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
-
Preferentially Expressed Antigen in Melanoma (PRAME) and the PRAME Family of Leucine-Rich Repeat Proteins
Current Cancer Drug Targets Preparation of Hymenialdisine, Analogues and Their Evaluation as Kinase Inhibitors
Current Medicinal Chemistry Anti-Tumor Activity of Non-Nucleosidic Reverse Transcriptase Inhibitors
Current Pharmaceutical Design Perinatal Management of Fetal Tumors
Current Pediatric Reviews The Ubiquitin-Proteasome System as a Prospective Molecular Target for Cancer Treatment and Prevention
Current Protein & Peptide Science Management of Incidental Findings in the Era of Next-generation Sequencing
Current Genomics Targeted Therapies for Advanced Non-Small Cell Lung Cancer
Combinatorial Chemistry & High Throughput Screening Fas Ligand Gene Therapy for Vascular Intimal Hyperplasia
Current Gene Therapy Patented Biomarkers for the Early Detection of Ovarian Cancer
Recent Patents on Biomarkers Apoptosis in Sepsis: Mechanisms, Clinical Impact and Potential Therapeutic Targets
Current Pharmaceutical Design Antisense Oligonucleotides as an Innovative Therapeutic Strategy in the Treatment of High-Grade Gliomas
Recent Patents on CNS Drug Discovery (Discontinued) An Investigative Approach to Treatment Modalities for Squamous Cell Carcinoma of Skin
Current Drug Delivery Ribonucleases and ImmunoRNases as Anticancer Drugs
Current Pharmaceutical Design Late Effects in Survivors of Childhood CNS Tumors: Review of Results From the Two Largest Survivorship Cooperative Groups
Current Cancer Therapy Reviews Aberrant Splicing, Hyaluronan Synthases and Intracellular Hyaluronan as Drivers of Oncogenesis and Potential Drug Targets
Current Cancer Drug Targets Nanostructural Hybrid Sensitizers for Photodynamic Therapy
Current Pharmaceutical Design From Body Art to Anticancer Activities: Perspectives on Medicinal Properties of Henna
Current Drug Targets The Epigenetic Origin of Aneuploidy
Current Genomics Role of Natural Phenolic Compounds in Cancer Chemoprevention via Regulation of the Cell Cycle
Current Pharmaceutical Biotechnology Compounds From Celastraceae Targeting Cancer Pathways and Their Potential Application in Head and Neck Squamous Cell Carcinoma: A Review
Current Genomics