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Positron Emission Tomography Tracer Design of Targeted Synthetic Peptides via F-Sydnone Alkyne Cycloaddition. | LitMetric

Positron Emission Tomography Tracer Design of Targeted Synthetic Peptides via F-Sydnone Alkyne Cycloaddition.

Bioconjug Chem

Department of Molecular and Medical Pharmacology and Crump Institute for Molecular Imaging, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, California 90095, United States.

Published: September 2021

AI Article Synopsis

  • Small peptides that bind specifically to CD8+ T cells show promise for diagnosing immune responses through molecular imaging.
  • Researchers developed F-labeled peptides targeting human CD8α using a fast and efficient chemical process, achieving high radiochemical yield.
  • The inclusion of a hydrophilic linker enhances the tracer's pharmacokinetics and improves image quality in PET imaging studies.

Article Abstract

Chemically synthesized, small peptides that bind with high affinity and specificity to CD8-expressing (CD8+) tumor-infiltrating T cells, yet retain the desirable characteristics of small molecules, hold valuable potential for diagnostic molecular imaging of immune response. Here, we report the development of F-labeled peptides targeting human CD8α with nanomolar affinity via the strain-promoted sydnone-alkyne cycloaddition with 4-[F]fluorophenyl sydnone. The F-sydnone is produced in one step, in high radiochemical yield, and the peptide labeling proceeds rapidly. A hydrophilic chemical linker results in a tracer with favorable pharmacokinetic properties and improved image contrast, as demonstrated by PET imaging studies.

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Source
http://dx.doi.org/10.1021/acs.bioconjchem.1c00379DOI Listing

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