Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

Evaluation of novel 111In-labeled gonadotropin-releasing hormone peptides for human prostate cancer imaging

Evaluation of novel 111In-labeled gonadotropin-releasing hormone peptides for human prostate cancer imaging
The purpose of this study was to evaluate the tumor targeting and imaging properties of novel 111In-labeled gonadotropin-releasing hormone (GnRH) peptides for human prostate cancer. Three new 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-linker-D-Phe-(D-Lys6-GnRH) peptides with different hydrocarbon linkers were designed to evaluate their effects on GnRH receptor binding affinities. The Aoc (aminooctanoic acid) linker was better than βAla (beta alanine) and Aun (aminoundecanoic acid) linkers in retaining strong receptor binding affinity. DOTA-Aoc-D-Phe-(D-Lys6-GnRH) exhibited 6.6 ± 0.1 nM GnRH receptor binding affinity. 111In-DOTA-Aoc-D-Phe-(D-Lys6-GnRH) exhibited fast tumor uptake and urinary clearance in DU145 human prostate cancer-xenografted nude mice. The DU145 tumor lesions could be clearly visualized by single photon emission computed tomography (SPECT)/CT using 111In-DOTA-Aoc-D-Phe-(D-Lys6-GnRH) as an imaging probe, providing an insight into the design of new GnRH peptides for prostate cancer in the future.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17308995

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