A DOTA-peptide conjugate by copper-free click chemistry

被引:30
|
作者
Martin, Molly E. [2 ]
Parameswarappa, Sharavathi G. [1 ]
O'Dorisio, M. Sue [2 ]
Pigge, F. Christopher [1 ]
Schultz, Michael K. [3 ,4 ]
机构
[1] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA
[2] Univ Iowa, Carver Coll Med, Dept Pediat, Iowa City, IA 52242 USA
[3] Univ Iowa, Carver Coll Med, Dept Radiol, Iowa City, IA 52242 USA
[4] Univ Iowa, Carver Coll Med, Dept Radiat Oncol, Iowa City, IA 52242 USA
关键词
DOTA; Copper-free; Click chemistry; Peptides; Chelators; Bioconjugates;
D O I
10.1016/j.bmcl.2010.06.111
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Attachment of DOTA to a novel monofluoro-cyclooctyne facilitates bioconjugation to an azide-modified peptide via Cu-free click chemistry. The resulting conjugate was radiolabeled with (111)In to afford a potential targeted molecular imaging agent with high specific activity and an excellent radiochemical purity. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4805 / 4807
页数:3
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