Abstract
Receptor tyrosine kinases (RTKs) are a superfamily of transmembrane proteins that mediate intracellular signaling by phosphorylating substrate proteins involved in cell proliferation, survival, differentiation or migration. The Human Epidermal growth factor Receptor (HER) family belongs to the RTKs superfamily, and comprises four members: EGFR (epidermal growth factor receptor), HER2, HER3 and HER4. Physiologically, these receptors are activated by the ligands of the EGF family. In solid tumors other mechanisms of activation, such as overexpression or molecular alterations have been reported, and have been linked to tumour initiation/progression. Because of that, several strategies have been developed to target HER receptors and include i) antibody-based therapies using monoclonal antibodies against the extracellular domain of these receptors, and ii) small molecule tyrosine kinase inhibitors (TKIs) against the intracellular kinase domain. In this review we will provide basic information about biological aspects of HER receptors and their ligands as well as the therapeutic strategies to target them. We also summarize general mechanisms of resistance generated in patients to such anti-HER therapies.
Keywords: Cancer, HER receptors, HER ligands, anti-HER therapies, therapy-resistance.
Current Pharmaceutical Design
Title:Targeting the EGF/HER Ligand-Receptor System in Cancer
Volume: 22 Issue: 39
Author(s): Azucena Esparís-Ogando, Juan Carlos Montero, Joaquín Arribas, Alberto Ocaña and Atanasio Pandiella
Affiliation:
Keywords: Cancer, HER receptors, HER ligands, anti-HER therapies, therapy-resistance.
Abstract: Receptor tyrosine kinases (RTKs) are a superfamily of transmembrane proteins that mediate intracellular signaling by phosphorylating substrate proteins involved in cell proliferation, survival, differentiation or migration. The Human Epidermal growth factor Receptor (HER) family belongs to the RTKs superfamily, and comprises four members: EGFR (epidermal growth factor receptor), HER2, HER3 and HER4. Physiologically, these receptors are activated by the ligands of the EGF family. In solid tumors other mechanisms of activation, such as overexpression or molecular alterations have been reported, and have been linked to tumour initiation/progression. Because of that, several strategies have been developed to target HER receptors and include i) antibody-based therapies using monoclonal antibodies against the extracellular domain of these receptors, and ii) small molecule tyrosine kinase inhibitors (TKIs) against the intracellular kinase domain. In this review we will provide basic information about biological aspects of HER receptors and their ligands as well as the therapeutic strategies to target them. We also summarize general mechanisms of resistance generated in patients to such anti-HER therapies.
Export Options
About this article
Cite this article as:
Esparís-Ogando Azucena, Montero Carlos Juan, Arribas Joaquín, Ocaña Alberto and Pandiella Atanasio, Targeting the EGF/HER Ligand-Receptor System in Cancer, Current Pharmaceutical Design 2016; 22 (39) . https://dx.doi.org/10.2174/1381612822666160715132233
DOI https://dx.doi.org/10.2174/1381612822666160715132233 |
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
?Revolutionizing Cancer Treatment: Nano-Therapeutics Targeting Tumor Microenvironment?
This thematic issue explores the forefront of cancer treatment, centering on the groundbreaking potential of nano-therapeutics meticulously designed to target the tumor microenvironment. At its core, the issue aims to unravel the latest advancements in nanotechnology, showcasing innovative materials, formulations, and delivery systems that hold promise for redefining cancer therapeutics. ...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
- 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
-
Improving Brain Drug Targeting Through Exploitation of The Nose-to- Brain Route: A Physiological and Pharmacokinetic Perspective
Current Drug Delivery Antidepressants: Update on Benefits and Risks
Current Psychopharmacology Signal Transduction and Heavy Ion Radiation Therapy: Biological Mechanisms, Biological Quality Assurance, and New Multimodality Approach
Current Signal Transduction Therapy Developments of Polo-like Kinase 1 (Plk1) Inhibitors as Anti-Cancer Agents
Mini-Reviews in Medicinal Chemistry The Role of a Disturbed Arginine/NO Metabolism in the Onset of Cancer Cachexia: A Working Hypothesis
Current Medicinal Chemistry Axitinib in the Treatment of Head and Neck Malignancies
Current Clinical Pharmacology Editorial [Hot topic: Cell Adhesion Molecules: Structure, Function, Drug Design, and Biomaterials (Executive Editor: Seetharama D. Satyanarayanajois)]
Current Pharmaceutical Design Metallic Colloid Nanotechnology, Applications in Diagnosis and Therapeutics
Current Pharmaceutical Design Nanotechnology and Radiopharmaceuticals: Diagnostic and Therapeutic Approaches
Current Drug Delivery Inhibition of Cyclin-Dependent Kinases - A Review of the Recent Patent Literature
Recent Patents on Anti-Cancer Drug Discovery Salinomycin Suppresses Tumorigenicity of Liver Cancer Stem Cells and Wnt/Beta-catenin Signaling
Current Stem Cell Research & Therapy Can Breast Cancer Stem Cells Evade the Immune System?
Current Medicinal Chemistry Unraveling Potential Candidate Targets Associated with Expression of p16<sup>INK4a</sup> or p16 Truncated Fragment by Comparative Proteomics Analysis
Current Proteomics How Recent Patents Have Changed our Clinical Approach in Cardio-Thoracic Surgery
Recent Patents on Regenerative Medicine Lipoxygenase Inhibitors for Cancer Prevention: Promises and Risks
Current Pharmaceutical Design MicroRNAs Involved in Oxidative Stress Processes Regulating Physiological and Pathological Responses
MicroRNA p53: Fighting Cancer
Current Cancer Drug Targets Incidentally Detected Increased FDG Uptake in Bowel and its Correlation with Hystopathological Data: Our Experience in a Case Series Study
Current Radiopharmaceuticals Peptides and Small Molecules Targeting the Plasminogen Activation System: Towards Prophylactic Anti-Metastasis Drugs for Breast Cancer
Recent Patents on Anti-Cancer Drug Discovery Epigenetic Regulation of Cytochrome P450 Enzymes and Clinical Implication
Current Drug Metabolism