@article {pmid25757604,
	title = {{(18){F}-{A}m{B}{F}3-{M}{J}9: a novel radiofluorinated bombesin derivative for prostate cancer imaging}},
	journal = {Bioorg. Med. Chem.},
	volume = {23},
	number = {7},
	year = {2015},
	month = {Apr},
	pages = {1500{\textendash}1506},
	abstract = {A novel radiofluorinated derivative of bombesin, (18)F-AmBF3-MJ9, was synthesized and evaluated for its potential to image prostate cancer by targeting the gastrin releasing peptide receptor (GRPR). AmBF3-MJ9 was prepared from an ammoniomethyl-trifluoroborate (AmBF3) conjugated alkyne 2 and azidoacetyl-MJ9 via a copper-catalyzed click reaction, and had good binding affinity for GRPR (Ki=0.5{\^A}{\textpm}0.1nM). The (18)F-labeling was performed via a facile one-step (18)F-(19)F isotope exchange reaction, and (18)F-AmBF3-MJ9 was obtained in 23{\^A}{\textpm}5\% (n=3) radiochemical yield in 25min with >99\% radiochemical purity and 100{\^A}{\textpm}32GBq/{\^I}{\textonequarter}mol specific activity. (18)F-AmBF3-MJ9 was stable in mouse plasma, and was partially (22-30\%) internalized after binding to GRPR. Positron emission tomography (PET) imaging and biodistribution studies in mice showed fast renal excretion and good uptake of (18)F-AmBF3-MJ9 by GRPR-expressing pancreas and PC-3 prostate cancer xenografts. Tumor uptake was 1.37{\^A}{\textpm}0.25\%ID/g at 1h, and 2.20{\^A}{\textpm}0.13\%ID/g at 2h post-injection (p.i.) with low background uptake and excellent tumor visualization (tumor-to-muscle ratios of 75.4{\^A}{\textpm}5.5). These data suggest that (18)F-AmBF3-MJ9 is a promising PET tracer for imaging GRPR-expressing prostate cancers.},
	author = {Pourghiasian, M. and Liu, Z. and Pan, J. and Zhang, Z. and Colpo, N. and Lin, K. S. and Perrin, D. M. and Benard, F.}
}
