Site-specific labeling of 'second generation' annexin V with Tc-99m(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 M. Verbruggen*, Dirk Rattat

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

24 Citations (Web of Science)

Abstract

In this study 'second generation' AnxV was specifically labeled with Tc-99m 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 Tc-99m(CO)(3) in comparison to Tc-99m-HYNIC-cys-AnxV and Tc-99m(CO)(3)-DTPA-cys-AnxV.
Original languageEnglish
Pages (from-to)1356-1363
JournalBioorganic & Medicinal Chemistry
Volume18
Issue number3
DOIs
Publication statusPublished - 1 Feb 2010

Keywords

  • Annexin V
  • Apoptosis
  • Technetium-99m
  • Tricarbonyl labeling
  • Imaging

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