Evaluation and comparison of a new DOTA and DTPA-bombesin agonist in vitro and in vivo in low and high GRPR expressing prostate and breast tumor models

Appl Radiat Isot. 2015 Feb:96:91-101. doi: 10.1016/j.apradiso.2014.11.006. Epub 2014 Nov 11.

Abstract

We evaluated and compared a new bombesin analog [Tyr-Gly5, Nle(14)]-BBN(6-14) conjugated to DOTA or DTPA and radiolabeled with In-111 in low and high GRPR expressing tumor models. Both peptides were radiolabeled with high radiochemical purity and specific activity. In vitro assays on T-47D, LNCaP and PC-3 cells showed that the affinity of peptides is similar and a higher binding and internalization of DOTA-peptide to PC-3 cells was observed. Both peptides could target PC-3 and LNCaP tumors in vivo and both tumor types could be visualized by microSPECT/CT.

Keywords: Bombesin; Comparison; DOTA; DTPA; GRPR.

Publication types

  • Comparative Study
  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bombesin / analogs & derivatives*
  • Bombesin / chemistry
  • Breast Neoplasms / diagnostic imaging*
  • Breast Neoplasms / metabolism*
  • Cell Line, Tumor
  • Drug Stability
  • Female
  • Heterocyclic Compounds, 1-Ring*
  • Heterografts
  • Humans
  • In Vitro Techniques
  • Indium Radioisotopes
  • Male
  • Mice, SCID
  • Neoplasm Transplantation
  • Pentetic Acid / analogs & derivatives*
  • Prostatic Neoplasms / diagnostic imaging*
  • Prostatic Neoplasms / metabolism*
  • Radionuclide Imaging
  • Radiopharmaceuticals* / chemistry
  • Receptors, Bombesin / metabolism*
  • Tissue Distribution

Substances

  • Heterocyclic Compounds, 1-Ring
  • Indium Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Bombesin
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Pentetic Acid
  • Bombesin