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

Marijke De Saint-Hubert; Felix M Mottaghy; Kathleen Vunckx; Johan Nuyts; Humphrey Fonge; Kristof Prinsen; Sigrid Stroobants; Luc Mortelmans; Niko Deckers; Leo Hofstra; Chris P M Reutelingsperger; Alfons Verbruggen; Dirk Rattat

doi:10.1016/j.bmc.2009.12.021

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

Bioorg Med Chem. 2010 Feb;18(3):1356-63. doi: 10.1016/j.bmc.2009.12.021. Epub 2010 Jan 5.

Authors

Marijke De Saint-Hubert¹, Felix M Mottaghy, Kathleen Vunckx, Johan Nuyts, Humphrey Fonge, Kristof Prinsen, Sigrid Stroobants, Luc Mortelmans, Niko Deckers, Leo Hofstra, Chris P M Reutelingsperger, Alfons Verbruggen, Dirk Rattat

Affiliation

¹ Department of Nuclear Medicine, University Hospital Gasthuisberg Leuven, Herestraat 49, B-3000 Leuven, Belgium.

PMID: 20053567
DOI: 10.1016/j.bmc.2009.12.021

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Annexin A5* / chemistry
Apoptosis*
Hepatocytes / cytology
Mice
Technetium* / chemistry
Tomography, Emission-Computed, Single-Photon / methods*

Substances

Annexin A5
Technetium