Optimizing uPAR-targeting radiopeptides for improved tissue distribution: progress towards radionuclide therapy.

ABSTRACT:

Purpose

The aim of this study was to develop radiopeptides for targeting the urokinase-type plasminogen activator receptor (uPAR) modified with an albumin-binding moiety to improve their tissue distribution profiles.

Methods

uPAR-11, uPAR-12, uPAR-14, uPAR-15, uPAR-17 and uPAR-18 were synthesized based on the AE105 nonapeptide which was modified with the p-tolyl-based albumin binder and variable linker entities and chelators. The ¹⁷⁷Lu-labeled peptides were evaluated in vitro with regard to their stability, albumin-binding properties and uPAR-binding affinity using HEK-uPAR cells. Biodistribution and SPECT/CT imaging studies were performed with HEK-uPAR xenografted nude mice. The acquired data were compared to those obtained with [¹⁷⁷Lu]Lu-DOTA-AE105.

SUBMITTER: Vaccarin C 

PROVIDER: S-EPMC12920294 | biostudies-literature | 2026 Mar

REPOSITORIES: biostudies-literature