Labeling Biomolecules with Radiorhenium - A Review of the Bifunctional Chelators

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Labeling Biomolecules with Radiorhenium - A Review of the Bifunctional Chelators

Anti-Cancer Agents in Medicinal Chemistry, 7(3): 367-377.

Author(s): Guozheng Liu and Donald J Hnatowich.

Affiliation: Division of Nuclear Medicine,University of Massachusetts Medical School, 55 Lake Avenue North,Worcester, MA 01655, USA.


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.


Radiolabeling, rhenium-188, rhenium-186, bifunctional chelator, radioimmunotherapy, biomolecule, coordination chemistry, radiopharmaceuticals.

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Article Details

Volume: 7
Issue Number: 3
First Page: 367
Last Page: 377
Page Count: 11
DOI: 10.2174/187152007780618144
Price: $58

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