Abstract
Eph receptors are a unique family of receptor tyrosine kinases (RTK) that play critical roles in embryonic patterning, neuronal targeting, and vascular development during normal embryogenesis. Eph RTKs and their ligands, the ephrins, are also frequently overexpressed in a variety of cancers and tumor cell lines. In particular, one family member, EphA2, is overexpressed in breast, prostate, lung, and colon cancers. Unlike traditional oncogenes that often function only in tumor cells, recent data show that Eph receptors mediate cellcell interactions both in tumor cells and in the tumor microenvironment, namely the tumor stroma and tumor vasculature. Thus, EphA2 receptors are attractive targets for drug design, as targeting these molecules could simultaneously inhibit several aspects of tumor progression. This review focuses on the multiple roles of EphA2 in cancer progression, the mechanisms by which EphA2 inhibition may halt this progression, and the pre-clinical results of EphA2 inhibition in various cancer model systems.
Keywords: eph receptor tyrosine kinases, ephrin ligands, tumor progression, angiogenesis
Current Cancer Drug Targets
Title: EphA2 Receptor Tyrosine Kinase as a Promising Target for Cancer Therapeutics
Volume: 5 Issue: 3
Author(s): Renee C. Ireton and Jin Chen
Affiliation:
Keywords: eph receptor tyrosine kinases, ephrin ligands, tumor progression, angiogenesis
Abstract: Eph receptors are a unique family of receptor tyrosine kinases (RTK) that play critical roles in embryonic patterning, neuronal targeting, and vascular development during normal embryogenesis. Eph RTKs and their ligands, the ephrins, are also frequently overexpressed in a variety of cancers and tumor cell lines. In particular, one family member, EphA2, is overexpressed in breast, prostate, lung, and colon cancers. Unlike traditional oncogenes that often function only in tumor cells, recent data show that Eph receptors mediate cellcell interactions both in tumor cells and in the tumor microenvironment, namely the tumor stroma and tumor vasculature. Thus, EphA2 receptors are attractive targets for drug design, as targeting these molecules could simultaneously inhibit several aspects of tumor progression. This review focuses on the multiple roles of EphA2 in cancer progression, the mechanisms by which EphA2 inhibition may halt this progression, and the pre-clinical results of EphA2 inhibition in various cancer model systems.
Export Options
About this article
Cite this article as:
Ireton C. Renee and Chen Jin, EphA2 Receptor Tyrosine Kinase as a Promising Target for Cancer Therapeutics, Current Cancer Drug Targets 2005; 5 (3) . https://dx.doi.org/10.2174/1568009053765780
DOI https://dx.doi.org/10.2174/1568009053765780 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
Enteral Administration of TKIs: Report of a Response to Ceritinib in an ALK-positive NSCLC Patient and Literature Review
Current Drug Targets Editorial [Hot Topic:Recent Advances in Developmental and Reproductive Toxicology (Executive Editor: Gian Mario Tiboni )]
Current Pharmaceutical Design Estrogen Receptor-Positive and Estrogen Receptor-Negative Human Breast Cancer Cells: Regulation of Expression of Cancer-Related Genes by Estradiol and Tamoxifen
Current Signal Transduction Therapy Nose to Brain Delivery of Nanoformulations for Neurotherapeutics in Parkinson’s Disease: Defining the Preclinical, Clinical and Toxicity Issues
Current Drug Delivery Targeting Peroxisome Proliferator-Activated Receptor Gamma for Generation of Antidiabetic Drug
Current Diabetes Reviews A Review of the Chemical and Pharmacological Aspects of the Genus Marrubium
Current Pharmaceutical Design Androgen Receptor in Human Health: A Potential Therapeutic Target
Current Drug Targets Pharmacodynamics of Radiolabelled Anticancer Drugs for Positron Emission Tomography
Current Pharmaceutical Design Thiazolidinone Constraint Combretastatin Analogs as Novel Antitubulin Agents: Design, Synthesis, Biological Evaluation and Docking Studies
Anti-Cancer Agents in Medicinal Chemistry Advances in Vaccine Adjuvants For Infectious Diseases
Current HIV Research Exploiting Internal Ribosome Entry Sites in Gene Therapy Vector Design
Current Gene Therapy Pharmacokinetics of Antifungal Agents in Neonates and Young Infants
Current Medicinal Chemistry Intraoperative Localisation of Impalpable Breast Lesions Utilising the ROLLIS Technique Following Peritumoral <sup>99m</sup>Tc-colloid Sentinel Node Lymphoscintigraphy
Current Radiopharmaceuticals Alpha-1-Adrenergic Receptor Blockade Modifies Insulin-Regulated Aminopeptidase (IRAP) Activity in Rat Prostate and Modulates Oxytocin Functions
Drug Metabolism Letters The JAK-STAT Pathway: A Therapeutic Target in Hematological Malignancies
Current Cancer Drug Targets Computer Techniques for Drug Development from Thai Traditional Medicine
Current Pharmaceutical Design Regulation of Apoptosis and Activity of the Osteoclast
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Myeloproliferative Neoplasms Including Polycythemia Vera, Essential Thrombocythemia, and Primary Myelofibrosis, Chronic Neutrophilic Leukemia, and Myeloproliferative Neoplasm, Unclassifiable
Current Cancer Therapy Reviews Emerging Roles of Meis1 in Cardiac Regeneration, Stem Cells and Cancer
Current Drug Targets Epigenetic Modulation: A Promising Avenue to Advance Hematopoietic Stem Cell-Based Therapy for Severe Autoimmune Disorders
Epigenetic Diagnosis & Therapy (Discontinued)