Abstract
Receptor tyrosine kinases (RTKs) are cell surface transmembrane proteins responsible for intracellular signal transduction. They are expressed in several cell types and, after activation by growth factor binding, trigger a series of intracellular pathways, leading to a wide variety of cell responses (e.g., differentiation, proliferation, migration and invasion, angiogenesis, survival). Over-expression and / or structural alteration of RTKs family members are often associated to human cancers and tumor cells are known to use RTK transduction pathways to achieve tumor growth, angiogenesis and metastasis. Therefore, RTKs represent pivotal target in approaches of cancer therapy. A number of small molecules acting as RTK inhibitors have been synthesized by pharmaceutical companies and are under clinical trials, are being analyzed in animal models or have been successfully marketed. Liganddependent downregulation of RTKs is a critical step for modulating their activity and the adaptor Cbl has been indicated as the key protein involved in negative regulation of RTKs, such as EGF and HGF receptors. These data suggest novel potential pharmacological targets for the treatment of human malignancies associated to oncogenic activation of RTKs.
Keywords: Tyrosine Kinases, Anti-Cancer Therapy, Growth Factor Receptor, Signal transduction, Cancer, Downregulation
Current Pharmaceutical Design
Title: Receptor Tyrosine Kinases as Target for Anti-Cancer Therapy
Volume: 8 Issue: 22
Author(s): S. Brunelleschi, L. Penengo, M. M. Santoro and G. Gaudino
Affiliation:
Keywords: Tyrosine Kinases, Anti-Cancer Therapy, Growth Factor Receptor, Signal transduction, Cancer, Downregulation
Abstract: Receptor tyrosine kinases (RTKs) are cell surface transmembrane proteins responsible for intracellular signal transduction. They are expressed in several cell types and, after activation by growth factor binding, trigger a series of intracellular pathways, leading to a wide variety of cell responses (e.g., differentiation, proliferation, migration and invasion, angiogenesis, survival). Over-expression and / or structural alteration of RTKs family members are often associated to human cancers and tumor cells are known to use RTK transduction pathways to achieve tumor growth, angiogenesis and metastasis. Therefore, RTKs represent pivotal target in approaches of cancer therapy. A number of small molecules acting as RTK inhibitors have been synthesized by pharmaceutical companies and are under clinical trials, are being analyzed in animal models or have been successfully marketed. Liganddependent downregulation of RTKs is a critical step for modulating their activity and the adaptor Cbl has been indicated as the key protein involved in negative regulation of RTKs, such as EGF and HGF receptors. These data suggest novel potential pharmacological targets for the treatment of human malignancies associated to oncogenic activation of RTKs.
Export Options
About this article
Cite this article as:
Brunelleschi S., Penengo L., Santoro M. M. and Gaudino G., Receptor Tyrosine Kinases as Target for Anti-Cancer Therapy, Current Pharmaceutical Design 2002; 8 (22) . https://dx.doi.org/10.2174/1381612023393530
DOI https://dx.doi.org/10.2174/1381612023393530 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
CDK5 and MAPT Gene Expression in Alzheimer's Disease Brain Samples
Current Alzheimer Research Novel Target Sites for Drug Screening: A Special Reference to Cancer, Rheumatoid Arthritis and Parkinson’s Disease
Current Signal Transduction Therapy Activation of Myosin Phosphatase by Epigallocatechin-Gallate Sensitizes THP-1 Leukemic Cells to Daunorubicin
Anti-Cancer Agents in Medicinal Chemistry Scaffold Hopping for Identification of Novel PKCβII Inhibitors Based on Ligand and Structural Approaches, Virtual Screening and Molecular Dynamics Study
Combinatorial Chemistry & High Throughput Screening Signal Transduction Targets in Prostate Cancer
Current Signal Transduction Therapy Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme
Current Medicinal Chemistry Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds
Current Pharmaceutical Design Carotenoids as Modulators of Intracellular Signaling Pathways
Current Signal Transduction Therapy Anticancer Actions of Omega-3 Fatty Acids - Current State and Future Perspectives
Anti-Cancer Agents in Medicinal Chemistry Why Anticancer Nanomedicine Needs Sugars?
Current Medicinal Chemistry The Chemopreventive and Chemotherapeutic Potentials of Tea Polyphenols
Current Pharmaceutical Biotechnology SENP1 as A Biomarker for the Diagnosis of Cancer: Review of the Science and Published Patents
Recent Patents on Biomarkers Compounds From Celastraceae Targeting Cancer Pathways and Their Potential Application in Head and Neck Squamous Cell Carcinoma: A Review
Current Genomics MicroRNAs in Cancer Gene Therapy: Another Look
Current Cancer Therapy Reviews Interleukin-6/interleukin-6 Receptor Pathway as a New Therapy Target in Epithelial Ovarian Cancer
Current Pharmaceutical Design The Immunoregulatory Protein Human B7H3 is a Tumor-Associated Antigen that Regulates Tumor Cell Migration and Invasion
Current Cancer Drug Targets Targeted Therapies in Lung Cancers: Current Landscape and Future Prospects
Recent Patents on Anti-Cancer Drug Discovery Mitochondrial Signaling and Hepatocellular Carcinoma: Molecular Mechanisms and Therapeutic Implications
Current Pharmaceutical Design Stem Cell Pharmacogenomics
Current Topics in Medicinal Chemistry A Perspective on Stem Cells as Biological Systems that Produce Differentiated Osteoblasts and Odontoblasts
Current Stem Cell Research & Therapy