead to shift in the HGF activation/inhibition balance ratio in favour of enhanced HGF production. Therefore, these HGF activation inhibitors may have a direct bearing on cancer invasion and metastasis. This review examines the accumulating evidence on the emerging role and therapeutic potential of HAI-1 and HAI-2 in cancer.
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Cite this article as:
Parr Christian, Sanders J. Andrew and Jiang G. Wen, Hepatocyte Growth Factor Activation Inhibitors – Therapeutic Potential in Cancer, Anti-Cancer Agents in Medicinal Chemistry 2010; 10 (1) . https://dx.doi.org/10.2174/1871520611009010047
DOI https://dx.doi.org/10.2174/1871520611009010047 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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