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 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Withdrawal Notice: Emerging Biomarkers and Contributing Factors of Prostate Cancer
Current Cancer Therapy Reviews SCAP/SREBPs are Central Players in Lipid Metabolism and Novel Metabolic Targets in Cancer Therapy
Current Topics in Medicinal Chemistry Cancer Stem Cells in Pediatric Brain Tumors
Current Stem Cell Research & Therapy Dietary and Plant Polyphenols Exert Neuroprotective Effects and Improve Cognitive Function in Cerebral Ischemia
Recent Patents on Food, Nutrition & Agriculture Molecular Mechanisms Underlying Psychological Stress and Cancer
Current Pharmaceutical Design Promoters and Control Elements: Designing Expression Cassettes for Gene Therapy
Current Gene Therapy Identifying the Cellular Targets of Bioactive Small Molecules with Activity-Based Probes
Current Medicinal Chemistry Targeting the Akt/PI3K Signaling Pathway as a Potential Therapeutic Strategy for the Treatment of Pancreatic Cancer
Current Medicinal Chemistry RNA Silencing: Recent Developments on miRNAs
Recent Patents on DNA & Gene Sequences Relation Between Helicobacter Pylori Infection and Gastroduodenal Diseases
Current Cancer Therapy Reviews Microarray Profiling Analysis Uncovers Common Molecular Mechanisms of Rubella Virus, Human Cytomegalovirus, and Herpes Simplex Virus Type 2 Infections in ECV304 Cells
Current Molecular Medicine BRCA1-Associated Triple-Negative Breast Cancer and Potential Treatment for Ruthenium-Based Compounds
Current Cancer Drug Targets New Strategies and Patent Therapeutics in EBV-Associated Diseases
Mini-Reviews in Medicinal Chemistry Therapeutic Effects of Vitamin D in Asthma and Allergy
Mini-Reviews in Medicinal Chemistry Patented Biomarkers for the Early Detection of Ovarian Cancer
Recent Patents on Biomarkers C-Abl Tyrosine Kinase Signaling: A New Player in AD Tau Pathology
Current Alzheimer Research FGF10 and FGF21 as Regulators in Adipocyte Development and Metabolism
Endocrine, Metabolic & Immune Disorders - Drug Targets Small Molecule Drugs and Targeted Therapy for Melanoma: Current Strategies and Future Directions
Current Medicinal Chemistry Possible Role of DNA Methylation in the Induction of Systemic Lupus Erythematosus
Current Rheumatology Reviews Targeting Leukostasis for the Treatment of Early Diabetic Retinopathy
Cardiovascular & Hematological Disorders-Drug Targets