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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Nucleo-Cytoplasmic Transport of Proteins as a Target for Therapeutic Drugs
Current Medicinal Chemistry The Role of Androgen Receptor Mutations in Prostate Cancer Progression
Current Genomics Meet Our Editorial Board Member
Protein & Peptide Letters License to Kill Tumors: How Much Hope is Justified for Trail?
Current Pharmaceutical Design Synthesis of Biologically Active Selenium-Containing Molecules From Greener Perspectives
Current Green Chemistry Rationale Design, Synthesis, Cytotoxicity Evaluation, and Molecular Docking Studies of 1,3,4-oxadiazole Analogues
Anti-Cancer Agents in Medicinal Chemistry RING-, HECT-, and RBR-type E3 Ubiquitin Ligases: Involvement in Human Cancer
Current Cancer Drug Targets Linking Biosynthetic Gene Clusters to their Metabolites via Pathway- Targeted Molecular Networking
Current Topics in Medicinal Chemistry Electrochemotherapy as First Line Cancer Treatment: Experiences from Veterinary Medicine in Developing Novel Protocols
Current Cancer Drug Targets Mortality and Morbidity of HIV Infected Patients Receiving HAART: A Cohort Study
Current HIV Research Targeting Protein Kinase Inhibitors with Traditional Chinese Medicine
Current Drug Targets Recent Progress on Neutralizing Antibodies against Hepatitis B Virus and its Implications
Infectious Disorders - Drug Targets Targeting Kinases in Cancer Therapies: Adverse Effects on Blood Platelets
Current Pharmaceutical Design Structure-Based Approach for the Discovery of Novel Selective Estrogen Receptor Modulators
Current Medicinal Chemistry Emerging Physical Approaches for Promoting siRNA Intracellular Delivery for Cancer Therapy
Current Organic Chemistry Protein Kinase CK2 Inhibitors: Emerging Anticancer Therapeutic Agents?
Anti-Cancer Agents in Medicinal Chemistry Neuropeptides as Autocrine Growth Factors in Cancer Cells
Current Pharmaceutical Design Image-Guided Drug Delivery with Single-Photon Emission Computed Tomography: A Review of Literature
Current Drug Targets Plasmid DNA Gene Therapy by Electroporation: Principles and Recent Advances
Current Gene Therapy Editorial [Hot Topic: The Impact of Microbiota and Cytokines on Inflammatory Bowel Disease (Executive Editors: Osamu Kanauchi and Keiichi Mitsuyama)]
Current Pharmaceutical Design