A practical guide to the construction of radiometallated bioconjugates for positron emission tomography Journal Article


Authors: Zeglis, B. M.; Lewis, J. S.
Article Title: A practical guide to the construction of radiometallated bioconjugates for positron emission tomography
Abstract: Positron emission tomography (PET) has become a vital imaging modality in the diagnosis and treatment of disease, most notably cancer. A wide array of small molecule PET radiotracers have been developed that employ the short half-life radionuclides 11C, 13N, 15O, and 18F. However, PET radiopharmaceuticals based on biomolecular targeting vectors have been the subject of dramatically increased research in both the laboratory and the clinic. Typically based on antibodies, oligopeptides, or oligonucleotides, these tracers have longer biological half-lives than their small molecule counterparts and thus require labeling with radionuclides with longer, complementary radioactive half-lives, such as the metallic isotopes 64Cu, 68Ga, 86Y, and 89Zr. Each bioconjugate radiopharmaceutical has four component parts: biomolecular vector, radiometal, chelator, and covalent link between chelator and biomolecule. With the exception of the radiometal, a tremendous variety of choices exists for each of these pieces, and a plethora of different chelation, conjugation, and radiometallation strategies have been utilized to create agents ranging from 68Ga-labeled pentapeptides to 89Zr-labeled monoclonal antibodies. Herein, the authors present a practical guide to the construction of radiometal-based PET bioconjugates, in which the design choices and synthetic details of a wide range of biomolecular tracers from the literature are collected in a single reference. In assembling this information, the authors hope both to illuminate the diverse methods employed in the synthesis of these agents and also to create a useful reference for molecular imaging researchers both experienced and new to the field. © 2011 The Royal Society of Chemistry.
Keywords: positron emission tomography; molecular imaging; monoclonal antibodies; diagnosis; radioactivity; radioisotopes; oligopeptides; biomolecules; diseases; zirconium; chelation; positrons; oligonucleotides; small molecules; gallium; bio-molecular; bioconjugates; component part; covalent link; diverse methods; half lives; imaging modality; pentapeptides; practical guide
Journal Title: Dalton Transactions
Volume: 40
Issue: 23
ISSN: 1477-9226
Publisher: Royal Society of Chemistry  
Date Published: 2011-06-21
Start Page: 6168
End Page: 6195
Language: English
DOI: 10.1039/c0dt01595d
PROVIDER: scopus
PUBMED: 21442098
PMCID: PMC3773488
DOI/URL:
Notes: --- - "Export Date: 17 August 2011" - "Source: Scopus"
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MSK Authors
  1. Brian Zeglis
    63 Zeglis
  2. Jason S Lewis
    245 Lewis