title: Radiolabeling of annexin A5 with (99m)Tc: comparison of HYNIC-Tc vs. iminothiolane-Tc-tricarbonyl conjugates.
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 (99m)Tc-tricarbonyl [(99m)Tc(H(2)O)(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 (99m)Tc. Similar radiolabeling yields and better chemical stability were obtained with the [anx A5-SH-(99m)Tc-tricarbonyl] complex. Since the [anx A5-HYNIC-(99m)Tc(tricine)(2)] conjugate shows isomeric forms which can affect the biological properties whereas [anx A5-SH-(99m)Tc-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.
authors.affiliation: Faculté de Médecine Lyon-Sud, Oullins, France. marie.laure.biechlin@ch-chambery.fr
authors.forename: Marie-Laure
authors.initials: ML
authors.lastname: Biechlin
authors.forename: Alain
authors.initials: A
authors.lastname: Bonmartin
authors.forename: François-Noël
authors.initials: FN
authors.lastname: Gilly
authors.forename: Marc
authors.initials: M
authors.lastname: Fraysse
authors.forename: Amaury
authors.initials: A
authors.lastname: du Moulinet d'Hardemare
mesh_terms: D017304:Annexin A5 / Q000737:chemistry*; D004355:Drug Stability; D006834:Hydrazines / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D009539:Nicotinic Acids / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000737:chemistry*; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D013667:Technetium / Q000737:chemistry*
chemical_list: C120392:6-hydrazinopyridine-3-carboxylic acid; D017304:Annexin A5; D006834:Hydrazines; D009539:Nicotinic Acids; D019275:Radiopharmaceuticals; D013438:Sulfhydryl Compounds; D013667:Technetium