Gallium labeled NOTA-based conjugates for peptide receptor-mediated medical ima...

• Author(s): Sá, Arsénio Vasconcelos de ; Matias, Áurea A. ; Prata, M. Isabel M. ; Geraldes, Carlos F. G. C. ; Ferreira, Paula M. T. ; André, João P.
• Date: 2010
• Persistent ID: http://hdl.handle.net/1822/14303
• Origin: RepositóriUM - Universidade do Minho
• Subject(s): Triaza; Orthogonal protection; Bifunctional chelators; Gallium; Radiopharmacy; Integrin αѵβ₃receptor
• Document Type: Article
• Language: English

Description

We report a straightforward and efficient synthetic strategy for the synthesis of three model glycine-arginine-glycine-aspartic-glycine (GRGDG) conjugates based on derivatives of NOTA and of their Ga(III) complexes targeted to the integrin αѵβ₃receptor. 71Ga NMR spectroscopy showed that the Ga(III)-labeled conjugates are highly stable in aqueous solution. The 67Ga-labeled conjugates proved to have high kinetic stability and showed a weak but specific binding to the receptors in a U87MG-glioblastoma cell line.