Prosthetic groups for radioiodination and astatination of peptides and proteins: A comparative study of five potential bioorthogonal labeling strategies

[Display omitted] 125I- and 211At-labeled azide and tetrazine based prosthetic groups for bioorthogonal conjugation were designed and tested in a comparative study of five bioorthogonal systems. All five bioconjugation reactions conducted on a model clickable peptide led to quantitative yields withi...

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Published inBioorganic & medicinal chemistry Vol. 27; no. 1; pp. 167 - 174
Main Authors Navarro, Laurent, Berdal, Marion, Chérel, Michel, Pecorari, Frédéric, Gestin, Jean-François, Guérard, François
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.01.2019
Elsevier
Subjects
Biochemistry & Molecular Biology
Cancer
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
CHEMISTRY
STABILITY
LINKER
EFFICIENT METHOD
ASTATINE-211
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Summary:[Display omitted] 125I- and 211At-labeled azide and tetrazine based prosthetic groups for bioorthogonal conjugation were designed and tested in a comparative study of five bioorthogonal systems. All five bioconjugation reactions conducted on a model clickable peptide led to quantitative yields within less than a minute to several hours depending on the system used. Transferability to the labeling of an IgG was demonstrated with one of the bioorthogonal system. This study provides several new alternatives to the conventional and suboptimal approach currently in use for radioiodination and astatination of biomolecules and should accelerate the development of new probes with these radionuclides for applications in nuclear imaging and targeted alpha-therapy.
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ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2018.11.034