Gallium labeled NOTA-based conjugates for peptide receptor-mediated medical imaging

✍ Scribed by Arsénio de Sá; Áurea A. Matias; M. Isabel M. Prata; Carlos F.G.C. Geraldes; P.M.T. Ferreira; João P. André

• Book ID: 104005020
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 184 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.10.059

✦ Synopsis

We report a straightforward and efficient synthetic strategy for the synthesis of three model glycine-arginine-glycine-aspartic acid-glycine (GRGDG) conjugates based on derivatives of NOTA and of their Ga(III) complexes targeted to the integrin α(ν)β(3) receptor. (71)Ga NMR spectroscopy showed that the Ga(III)-labeled conjugates are highly stable in aqueous solution. The (67)Ga-labeled conjugates proved to have high kinetic stability and showed a weak but specific binding to the receptors in a U87MG-glioblastoma cell line.