Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology.

ABSTRACT:

Background

The gastrin-releasing peptide receptor (GRPR) has been extensively studied as a biomolecular target for peptide-based radiotheranostics. However, the lack of metabolic stability and the rapid clearance of peptide radioligands, including radiolabeled GRPR-antagonists, often impede clinical application. Aiming at circumventing these drawbacks, we have designed three new GRPR-antagonist radioligands using [^99mTc]Tc-DB15 ([^99mTc]Tc-N₄-AMA-DIG-_DPhe-Gln-Trp-Ala-Val-Sar-His-Leu-NHEt; AMA: p-aminomethylaniline; DIG: diglycolate) as a motif, due to its high GRPR-affinity and stability to neprilysin (NEP). The new analogues carry the DOTAGA-chelator (1,4,7,10-tetraazacyclododecane-1-glutaric acid-4,7,10-triacetic acid) through different

SUBMITTER: Kanellopoulos P 

PROVIDER: S-EPMC10873254 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature