Comparative study of 64Cu/NOTA-[D-Tyr6,βAla11,Thi13,Nle14]BBN(6-14) monomer and dimers for prostate cancer PET imaging.

EJNMMI Research
Patrick FournierBrigitte Guérin

Abstract

Gastrin-releasing peptide receptors [GRPR] are highly over-expressed in multiple cancers and have been studied as a diagnostic target. Multimeric gastrin-releasing peptides are expected to have enhanced tumor uptake and affinity for GRPR. In this study, a 64Cu-labeled 1,4,7-triazacyclononane-1,4,7-triacetic acid [NOTA]-monomer and two NOTA-dimers of [D-Tyr6,βAla11, Thi13, Nle14]bombesin(6-14) ] [BBN(6-14)] were compared. Monomeric and dimeric peptides were synthesized on solid phase support and radiolabeled with 64Cu. NOTA-dimer 1 consists of asymmetrically linked BBN(6-14), while NOTA-dimer 2 has similar spacer between the two BBN(6-14) ligands and the chelator. In vitro GRPR-binding affinities were determined with competitive binding assays on PC3 human prostate cancer cells. In vivo stability and biodistribution of radiolabeled compounds were assessed in Balb/c mice. Cellular uptake and efflux were measured with radiolabeled NOTA-monomer and NOTA-dimer 2 on PC3 cells for up to 4 h. In vivo biodistribution kinetics were measured in PC3 tumor-bearing Balb/c nude mice by μ-positron emission tomography [μPET] imaging and confirmed by dissection and counting. NOTA-monomer, NOTA-dimers 1 and 2 were prepared with purity of 99%. The...Continue Reading

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Citations

Mar 16, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mazen JamousWalter Mier
May 30, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Gabriel FischerCarmen Wängler
Apr 15, 2014·Contrast Media & Molecular Imaging·Donghui PanMin Yang
Sep 16, 2014·Neoplasia : an International Journal for Oncology Research·Frédéric CoutureBrigitte Guérin
Feb 26, 2016·Natural Product Reports·C L CharronL G Luyt
Apr 25, 2020·Bioorganic Chemistry·Fariba MalekiNourollah Sadeghzadeh

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