125I-Radiolabeled Morpholine-Containing Arginine鈥揋lycine鈥揂spartate (RGD) Ligand of 伪v尾3 Integrin As a Molecular Imaging Probe for Angiogenesis

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• 作者：Francesca Bianchini ; Nicoletta Cini ; Andrea Trabocchi ; Anna Bottoncetti ; Silvia Raspanti ; Eleonora Vanzi ; Gloria Menchi ; Antonio Guarna ; Alberto Pupi ; Lido Calorini
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：June 14, 2012
• 年：2012
• 卷：55
• 期：11
• 页码：5024-5033
• 全文大小：455K
• 年卷期：v.55,no.11(June 14, 2012)
• ISSN：1520-4804

文摘

In this paper, using a hybrid small-animal Micro SPECT/CT imaging system, we report that a new ¹²⁵I-Cilengitide-like RGD-cyclopentapeptide, containing d-morpholine-3-carboxylic acid, interacts in vivo with 伪_v尾₃ integrin expressed by melanoma cells. Images clearly show that the ¹²⁵I-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 ¹²⁵I-labeled morpholine-based RGD-cyclopentapeptides targeting 伪_v尾₃ positive tumors may play a role in future therapeutic strategies.