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
Number of pages	8
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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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

@article{123c7d7dcfd045d8abe05ffb2b6362a8,

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",

year = "2010",

month = feb,

day = "1",

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

language = "English",

volume = "18",

pages = "1356--1363",

journal = "Bioorganic \& Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "3",

}

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

TY - JOUR

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

Y1 - 2010/2/1

N2 - 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.

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

U2 - 10.1016/j.bmc.2009.12.021

DO - 10.1016/j.bmc.2009.12.021

M3 - Article

C2 - 20053567

SN - 0968-0896

VL - 18

SP - 1356

EP - 1363

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 3

ER -

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

Abstract

Keywords

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