Abstract
Members of epidermal growth factor receptor (EGFR) or ErbB receptor family play a critical role in a wide range of human cancers. In the past decade, there has been a remarkable progress in developing ErbB targeted therapeutics. However, a substantial portion of patients has non-responsive disease or subsequently shows evidence of tumour relapse following initial success with anti-ErbB agents. Improved insights into the biology of ErbB receptor family have led to more effective second- and third-generation anti-ErbB therapies. In this review, we have summarised salient features of the ErbB receptor physiology and highlighted key mechanisms involved in abnormal ErbB signalling in tumorigenesis. The rationale of anti-ErbB receptor therapies are outlined along with key mechanisms proposed for resistance to treatment as well as the current concept of combined anti-ErbB therapies. In conclusion, improved understanding of the molecular pathways that confer resistance to anti-ErbB therapeutics will be essential in minimising tumour resistance to ErbB targeted treatments.
Keywords: EGFR, ErbB, receptor tyrosine kinase, monoclonal antibodies, small molecule inhibitors, cancers, tumorigenesis, tumour resistance, dimerization, gene amplifications
Current Pharmaceutical Design
Title:Targeting the EGFR-family for Therapy: Biological Challenges and Clinical Perspective
Volume: 18 Issue: 19
Author(s): Rachana Patel and Hing Y. Leung
Affiliation:
Keywords: EGFR, ErbB, receptor tyrosine kinase, monoclonal antibodies, small molecule inhibitors, cancers, tumorigenesis, tumour resistance, dimerization, gene amplifications
Abstract: Members of epidermal growth factor receptor (EGFR) or ErbB receptor family play a critical role in a wide range of human cancers. In the past decade, there has been a remarkable progress in developing ErbB targeted therapeutics. However, a substantial portion of patients has non-responsive disease or subsequently shows evidence of tumour relapse following initial success with anti-ErbB agents. Improved insights into the biology of ErbB receptor family have led to more effective second- and third-generation anti-ErbB therapies. In this review, we have summarised salient features of the ErbB receptor physiology and highlighted key mechanisms involved in abnormal ErbB signalling in tumorigenesis. The rationale of anti-ErbB receptor therapies are outlined along with key mechanisms proposed for resistance to treatment as well as the current concept of combined anti-ErbB therapies. In conclusion, improved understanding of the molecular pathways that confer resistance to anti-ErbB therapeutics will be essential in minimising tumour resistance to ErbB targeted treatments.
Export Options
About this article
Cite this article as:
Patel Rachana and Y. Leung Hing, Targeting the EGFR-family for Therapy: Biological Challenges and Clinical Perspective, Current Pharmaceutical Design 2012; 18 (19) . https://dx.doi.org/10.2174/138161212800626148
DOI https://dx.doi.org/10.2174/138161212800626148 |
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
-
Genetics of Primary CoQ10 Deficiency
Current Genomics Development of Doxorubicin Quantification by Reductive Amination
Current Analytical Chemistry Editorial [ Hot Topic: Modifying Cardiovascular Risk Factors: Novel Cardiovascular Targets for Treatment by Noninvasive Imaging Techniques (Executive Editors: Aurelio Leone and Luigi Landini) ]
Current Pharmaceutical Design Interrelationship Between Kidney Function and Percutaneous Mitral Valve Interventions: A Comprehensive Review
Current Cardiology Reviews Perinatal Exposure to Bisphenol A and Developmental Programming of the Cardiovascular Changes in the Offspring
Current Medicinal Chemistry Pathophysiology of Post-Operative Low Cardiac Output Syndrome
Current Vascular Pharmacology Toll Like Receptors Signaling Pathways as a Target for Therapeutic Interventions
Current Signal Transduction Therapy Metabolic Features of Alcoholic Liver Disease
Reviews on Recent Clinical Trials Salvia miltiorrhiza: A Potential Red Light to the Development of Cardiovascular Diseases
Current Pharmaceutical Design Is a "Mitochondrial Psychiatry" in the Future? A Review
Current Psychiatry Reviews The Cardiovascular Nutrapharmacology of Resveratrol: Pharmacokinetics, Molecular Mechanisms and Therapeutic Potential
Current Medicinal Chemistry Calreticulin in the Heart: From Embryological Development to Cardiac Pathology.
Current Molecular Medicine From Mars to Venus: Gender Differences in the Management and Outcomes of Acute Coronary Syndromes
Current Pharmaceutical Design The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects
Mini-Reviews in Medicinal Chemistry The Evolving Roles of Nuclear Cardiology
Current Cardiology Reviews Eisenmenger Syndrome: Recent Advances in Pharmacotherapy
Cardiovascular & Hematological Agents in Medicinal Chemistry Common Genetic Conditions of Ischemic Stroke to Keep in Mind
Current Molecular Medicine Oxidative-Nitrosative Stress as a Contributing Factor to Cardiovascular Disease in Subjects with Diabetes
Current Vascular Pharmacology Stem Cell-Derived Microvesicles: A Cell Free Therapy Approach to the Regenerative Medicine
Current Biotechnology Immunomodulatory Gene Therapy in Lysosomal Storage Disorders
Current Gene Therapy