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

作者：Guo Haixun; Gallazzi Fabio; Sklar Larry A; Miao Yubin^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(18): 5184-5187.

DOI：10.1016/j.bmcl.2011.07.055

• Gonadotropin-releasing hormone receptor
• Receptor-targeting peptide
• Prostate cancer
• Imaging

The purpose of this study was to evaluate the tumor targeting and imaging properties of a novel In-111-labeled gonadotropin-releasing hormone (GnRH) peptide {1,4,7,10-tetraazacyclododecane1,4,7,10-tetraacetic acid (DOTA)-Ahx-(D-Lys(6)-GnRH1)} for human prostate cancer. The biodistribution and tumor imaging properties of In-111-DOTA-Ahx-(D-Lys(6)-GnRH1) were determined in DU145 human prostate cancer-xenografted nude mice. In-111-DOTA-Ahx-(D-Lys(6)-GnRH1) exhibited rapid tumor uptake (1.27 +/- 0.40% ID/g at 0.5 h 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 0.5 h post-injection of In-111-DOTA-Ahx-(D-Lys(6)GnRH1). The successful imaging of DU145 human prostate cancer-xenografted tumor lesions using In-111-DOTA-Ahx-(D-Lys(6)-GnRH1) highlighted its potential as a novel imaging probe for human prostate cancer imaging.

• 出版日期2011-9-15