HYNIC and DOMA conjugated radiolabeled bombesin analogs as receptor-targeted probes for scintigraphic detection of breast tumor.

ABSTRACT:

Background

Among the many peptide receptor systems, gastrin-releasing-peptide (GRP) receptors, the mammalian equivalent of bombesin (BN) receptors, are potential targets for diagnosis and therapy of breast tumors due to their overexpression in various frequently occurring human cancers. The aim of this study was to synthesize and comparative evaluation of ^99mTc-labeled new BN peptide analogs. Four new BN analogs, HYNIC-Asp[PheNle]BN(7-14)NH₂, BN1; HYNIC-Pro-Asp[TyrMet]BN(7-14)NH₂, BN2; HYNIC-Asp-Asn[Lys-CHAla-Nle]BN(7-14)NH₂, BN3; and DOMA-GABA[Pro-Tyr-Nle]BN(7-14)NH₂, BN4 were synthesized and biologically evaluated for targeted imaging of GRP receptor-positive breast-tumors.

Methods

Solid-phase synthesis using Fmoc-chem

SUBMITTER: De K 

PROVIDER: S-EPMC6423188 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature