¹²⁵I-Radiolabeled Morpholine-Containing Arginine–Glycine–Aspartate (RGD) Ligand of α_vβ₃ Integrin As a Molecular Imaging Probe for Angiogenesis

Abstract

In this paper, using a hybrid small-animal Micro SPECT/CT imaging system, we report that a new (125)I-Cilengitide-like RGD-cyclopentapeptide, containing d-morpholine-3-carboxylic acid, interacts in vivo with α(v)β(3) integrin expressed by melanoma cells. Images clearly show that the (125)I-compound has the capacity to monitor the growth of a melanoma xenograft. Indeed, retention of the labeled ligand in the tumor mass has a good tumor/background ratio, and a significant reduction of its uptake was observed after injection of unlabeled ligand. These results suggest that the use of (125)I-labeled morpholine-based RGD-cyclopentapeptides targeting α(v)β(3) positive tumors may play a role in future therapeutic strategies.