Title

Labeling biomolecules with radiorhenium: a review of the bifunctional chelators

UMMS Affiliation

Department of Radiology, Division of Nuclear Medicine

Date

5-17-2007

Document Type

Article

Subjects

Animals; Chelating Agents; Humans; Hydrazines; Hydroxamic Acids; Nicotinic Acids; Phosphines; Radioisotopes; Radiopharmaceuticals; Rhenium; Succinates

Disciplines

Life Sciences | Medicine and Health Sciences

Abstract

For radiotherapy, biomolecules such as intact antibodies, antibody fragments, peptides, DNAs and other oligomers have all been labeled with radiorhenium ((186)Re and (188)Re). 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.

Rights and Permissions

Citation: Anticancer Agents Med Chem. 2007 May;7(3):367-77.

Related Resources

Link to Article in PubMed

Journal Title

Anti-cancer agents in medicinal chemistry

PubMed ID

17504162