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

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


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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Gonadotropin-Releasing Hormone* / pharmacokinetics
  • Humans
  • Immunohistochemistry
  • Indium Radioisotopes*
  • Male
  • Mice
  • Mice, Nude
  • Molecular Structure
  • Neoplasm Transplantation
  • Neoplasms, Experimental / diagnosis
  • Prostatic Neoplasms / diagnosis*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon
  • Transplantation, Heterologous


  • Indium Radioisotopes
  • Gonadotropin-Releasing Hormone