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.
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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 |
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