Applied Radiation and Isotopes 2015-02-01

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.

Priscilla B Pujatti, Julie M Foster, Ciara Finucane, Chantelle D Hudson, Jerome C Burnet, Kerly F M Pasqualoto, Jair Mengatti, Stephen J Mather, Elaine B de Araújo, Jane K Sosabowski

Index: Appl. Radiat. Isot. 96 , 91-101, (2014)

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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. Copyright © 2014 Elsevier Ltd. All rights reserved.