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

来源：

CARBOHYDRATE RESEARCH | 2011年 / 346卷 / 01期

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

页码：26 / 34

页数：9