Abstract
For radiotherapy, biomolecules such as intact antibodies, antibody fragments, peptides, DNAs and other oligomers have all been labeled with radiorhenium (186Re and 188Re). Three different approaches have been employed that may be referred to as direct, indirect and integral labeling. Direct labeling applies to proteins and involves the initial reduction of endogenous disulfide bridges to provide chelation sites. Indirect labeling can apply to most biomolecules and involves the initial attachment of an exogenous chelator. Finally, integral labeling is a special case applying only to small molecules in which the metallic radionuclide serves to link two parts of a biomolecule together in forming the labeled complex. While the number of varieties for the direct and integral radiolabeling approaches is rather limited, a fairly large and diverse number of chelators have been reported in the case of indirect labeling. Our objective herein is to provide an overview of the various chelators that have been used in the indirect labeling of biomolecules with radiorhenium, including details on the labeling procedures, the stability of the radiolabel and, where possible, the influence of the label on biological properties.
Keywords: Radiolabeling, rhenium-188, rhenium-186, bifunctional chelator, radioimmunotherapy, biomolecule, coordination chemistry, radiopharmaceuticals
Anti-Cancer Agents in Medicinal Chemistry
Title: Labeling Biomolecules with Radiorhenium - A Review of the Bifunctional Chelators
Volume: 7 Issue: 3
Author(s): Guozheng Liu and Donald J. Hnatowich
Affiliation:
Keywords: Radiolabeling, rhenium-188, rhenium-186, bifunctional chelator, radioimmunotherapy, biomolecule, coordination chemistry, radiopharmaceuticals
Abstract: For radiotherapy, biomolecules such as intact antibodies, antibody fragments, peptides, DNAs and other oligomers have all been labeled with radiorhenium (186Re and 188Re). Three different approaches have been employed that may be referred to as direct, indirect and integral labeling. Direct labeling applies to proteins and involves the initial reduction of endogenous disulfide bridges to provide chelation sites. Indirect labeling can apply to most biomolecules and involves the initial attachment of an exogenous chelator. Finally, integral labeling is a special case applying only to small molecules in which the metallic radionuclide serves to link two parts of a biomolecule together in forming the labeled complex. While the number of varieties for the direct and integral radiolabeling approaches is rather limited, a fairly large and diverse number of chelators have been reported in the case of indirect labeling. Our objective herein is to provide an overview of the various chelators that have been used in the indirect labeling of biomolecules with radiorhenium, including details on the labeling procedures, the stability of the radiolabel and, where possible, the influence of the label on biological properties.
Export Options
About this article
Cite this article as:
Liu Guozheng and Hnatowich J. Donald, Labeling Biomolecules with Radiorhenium - A Review of the Bifunctional Chelators, Anti-Cancer Agents in Medicinal Chemistry 2007; 7 (3) . https://dx.doi.org/10.2174/187152007780618144
DOI https://dx.doi.org/10.2174/187152007780618144 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Patent Selections
Recent Patents on Biomedical Engineering (Discontinued) Drug Evolution Concept in Drug Design: 2. Chimera Method
Medicinal Chemistry Synthesis and Biological Evaluation of Oxopyrido[2,3-d] Pyrimidine-7- ones Derivatives as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors
Letters in Drug Design & Discovery Synthesis of 4-Arylaminoquinazolines from 2-amino-N'-Arylbenzamidines and Orthoesters via the Dimroth Rearrangement of Intermediate Quinazolin-4(3H)- Imines
Current Organic Chemistry Patent Selections
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Use of Methylphenidate for Physical and Psychological Symptoms in Cancer Patients: A Review
Current Drug Targets The Apoptosis Mechanism of Epirubicin Combined with BCG on Human Bladder Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Nutritional Interventions for Elderly and Considerations for the Development of Geriatric Foods
Current Aging Science The Role of a Human Hematopoietic Mesenchymal Progenitor in Wound Healing and Fibrotic Diseases and Implications for Therapy
Current Stem Cell Research & Therapy Exploring Protein-Protein Interactions with Synthetic Peptide Arrays
Mini-Reviews in Organic Chemistry Highly Disordered Proteins in Prostate Cancer
Current Protein & Peptide Science Vitamin D, Pit-1, GH, and PRL: Possible Roles in Breast Cancer Development
Current Medicinal Chemistry Genetic Modifications of Icosahedral Plant Virus-based Nanoparticles for Vaccine and Immunotherapy Applications
Current Protein & Peptide Science Recent Patents Relating to siRNAs and Therapeutic Strategies for Genetic Diseases
Recent Patents on DNA & Gene Sequences Pharmacological Interventions to Attenuate Alzheimer’s Disease Progression: The Story So Far
Current Alzheimer Research Tumor Initiation in Human Malignant Melanoma and Potential Cancer Therapies
Anti-Cancer Agents in Medicinal Chemistry CYP4Z1 – A Human Cytochrome P450 Enzyme that Might Hold the Key to Curing Breast Cancer
Current Pharmaceutical Design The Place of the Bioisosteric Sila-Substitution in Drug Design
Drug Design Reviews - Online (Discontinued) Similar and Shared Nongenomic Mechanisms of Action of Estrogen and Thyroid Hormone
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Selective Inhibition of Esophageal Cancer Stem-like Cells with Salinomycin
Anti-Cancer Agents in Medicinal Chemistry