A Click procedure with heterogeneous copper to tether technetium-99m chelating agents and rhenium complexes. Evaluation of the chelating properties and biodistribution of the new radiolabelled glucose conjugates

被引:27
作者
Benoist, Eric [1 ,2 ]
Coulais, Yvon [3 ]
Almant, Mehdi
Kovensky, Jose
Moreau, Vincent
Lesur, David
Artigau, Marine [1 ,2 ]
Picard, Claude [1 ,2 ]
Galaup, Chantal [1 ,2 ]
Gouin, Sebastien G.
机构
[1] SPCMIB, Lab Synth & Physicochim Mol Interet Biol, UMR 5068, F-31062 Toulouse 9, France
[2] Univ Toulouse, Lab Synth & Physicochim Mol Interet Biol, SPCMIB, UPS,UMR 5068, F-31062 Toulouse 9, France
[3] Fac Med Purpan, Lab Traceurs & Traitement Image, F-31062 Toulouse 9, France
关键词
Glycoconjugates; Heterogeneous click chemistry; Bioconjugation; Metal complexes; IN-VITRO; METAL COMPLEXATION; HUMAN THYMIDINE; TO-CHELATE; TECHNETIUM; CHEMISTRY; INHIBITORS; DESIGN; VIVO; BIOMOLECULES;
D O I
10.1016/j.carres.2010.10.011
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
An efficient protocol was developed to tether chelating agents and rhenium complexes onto a glucoside scaffold with a heterogeneous copper catalyst via click chemistry. The supported catalyst avoids the formation of unwanted copper complexes during the cyclisation step. The possibility to graft a pre-chelated M(CO)(3) core by click chemistry onto a biomolecule was highlighted for the first time. Tc-99m(CO)(3)-glucoconjugates displayed excellent in vitro stability, a fast in vivo blood clearance and a low specific organ uptake or long-term retention in spleen and stomach. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:26 / 34
页数:9
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