title: Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK.
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 and18F-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).
authors.affiliation: Radiochemistry Research and Training Facility, USA. jlsutcliffe@ucdavis.edu and Department of Biomedical Engineering, USA and Department of Internal Medicine, Division of Hematology and Oncology, USA.
authors.forename: Ryan A
authors.initials: RA
authors.lastname: Davis
authors.affiliation: Radiochemistry Research and Training Facility, USA. jlsutcliffe@ucdavis.edu and Department of Biomedical Engineering, USA.
authors.forename: Kevin
authors.initials: K
authors.lastname: Lau
authors.affiliation: Radiochemistry Research and Training Facility, USA. jlsutcliffe@ucdavis.edu and Department of Biomedical Engineering, USA and Department of Internal Medicine, Division of Hematology and Oncology, USA.
authors.forename: Sven H
authors.initials: SH
authors.lastname: Hausner
authors.affiliation: Radiochemistry Research and Training Facility, USA. jlsutcliffe@ucdavis.edu and Department of Biomedical Engineering, USA and Department of Internal Medicine, Division of Hematology and Oncology, USA and Center for Molecular and Genomic Imaging, University of California, Davis, 2921 Stockton Blvd., Sacramento, CA 95817, USA.
authors.forename: Julie L
authors.initials: JL
authors.lastname: Sutcliffe
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry*; D049268:Positron-Emission Tomography / Q000379:methods; D060327:Solid-Phase Synthesis Techniques / Q000379:methods
chemical_list: D005462:Fluorine Radioisotopes; D010456:Peptides, Cyclic; C550210:cyclo(Arg-Gly-Asp-Tyr-Lys); C000615276:Fluorine-18