1 research outputs found
Hybrid Bombesin Analogues: Combining an Agonist and an Antagonist in Defined Distances for Optimized Tumor Targeting
Radiolabeled
hybrid ligands with defined distances between an agonist
and an antagonist for the gastrin-releasing peptide receptor were
found to have excellent tumor-targeting properties. Oligoprolines
served as rigid scaffolds that allowed for tailoring distances of
10, 20, and 30 Ã… between the recognition elements. In vitro and
in vivo studies revealed that the hybrid ligand with a distance of
20 Ã… between the recognition elements exhibits the highest yet
observed tumor cell uptake and retention time in prostate cancer cells