Abstract
Overexpression of the epidermal growth factor receptor tyrosine kinase (EGFR-TK) has been documented in numerous human cancers of epithelial origin, and was found to correlate with resistance to treatment and poor prognosis. Recognizing the central role that this receptor plays in cancer development and progression, various approaches have been developed to target it in order to more specifically eradicate cancer cells. These methods include, among others, low-molecular weight inhibitors of the TK domain that are commonly designed to treat those tumors that overexpress the EGFR. Nevertheless, no currently available assay provides non-invasive, longitudinal and sensitive quantitation of receptor levels in tumors so as to better identify candidate patients for EGFR-targeted therapies. Hence, attempts have been made to develop radiolabeled molecular imaging agents as potential bioprobes to quantitatively monitor treatment efficiency. Such EGFR-targeted bioprobes could not only improve patient selection and treatment monitoring, but also allow a direct delivery of radionuclides for radiotherapy. In this review, the role that EGFR plays in cancer development and therapy is briefly presented, followed by a short review of prominent milestones in the development of EGFR-TK inhibitors. These inhibitors constitute the fundamental core structure for the development of radiolabeled probes to visualize the EGFR in vivo. The considerations that need to be taken into account for the development of such probes will be presented, along with a critical examination on the progress that has been made thus far in the field.
Keywords: EGFR, [18F], [11C], PET, cancer, molecular imaging, nuclear medicine
Current Topics in Medicinal Chemistry
Title: Cancer Molecular Imaging: Radionuclide-Based Biomarkers of the Epidermal Growth Factor Receptor (EGFR)
Volume: 7 Issue: 18
Author(s): Eyal Mishani and Galith Abourbeh
Affiliation:
Keywords: EGFR, [18F], [11C], PET, cancer, molecular imaging, nuclear medicine
Abstract: Overexpression of the epidermal growth factor receptor tyrosine kinase (EGFR-TK) has been documented in numerous human cancers of epithelial origin, and was found to correlate with resistance to treatment and poor prognosis. Recognizing the central role that this receptor plays in cancer development and progression, various approaches have been developed to target it in order to more specifically eradicate cancer cells. These methods include, among others, low-molecular weight inhibitors of the TK domain that are commonly designed to treat those tumors that overexpress the EGFR. Nevertheless, no currently available assay provides non-invasive, longitudinal and sensitive quantitation of receptor levels in tumors so as to better identify candidate patients for EGFR-targeted therapies. Hence, attempts have been made to develop radiolabeled molecular imaging agents as potential bioprobes to quantitatively monitor treatment efficiency. Such EGFR-targeted bioprobes could not only improve patient selection and treatment monitoring, but also allow a direct delivery of radionuclides for radiotherapy. In this review, the role that EGFR plays in cancer development and therapy is briefly presented, followed by a short review of prominent milestones in the development of EGFR-TK inhibitors. These inhibitors constitute the fundamental core structure for the development of radiolabeled probes to visualize the EGFR in vivo. The considerations that need to be taken into account for the development of such probes will be presented, along with a critical examination on the progress that has been made thus far in the field.
Export Options
About this article
Cite this article as:
Mishani Eyal and Abourbeh Galith, Cancer Molecular Imaging: Radionuclide-Based Biomarkers of the Epidermal Growth Factor Receptor (EGFR), Current Topics in Medicinal Chemistry 2007; 7 (18) . https://dx.doi.org/10.2174/156802607782507457
DOI https://dx.doi.org/10.2174/156802607782507457 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Epithelial-Mesenchymal Transition: Implications in Cancer Progression and Metastasis
Current Pharmaceutical Biotechnology Saponins in Tumor Therapy
Mini-Reviews in Medicinal Chemistry Multiple VEGF Family Members are Simultaneously Expressed in Ovarian Cancer: a Proposed Model for Bevacizumab Resistance
Current Pharmaceutical Design Structure Based Lead Optimization Approach in Discovery of Selective DPP4 Inhibitors
Mini-Reviews in Medicinal Chemistry Structural and Mechanistic Bases of the Anticancer Activity of Natural Aporphinoid Alkaloids
Current Topics in Medicinal Chemistry Inhibition of Autophagy Strengthens Celastrol-Induced Apoptosis in Human Pancreatic Cancer In Vitro and In Vivo Models
Current Molecular Medicine Natural Products Derived from Traditional Chinese Medicine as Novel Inhibitors of the Epidermal Growth Factor Receptor
Combinatorial Chemistry & High Throughput Screening How is Gene Transfection Able to Improve Current Chemotherapy? The Role of Combined Therapy in Cancer Treatment
Current Medicinal Chemistry Herpes Simplex Encephalitis: From Virus to Therapy
Infectious Disorders - Drug Targets A Role of Immunotherapy in Metastatic Malignant Melanoma
Central Nervous System Agents in Medicinal Chemistry Cancer Stem Cells – Are Surface Markers Alone Sufficient?
Current Stem Cell Research & Therapy Effects of Galbanic Acid on Proliferation, Migration, and Apoptosis of Glioblastoma Cells Through the PI3K/Akt/MTOR Signaling Pathway
Current Molecular Pharmacology Herpes Simplex Viruses in Antiviral Drug Discovery
Current Pharmaceutical Design Mapping the High Throughput SEREX Technology Screening for Novel Tumor Antigens
Combinatorial Chemistry & High Throughput Screening MiRNA-29: A microRNA Family with Tumor-Suppressing and Immune-Modulating Properties
Current Molecular Medicine Nanostructures for Drug Delivery to the Brain
Current Medicinal Chemistry Preventive and Protective Roles of Dietary Nrf2 Activators Against Central Nervous System Diseases
CNS & Neurological Disorders - Drug Targets Adenovirus-based Immunotherapy for Prostate Cancer
Current Cancer Therapy Reviews Suicide Gene Therapy Mediated by the Herpes Simplex Virus Thymidine Kinase Gene / Ganciclovir System: Fifteen Years of Application
Current Gene Therapy Cytotoxic and Anticancer Activities of Isatin and Its Derivatives: A Comprehensive Review from 2000-2008
Anti-Cancer Agents in Medicinal Chemistry