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Bioorg Med Chem Lett. 2011 Sep 15;21(18):5184-7. doi: 10.1016/j.bmcl.2011.07.055. Epub 2011 Jul 23.

A novel indium-111-labeled gonadotropin-releasing hormone peptide for human prostate cancer imaging.

Author information

1
College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.

Abstract

The purpose of this study was to evaluate the tumor targeting and imaging properties of a novel (111)In-labeled gonadotropin-releasing hormone (GnRH) peptide {1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Ahx-(D-Lys(6)-GnRH1)} for human prostate cancer. The biodistribution and tumor imaging properties of (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1) were determined in DU145 human prostate cancer-xenografted nude mice. (111)In-DOTA-Ahx-(d-Lys(6)-GnRH1) exhibited rapid tumor uptake (1.27 ± 0.40% ID/g at 0.5h post-injection) coupled with fast whole-body clearance through the urinary system. The DU145 human prostate cancer-xenografted tumor lesions were clearly visualized by single photon emission computed tomography (SPECT)/CT at 0.5h post-injection of (111)In-DOTA-Ahx-(D-Lys(6)-GnRH1). The successful imaging of DU145 human prostate cancer-xenografted tumor lesions using (111)In-DOTA-Ahx-(d-Lys(6)-GnRH1) highlighted its potential as a novel imaging probe for human prostate cancer imaging.

PMID:
21821417
PMCID:
PMC3159814
DOI:
10.1016/j.bmcl.2011.07.055
[Indexed for MEDLINE]
Free PMC Article

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