In vitro and in vivo evaluation of a64Cu-labeled NOTA-Bn-SCN-Aoc-bombesin analogue in gastrin-releasing peptide receptor expressing prostate cancer

Jeffrey M. Craft, Ravindra A. De Silva, Kimberly A. Lears, Rebecca Andrews, Kexian Liang, Samuel Achilefu, Buck E. Rogers, Jeffrey M. Craft, Ravindra A. De Silva, Kimberly A. Lears, Rebecca Andrews, Kexian Liang, Samuel Achilefu, Buck E. Rogers

Index: Nucl. Med. Biol. 39(5) , 609-16, (2012)

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Abstract

Introduction Bombesin (BN) is an amphibian peptide that binds to the gastrin-releasing peptide receptor (GRPR). It has been demonstrated that BN analogues can be radiolabeled for potential diagnosis and treatment of GRPR-expressing malignancies. Previous studies have conjugated various chelators to the eight C-terminal amino acids of BN [BN(7-14)] for radiolabeling with 64Cu. Recently, (1,4,7-triazacyclononane-1,4,7-triacetic acid) (NOTA) has been evaluated as the five-coordinate 64Cu complex, with results indicating GRPR-specific tumor uptake. This study aimed to conjugate S-2-(4-isothiocyanatobenzyl)-NOTA (p-SCN-Bn-NOTA) to BN(7-14) such that it could form a six-coordinate complex with 64Cu and to evaluate the resulting peptide.