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Am J Nucl Med Mol Imaging 2013;3(1):57-70

Original Article
18F-click labeling of a bombesin antagonist with an
alkyne-18F-ArBF3-: in vivo PET imaging of tumors
expressing the GRP-receptor

Ying Li, Zhibo Liu, Curtis W Harwig, Maral Pourghiasian, Joseph Lau, Kuo-Shyan Lin, Paul Schaffer,
Francois Benard, David M Perrin

Chemistry Department, 2036 Main Mall, University of British Columbia, Vancouver, B.C., Canada V6T-1Z1;
BC Cancer Agency - Vancouver Centre, Centre for Functional Imaging, 600 West 10th Avenue, Vancouver, B.C.
Canada V5Z-4E6; 3Triumf, 4004 Wesbrook Mall, Vancouver, B.C. Canada V6T-2A3

Received November 19, 2012; Accepted December 10, 2012; Epub January 5, 2013; Published January 15, 2013

Abstract: A clickable alkyne-modified arylborimidine is rapidly converted in 15 minutes to a highly polar 18F-aryltrifluoroborate
anion (18F-ArBF3-) at high specific activity. Following labeling, the alkyne-18F-ArBF3- was conjugated to the peptide bombesin (BBN)
within 25 minutes in a second step without need for prior work-up making this one-pot-twostep method easy, user-friendly, and
generally applicable. Bombesin was chosen to provide functional PET images of prostate cancer xenografts in mice of which there
are few. Whereas BBN is labeled to provide some of the first in vivo tumor images based on this technique, click-labeling is
recognized for its generality and broad substrate scope. Hence these results are likely to be useful for click labeling most peptides
and other biomolecules. (ajnmmi1210003).

Keywords: 18F-labeling, PET imaging, click chemistry, bombesin imaging

Address all correspondence to:
Dr. David M Perrin,
Chemistry Department, UBC, 2036 Main Mall,
Vancouver, B.C., V6T-1Z1, Canada. Phone: 604
8220567; E-mail: dperrin@chem.ubc.ca