Abstract
Radiopharmaceuticals constitute diagnostic and therapeutic tools for both clinical and preclinical applications. They are a blend of a tracer moiety that mediates a site specific accumulation and an effector: a radioisotope whose decay enables either molecular imaging or exhibits cytotoxic effects. Radioactive halogens and lanthanides are the most commonly used isotopes for radiopharmaceuticals. Due to their ready availability and the facile labeling metallic radionuclides offer ideal characteristics for applications in nuclear medicine. A stable link between the radionuclide and the carrier molecule is the primary prerequisite for in vivo applications. The radionuclide is selected according to its physical and chemical properties i.e. half-life, the type of decay, the energy emitted and its availability. Bifunctional chelating agents are used to stably link the radiometal to the carrier moiety of the radiopharmaceutical. The design of the bifunctional chelator has to consider the impact of the radiometal chelate on the biological properties of the target-specific pharmaceutical. Here, with an emphasis on oncology, we review applications of radiopharmaceuticals that contain bifunctional chelators, while highlighting successes and identifying the key challenges that need to be addressed for the successful translation of target binding molecules into tracers for molecular imaging and endoradiotherapy.
Keywords: Bifunctional chelating agent (BFCA), DOTA, nuclear medicine, radiochemistry, radiometals, radiopharmaceuticals, targeting, theranostics
Current Medicinal Chemistry
Title:Bifunctional Chelators in the Design and Application of Radiopharmaceuticals for Oncological Diseases
Volume: 19 Issue: 17
Author(s): D. Sarko, M. Eisenhut, U. Haberkorn and W. Mier
Affiliation:
Keywords: Bifunctional chelating agent (BFCA), DOTA, nuclear medicine, radiochemistry, radiometals, radiopharmaceuticals, targeting, theranostics
Abstract: Radiopharmaceuticals constitute diagnostic and therapeutic tools for both clinical and preclinical applications. They are a blend of a tracer moiety that mediates a site specific accumulation and an effector: a radioisotope whose decay enables either molecular imaging or exhibits cytotoxic effects. Radioactive halogens and lanthanides are the most commonly used isotopes for radiopharmaceuticals. Due to their ready availability and the facile labeling metallic radionuclides offer ideal characteristics for applications in nuclear medicine. A stable link between the radionuclide and the carrier molecule is the primary prerequisite for in vivo applications. The radionuclide is selected according to its physical and chemical properties i.e. half-life, the type of decay, the energy emitted and its availability. Bifunctional chelating agents are used to stably link the radiometal to the carrier moiety of the radiopharmaceutical. The design of the bifunctional chelator has to consider the impact of the radiometal chelate on the biological properties of the target-specific pharmaceutical. Here, with an emphasis on oncology, we review applications of radiopharmaceuticals that contain bifunctional chelators, while highlighting successes and identifying the key challenges that need to be addressed for the successful translation of target binding molecules into tracers for molecular imaging and endoradiotherapy.
Export Options
About this article
Cite this article as:
Sarko D., Eisenhut M., Haberkorn U. and Mier W., Bifunctional Chelators in the Design and Application of Radiopharmaceuticals for Oncological Diseases, Current Medicinal Chemistry 2012; 19 (17) . https://dx.doi.org/10.2174/092986712800609751
DOI https://dx.doi.org/10.2174/092986712800609751 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
LPS In Patients With Left Ventricular Dysfunction Of Ischemic And Non-Ischemic Origin
Cardiovascular & Hematological Disorders-Drug Targets A Critical Approach of Guideline Therapeutic Recommendations for NAFLD
Current Vascular Pharmacology EPC Dysfunction and Immune Networks: Translating Opportunities for Clinical Setting in Personalized Medicine
Current Medicinal Chemistry Editorial (Thematic Issue: The Changing Face of Metabolic Syndrome and its Components in the Light of Current Knowledge)
Current Vascular Pharmacology Regulation of the Protein C Anticoagulant and Antiinflammatory Pathways
Current Medicinal Chemistry Fibrillar, Fibril-associated and Basement Membrane Collagens of the Arterial Wall: Architecture, Elasticity and Remodeling Under Stress
Current Pharmaceutical Design Modelling Anxiety in Humans for Drug Development
Current Neuropharmacology Carotid Artery Stenting for the Prevention of Thromboembolic Stroke
Vascular Disease Prevention (Discontinued) Functional Food with Some Health Benefits, So Called Superfood: A Review
Current Nutrition & Food Science Platelet Microparticles Induce Angiogenesis and Neurogenesis after Cerebral Ischemia
Current Neurovascular Research Chemical Diversity of Grape Products, a Complex Blend of Bioactive Secondary Metabolites
The Natural Products Journal Neuronal Generation from Somatic Stem Cells: Current Knowledge and Perspectives on the Treatment of Acquired and Degenerative Central Nervous System Disorders
Current Gene Therapy Blood-Brain Barrier Transport of Drugs for the Treatment of Brain Diseases
CNS & Neurological Disorders - Drug Targets Will Medicinal Cannabinoids Prove to be Useful Clinically?
Current Drug Therapy Late versus Early Onset Depression in Elderly Patients: Vascular Risk and Cognitive Impairment
Current Aging Science The Role of Mitochondria in Piperine Mediated Cardioprotection in Isoproterenol Induced Myocardial Ischemia
Current Pharmaceutical Design Current Issues in the Utility of Blood Oxygen Level Dependent MRI for the Assessment of Modulations in Tumor Oxygenation
Current Medical Imaging Cancer Treatment-Induced Cardiotoxicity: a Cardiac Stem Cell Disease?
Cardiovascular & Hematological Agents in Medicinal Chemistry Weight Loss and the Risk of Dementia: A Meta-analysis of Cohort Studies
Current Alzheimer Research Neuron-Specific Mitochondrial DNA Deletion Levels in Sporadic Alzheimer´s Disease
Current Alzheimer Research