Abstract
Clarification of the molecular mechanisms of oncogenesis and drug resistance is a prerequisite for the development of new treatment strategies like molecularly targeted therapies. Recent studies demonstrate that EphA2 is overexpressed in human cancers and that EphA2 increases tumor invasion and survival. Thus, an EphA2 receptor antagonist, such as a specific tyrosine kinase inhibitor (in the form of an antibody, small molecule, peptide, or siRNA) or an antibody – drug conjugate that targets the EphA2 receptor could be the basis for a novel targeted antineoplastic therapy. This review summarizes the role of EphA2 in tumorigenesis and the development of EphA2 receptor antagonists as candidate anti-cancer agents. We suggests that continued research into the function of EphA2 signaling in the pathobiology of neoplasia could lead to more rationally designed therapeutics targeting EphA2 in solid tumors.
Keywords: Cancer, drug target, EphA, neoplasms, anticancer therapy, tyrosine kinase inhibitor, microvessel density, receptor tyrosine kinases, vascular endothelial cadherin, mitogen-activated protein kinase
Current Cancer Drug Targets
Title: EphA2-Dependent Molecular Targeting Therapy for Malignant Tumors
Volume: 11 Issue: 9
Author(s): RONG Biao-xue, CAI Xi-guang, YANG Shuan-ying, LI Wei and MING Zong-juan
Affiliation:
Keywords: Cancer, drug target, EphA, neoplasms, anticancer therapy, tyrosine kinase inhibitor, microvessel density, receptor tyrosine kinases, vascular endothelial cadherin, mitogen-activated protein kinase
Abstract: Clarification of the molecular mechanisms of oncogenesis and drug resistance is a prerequisite for the development of new treatment strategies like molecularly targeted therapies. Recent studies demonstrate that EphA2 is overexpressed in human cancers and that EphA2 increases tumor invasion and survival. Thus, an EphA2 receptor antagonist, such as a specific tyrosine kinase inhibitor (in the form of an antibody, small molecule, peptide, or siRNA) or an antibody – drug conjugate that targets the EphA2 receptor could be the basis for a novel targeted antineoplastic therapy. This review summarizes the role of EphA2 in tumorigenesis and the development of EphA2 receptor antagonists as candidate anti-cancer agents. We suggests that continued research into the function of EphA2 signaling in the pathobiology of neoplasia could lead to more rationally designed therapeutics targeting EphA2 in solid tumors.
Export Options
About this article
Cite this article as:
Biao-xue RONG, Xi-guang CAI, Shuan-ying YANG, Wei LI and Zong-juan MING, EphA2-Dependent Molecular Targeting Therapy for Malignant Tumors, Current Cancer Drug Targets 2011; 11 (9) . https://dx.doi.org/10.2174/156800911798073050
DOI https://dx.doi.org/10.2174/156800911798073050 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
- 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
-
Optimising the Azeotropic Drying of 18F-Fluorine Wayto Improve the 18F-Fluorocholine Radiochemical Yield
Current Radiopharmaceuticals FADS1 is a Prognostic Biomarker in Bladder Cancer: A Study Based on TCGA Data
Combinatorial Chemistry & High Throughput Screening Suppression of Cancer Invasiveness by Dietary Compounds
Mini-Reviews in Medicinal Chemistry The Emerging Role of Coenzyme Q-10 in Aging, Neurodegeneration, Cardiovascular Disease, Cancer and Diabetes Mellitus
Current Neurovascular Research Collateral Damage Control in Cancer Therapy: Defining the Stem Identity in Gliomas
Current Pharmaceutical Design Comparison of Artemisia annua Bioactivities between Traditional Medicine and Chemical Extracts
Current Bioactive Compounds Trace of Long Non-Coding RNAs in Signaling Pathways in Thyroid Cancer
Current Signal Transduction Therapy Phytochemicals Resveratrol and Sulforaphane as Potential Agents for Enhancing the Anti-Tumor Activities of Conventional Cancer Therapies
Current Pharmaceutical Biotechnology The NK-1 Receptor: A New Target in Cancer Therapy
Current Drug Targets The Accomplices of NF-κB Lead to Radioresistance
Current Protein & Peptide Science Crosstalk Between Epidermal Growth Factor Receptor- and Insulin-Like Growth Factor-1 Receptor Signaling: Implications for Cancer Therapy
Current Cancer Drug Targets Estrogen Catechols Detection as Biomarkers in Schistosomiasis Induced Cancer and Infertility
Letters in Drug Design & Discovery Cyclin Dependent Kinase 1 Inhibitors: A Review of Recent Progress
Current Medicinal Chemistry Development of Peptide and Protein Based Radiopharmaceuticals
Current Pharmaceutical Design Exploring the Role of Phytochemicals as Potent Natural Photosensitizers in Photodynamic Therapy
Anti-Cancer Agents in Medicinal Chemistry Identification of a RhoA- and SRF-Dependent Mechanism of Androgen Action that is Associated with Prostate Cancer Progression
Current Drug Targets Metals and Metal Derivatives in Medicine
Mini-Reviews in Medicinal Chemistry Gadd45 Proteins as Critical Signal Transducers Linking NF-κB to MAPK Cascades
Current Cancer Drug Targets Hybrid PET/MRI for In Vivo Imaging of Cancer: Current Clinical Experiences and Recent Advances
Current Medical Imaging Novel Approaches Towards Designing of Isoform-Selective Inhibitors Against Class II Histone Deacetylases: The Acute Requirement for Targetted Anticancer Therapy
Current Topics in Medicinal Chemistry