(18)F-click labeling of a bombesin antagonist with an alkyne-(18)F-ArBF(3) (-): in vivo PET imaging of tumors expressing the GRP-receptor.
A clickable alkyne-modified arylborimidine is rapidly converted in 15 minutes to a highly polar (18)F-aryltrifluoroborate anion ((18)F-ArBF(3) (-)) at high specific activity. Following labeling, the alkyne-(18)F-ArBF(3) (-) was conjugated to the peptide bombesin (BBN) within 25 minutes in a second step without need for prior work-up making this one-pot-two-step 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.
Chemistry Department, 2036 Main Mall, University of British Columbia Vancouver, B.C., Canada V6T-1Z1.
Ying
Y
Li
Zhibo
Z
Liu
Curtis W
CW
Harwig
Maral
M
Pourghiasian
Joseph
J
Lau
Kuo-Shyan
KS
Lin
Paul
P
Schaffer
Francois
F
Benard
David M
DM
Perrin
18F-labeling; PET imaging; bombesin imaging; click chemistry