In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry: Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F] fluoropropionyl-peptides

Sven H. Hausner, Jan Marik, M. Karen J Gagnon, Julie Sutcliffe

Research output: Contribution to journalArticle

77 Citations (Scopus)

Abstract

Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F- "click" radio-labeling and solid-phase radiolabeling using 4-[ 18F]fiuorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.

Original languageEnglish (US)
Pages (from-to)5901-5904
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number19
DOIs
StatePublished - Oct 9 2008

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Click Chemistry
Positron-Emission Tomography
Peptides
Fluorine
Cell Surface Receptors
Radio
Pharmacokinetics
2-18F-fluoropropionic acid

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

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AU - Sutcliffe, Julie

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AB - Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase 18F- "click" radio-labeling and solid-phase radiolabeling using 4-[ 18F]fiuorobenzoic and 2-[18F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.

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