Site-specific labeling of 'second generation' annexin V with (99m)Tc(CO)(3) for improved imaging of apoptosis in vivo.
Bioorganic & medicinal chemistry 2010 Jan 4; In press
De Saint-Hubert M, Mottaghy F FM, Vunckx K, Nuyts J, Fonge H, Prinsen K, Stroobants S, Mortelmans L, Deckers N, Hofstra L, Reutelingsperger C CP, Verbruggen A, Rattat D
Department of Nuclear Medicine, University Hospital Gasthuisberg Leuven, Herestraat 49, B-3000 Leuven, Belgium.
In this study 'second generation' AnxV was specifically labeled with (99m)Tc in three different ways outside the binding region of the protein to obtain an improved target-to-background activity ratio. The compounds were tested in vitro and in vivo in normal mice and in a model of hepatic apoptosis (anti-Fas mAb). The apoptosis binding was most prominent for the HIS-tagged 'second generation' AnxV labeled with (99m)Tc(CO)(3) in comparison to (99m)Tc-HYNIC-cys-AnxV and (99m)Tc(CO)(3)-DTPA-cys-AnxV.