125I-Radiolabeled Morpholine-Containing Arginine–Glycine–Aspartate (RGD) Ligand of αvβ3 Integrin As a Molecular Imaging Probe for Angiogenesis

Autor:	E. Vanzi, Nicoletta Cini, Lido Calorini, Francesca Bianchini, Antonio Guarna, Gloria Menchi, Alberto Pupi, Andrea Trabocchi, S. Raspanti, Anna Bottoncetti
Rok vydání:	2012
Předmět:	Integrin alphaVbeta3 Arginine biology Angiogenesis Ligand Integrin Molecular biology Transplantation chemistry.chemical_compound chemistry In vivo Morpholine Drug Discovery biology.protein Molecular Medicine
Zdroj:	Journal of Medicinal Chemistry. 55:5024-5033
ISSN:	1520-4804 0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::5c73b62d69378e574b0d16a611bb7877 https://doi.org/10.1021/jm2016232 Zobrazit plný text záznamu