Neurotensin analogs by fluoroglycosylation at N^ω-carbamoylated arginines for PET imaging of NTS1-positive tumors.

ABSTRACT: Since neurotensin (NT) receptors of subtype-1 (NTS1) are expressed by different types of malignant tumors, such as pancreatic adenocarcinoma, colorectal and prostate carcinoma, they represent an interesting target for tumor imaging by positron emission tomography (PET) and endoradiotherapy. Previously reported neurotensin-derived NTS1 ligands for PET were radiolabeled by modification and prelongation of the N-terminus of NT(8-13) peptide analogs. In this study, we demonstrate that modifying Arg⁸ or Arg⁹ by N^ω-carbamoylation and subsequent fluoroglycosylation provides a suitable approach for the development of NT(8-13) analogs as PET imaging agents. The N^ω-carbamoylated and fluoroglycosylated NT(8-13) analogs retained high NTS1 affinity in the one

SUBMITTER: Schindler L 

PROVIDER: S-EPMC9440028 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature