Bioorg Med Chem. 2010 Feb;18(3):1356-63. Epub 2010 Jan 5.

Site-specific labeling of 'second generation' annexin V with 99mTc(CO)3 for improved imaging of apoptosis in vivo.

De Saint-Hubert M, Mottaghy FM, Vunckx K, Nuyts J, Fonge H, Prinsen K, Stroobants S, Mortelmans L, Deckers N, Hofstra L, Reutelingsperger CP, Verbruggen A, Rattat D.

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Department of Nuclear Medicine, University Hospital Gasthuisberg Leuven, Herestraat 49, B-3000 Leuven, Belgium.

Abstract

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.

PMID:: 20053567; [PubMed - indexed for MEDLINE]

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Site-specific labeling of 'second generation' annexin V with 99mTc(CO)3 for improved imaging of apoptosis in vivo.

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