Radiolabeling of annexin A5 with 99mTc: comparison of HYNIC-Tc vs. iminothiolane-Tc-tricarbonyl conjugates

Biechlin, Marie-Laure; Bonmartin, Alain; Gilly, François-Noël; Fraysse, Marc; du Moulinet d'Hardemare, Amaury

doi:10.1016/j.nucmedbio.2008.05.009

« Previous Next »Nuclear Medicine and Biology
Volume 35, Issue 6 , Pages 679-687, August 2008

Radiolabeling of annexin A5 with ^99mTc: comparison of HYNIC-Tc vs. iminothiolane-Tc-tricarbonyl conjugates

Marie-Laure Biechlin
- Faculté de Médecine Lyon-Sud (EA 3738), 69921 Oullins, France
- Radiopharmacie, Centre Hospitalier de Chambéry, 73000 Chambéry, France
- Corresponding authors. Marie-Laure Biechlin is to be contacted at Centre Hospitalier de Chambéry, Service de médecine nucléaire, Rue Pierre et Marie Curie, 73 000 Chambéry, France. Tel.: +33 4 79 96 50 72; fax: +33 4 79 96 51 78. Amaury du Moulinet d'Hardemare, Département de Chimie Moléculaire, Equipe de Chimie Inorganique Redox et Biomimétique, Université Joseph Fourier-Grenoble I (DCM UMR 5250, ICMG), 301 rue de la Chimie, 38041 Grenoble cedex 9, France. Tel.: +33 4 76 63 57 05; fax: +33 4 76 51 48 36.
Alain Bonmartin
- Faculté de Médecine Lyon-Sud (EA 3738), 69921 Oullins, France
François-Noël Gilly
- Faculté de Médecine Lyon-Sud (EA 3738), 69921 Oullins, France
Marc Fraysse
- Radiopharmacie, Centre Hospitalier Lyon Sud, 69495 Pierre-Bénite, France
Amaury du Moulinet d'Hardemare
- Département de Chimie Moléculaire, Equipe de Chimie Inorganique Redox et Biomimétique, Université Joseph Fourier-Grenoble I (DCM UMR 5250, ICMG), 38041 Grenoble cedex 9, France
- Corresponding authors. Marie-Laure Biechlin is to be contacted at Centre Hospitalier de Chambéry, Service de médecine nucléaire, Rue Pierre et Marie Curie, 73 000 Chambéry, France. Tel.: +33 4 79 96 50 72; fax: +33 4 79 96 51 78. Amaury du Moulinet d'Hardemare, Département de Chimie Moléculaire, Equipe de Chimie Inorganique Redox et Biomimétique, Université Joseph Fourier-Grenoble I (DCM UMR 5250, ICMG), 301 rue de la Chimie, 38041 Grenoble cedex 9, France. Tel.: +33 4 76 63 57 05; fax: +33 4 76 51 48 36.

Received 18 March 2008; received in revised form 24 April 2008; accepted 27 May 2008.

Abstract

In the perspective of expanding the use of annexin A5 (anx A5) as radioactive tracer of cell death in vivo, we recently described its radiolabeling with ^99mTc-tricarbonyl [^99mTc(H₂O)₃(CO)₃]⁺ via the mercaptobutyrimidyl group (anx A5-SH). The aim of the present article was to compare this new method with the HYNIC strategy (anx A5-HYNIC), recognized at present as the reference for the radiolabeling of proteins with ^99mTc. Similar radiolabeling yields and better chemical stability were obtained with the [anx A5-SH-^99mTc-tricarbonyl] complex. Since the [anx A5-HYNIC-^99mTc(tricine)₂] conjugate shows isomeric forms which can affect the biological properties whereas [anx A5-SH-^99mTc-tricarbonyl] is less or not prone to such drawback, the latter seems superior to the former. Furthermore, (anx A5-SH) is readily obtained via commercial sources of Traut's reagent whereas (anx A5-HYNIC) is not. The results provide encouraging evidence in the development of anx A5-labeled reagent for apoptose imaging.