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

doi:10.1016/j.bmc.2009.12.021

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 journal › Article › Academic › peer-review

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 language	English
Pages (from-to)	1356-1363
Journal	Bioorganic & Medicinal Chemistry
Volume	18
Issue number	3
DOIs	https://doi.org/10.1016/j.bmc.2009.12.021
Publication status	Published - 1 Feb 2010

Keywords

Annexin V
Apoptosis
Technetium-99m
Tricarbonyl labeling
Imaging

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10.1016/j.bmc.2009.12.021

Cite this

De Saint-Hubert, M., Mottaghy, F. M., Vunckx, K., Nuyts, J., Fonge, H., Prinsen, K., Stroobants, S., Mortelmans, L., Deckers, N., Hofstra, L., Reutelingsperger, C. P. M., Verbruggen, A. M., & Rattat, D. (2010). Site-specific labeling of 'second generation' annexin V with Tc-99m(CO)(3) for improved imaging of apoptosis in vivo. Bioorganic & Medicinal Chemistry, 18(3), 1356-1363. https://doi.org/10.1016/j.bmc.2009.12.021

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title = "Site-specific labeling of 'second generation' annexin V with Tc-99m(CO)(3) for improved imaging of apoptosis in vivo",

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. ",

keywords = "Annexin V, Apoptosis, Technetium-99m, Tricarbonyl labeling, Imaging",

author = "{De Saint-Hubert}, Marijke and Mottaghy, {Felix M.} and Kathleen Vunckx and Johan Nuyts and Humphrey Fonge and Kristof Prinsen and Sigrid Stroobants and Luc Mortelmans and Niko Deckers and Leo Hofstra and Reutelingsperger, {Chris P. M.} and Verbruggen, {Alfons M.} and Dirk Rattat",

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doi = "10.1016/j.bmc.2009.12.021",

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De Saint-Hubert, M, Mottaghy, FM, Vunckx, K, Nuyts, J, Fonge, H, Prinsen, K, Stroobants, S, Mortelmans, L, Deckers, N, Hofstra, L, Reutelingsperger, CPM, Verbruggen, AM & Rattat, D 2010, 'Site-specific labeling of 'second generation' annexin V with Tc-99m(CO)(3) for improved imaging of apoptosis in vivo', Bioorganic & Medicinal Chemistry, vol. 18, no. 3, pp. 1356-1363. https://doi.org/10.1016/j.bmc.2009.12.021

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T1 - Site-specific labeling of 'second generation' annexin V with Tc-99m(CO)(3) for improved imaging of apoptosis in vivo

AU - De Saint-Hubert, Marijke

AU - Mottaghy, Felix M.

AU - Vunckx, Kathleen

AU - Nuyts, Johan

AU - Fonge, Humphrey

AU - Prinsen, Kristof

AU - Stroobants, Sigrid

AU - Mortelmans, Luc

AU - Deckers, Niko

AU - Hofstra, Leo

AU - Reutelingsperger, Chris P. M.

AU - Verbruggen, Alfons M.

AU - Rattat, Dirk

PY - 2010/2/1

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AB - 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.

KW - Annexin V

KW - Apoptosis

KW - Technetium-99m

KW - Tricarbonyl labeling

KW - Imaging

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M3 - Article

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