In vivo positron emission tomography (PET) imaging with an alphavbeta6 specific peptide radiolabeled using 18F-"click" chemistry: evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18F]fluoropropionyl-peptides.
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [(18)F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase (18)F-"click" radiolabeling and solid-phase radiolabeling using 4-[(18)F]fluorobenzoic and 2-[(18)F]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.
Hausner
Sven H
SH
Department of Biomedical Engineering, University of California Davis, Davis, California 95616, USA.
Marik
Jan
J
Gagnon
M Karen J
MK
Sutcliffe
Julie L
JL
D000818:Animals; D000951:Antigens, Neoplasm / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D001565:Benzoates / Q000737:chemistry*; D045744:Cell Line, Tumor; D005462:Fluorine Radioisotopes; D006801:Humans; D016023:Integrins / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis*; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography / Q000379:methods*; D011422:Propionates / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics; D012680:Sensitivity and Specificity; D013237:Stereoisomerism; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
D000951:Antigens, Neoplasm; D001565:Benzoates; D005462:Fluorine Radioisotopes; D016023:Integrins; D010455:Peptides; D011422:Propionates; D019275:Radiopharmaceuticals; C073878:integrin alphavbeta6; C022893:4-fluorobenzoic acid
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