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

  作者 Guo, HX; Gallazzi, F; Sklar, LA; Miao, YB  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2011年21-18;  页码  5184-5187  
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[摘要]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-tetraazacyclododecane1,4,7,10-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 0.5 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 (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. (C) 2011 Elsevier Ltd. All rights reserved.

 
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