Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK

Ryan A. Davis, Kevin Lau, Sven H. Hausner, Julie Sutcliffe

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Solid-phase peptide synthesis, head-to-tail cyclization, and subsequent radiolabeling provided a reproducible, simple, rapid synthetic method to generate the cyclic peptide radiotracer cRGDyK([18F]FBA). Herein is reported the first on-resin cyclization and 18F-radiolabeling of a cyclic peptide (cRGDyK) in an overall peptide synthesis yield of 88% (cRGDyK(NH2)) and subsequent radiolabeling yield of 14 ± 2% (decay corrected, n = 4). This approach is generally applicable to the development of an automated process for the synthesis of cyclic radiolabeled peptides for positron emission tomography (PET).

Original languageEnglish (US)
Pages (from-to)8659-8663
Number of pages5
JournalOrganic and Biomolecular Chemistry
Volume14
Issue number37
DOIs
StatePublished - 2016

Fingerprint

Cyclic Peptides
Solid-Phase Synthesis Techniques
Fluorine
peptides
fluorine
solid phases
Cyclization
synthesis
Peptides
Positron emission tomography
Positron-Emission Tomography
Resins
resins
positrons
tomography
decay

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK. / Davis, Ryan A.; Lau, Kevin; Hausner, Sven H.; Sutcliffe, Julie.

In: Organic and Biomolecular Chemistry, Vol. 14, No. 37, 2016, p. 8659-8663.

Research output: Contribution to journalArticle

Davis, Ryan A. ; Lau, Kevin ; Hausner, Sven H. ; Sutcliffe, Julie. / Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK. In: Organic and Biomolecular Chemistry. 2016 ; Vol. 14, No. 37. pp. 8659-8663.
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