Abstract
c-Met, also known as the surface receptor of hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase with heterodimer transmembrane. c-Met involves in the activation of several signaling pathways, most of them are implicated in aggressive cancer phenotypes. In a variety of human malignances, c-Met/HGF signaling has been found aberrant, and in many instances, has been correlated with advanced disease stage and poor prognosis. Thus, the c-Met has identified as an emerging and interesting target for cancer chemotherapy. In this review, we briefly summarize signaling pathways of c-Met, and discuss the crystal structures of representative c-Met and the binding modes with their ligands. We also present updates on the design, synthesis and structure-activity relationship analysis of c-Met inhibitors developed from 2014 till now. At last, we review the c-Met inhibitors that are in clinical development and highlight the future prospects.
Keywords: c-Met inhibitors, hepatocyte growth factor receptor (HGFR), ATP-competitive inhibitors, anticancer agents, structure-activity relationship analysis, binding modes.
Current Medicinal Chemistry
Title:Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present)
Volume: 24 Issue: 1
Author(s): Peng-Cheng Lv, Zhong-Chang Wang and Hai-Liang Zhu
Affiliation:
Keywords: c-Met inhibitors, hepatocyte growth factor receptor (HGFR), ATP-competitive inhibitors, anticancer agents, structure-activity relationship analysis, binding modes.
Abstract: c-Met, also known as the surface receptor of hepatocyte growth factor receptor (HGFR), is a receptor tyrosine kinase with heterodimer transmembrane. c-Met involves in the activation of several signaling pathways, most of them are implicated in aggressive cancer phenotypes. In a variety of human malignances, c-Met/HGF signaling has been found aberrant, and in many instances, has been correlated with advanced disease stage and poor prognosis. Thus, the c-Met has identified as an emerging and interesting target for cancer chemotherapy. In this review, we briefly summarize signaling pathways of c-Met, and discuss the crystal structures of representative c-Met and the binding modes with their ligands. We also present updates on the design, synthesis and structure-activity relationship analysis of c-Met inhibitors developed from 2014 till now. At last, we review the c-Met inhibitors that are in clinical development and highlight the future prospects.
Export Options
About this article
Cite this article as:
Lv Peng-Cheng, Wang Zhong-Chang and Zhu Hai-Liang, Recent Advances in the Design and Synthesis of c-Met Inhibitors as Anticancer Agents (2014-Present), Current Medicinal Chemistry 2017; 24 (1) . https://dx.doi.org/10.2174/0929867323666161028161441
DOI https://dx.doi.org/10.2174/0929867323666161028161441 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![](/images/wayfinder.jpg)
- 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
- Announcements
Related Articles
-
Quercetin in Attenuation of Ischemic/Reperfusion Injury: A Review
Current Molecular Pharmacology Mitochondrial DNA Mutations in Cancer: A Review
Current Topics in Medicinal Chemistry Silymarin in the Prevention and Treatment of Liver Diseases and Primary Liver Cancer
Current Pharmaceutical Biotechnology Circulating Biomarkers for Tumor Angiogenesis: Where Are We?
Current Medicinal Chemistry Regulation of Cell Growth by Estrogen Signaling and Potential Targets in Thyroid Cancer
Current Cancer Drug Targets Tumor Stroma as a Target in Cancer
Current Cancer Drug Targets Small Molecules as Drugs to Upregulate Metastasis Suppressors in Cancer Cells
Current Medicinal Chemistry In Vivo Cellular Imaging for Translational Medical Research
Current Medical Imaging Herbal Phytochemicals as Immunomodulators
Current Immunology Reviews (Discontinued) Vascular Endothelial Growth Factor: A New Paradigm for Targeting Various Diseases
Current Angiogenesis (Discontinued) Thiazolidinediones and Type 2 Diabetes: From Cellular Targets to Cardiovascular Benefit
Current Drug Targets Pharmacological Inhibitors of NAD Biosynthesis as Potential An ticancer Agents
Recent Patents on Anti-Cancer Drug Discovery Targeting EZH2 for Cancer Therapy: Progress and Perspective
Current Protein & Peptide Science CRISPR/Cas9 Genome Editing Tool: A Promising Tool for Therapeutic Applications on Respiratory Diseases
Current Gene Therapy New Indications for Established Drugs: Combined Tumor-Stroma-Targeted Cancer Therapy with PPARγ Agonists, COX-2 Inhibitors, mTOR Antagonists and Metronomic Chemotherapy
Current Cancer Drug Targets Non-steroidal Anti-Inflammatory Drugs and Melanoma
Current Pharmaceutical Design Endothelin Receptors in Gastrointestinal Smooth Muscle
Current Protein & Peptide Science HTLV-1-Associated Myelopathy/Tropical Spastic Paraparesis (HAM/TSP) Inflammatory Network
Inflammation & Allergy - Drug Targets (Discontinued) Preclinical Evaluation of a Monoclonal Antibody (3C6) Specific for Prostate-Specific Membrane Antigen
Current Radiopharmaceuticals Identification of a RhoA- and SRF-Dependent Mechanism of Androgen Action that is Associated with Prostate Cancer Progression
Current Drug Targets