Strain-Promoted Copper-Free "Click" Chemistry for 18F Radiolabeling of Bombesin

被引:107
|
作者
Campbell-Verduyn, Lachlan S. [2 ]
Mirfeizi, Leila [1 ]
Schoonen, Anne K. [2 ]
Dierckx, Rudi A. [1 ]
Elsinga, Philip H. [1 ]
Feringa, Ben L. [2 ]
机构
[1] Univ Groningen, Dept Nucl Med & Mol Imaging, Univ Med Ctr Groningen, NL-9713 GZ Groningen, Netherlands
[2] Univ Groningen, Stratingh Inst Chem, NL-9747 AG Groningen, Netherlands
关键词
click chemistry; imaging agents; isotopic labeling; peptides; radiopharmaceuticals; RECEPTOR TARGETED RADIOPHARMACEUTICALS; AZIDE-ALKYNE CYCLOADDITION; PROSTATE-CANCER; 1,3-DIPOLAR CYCLOADDITION; LABELING METHOD; LIVING CELLS; PEPTIDE; ANALOGS; PET; F-18;
D O I
10.1002/anie.201105547
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Click for PET: The GRP-receptor-specific peptide bombesin, which is often used for nuclear imaging of tumors, can be labeled with 18F in a mild and rapid manner by using a copper-free azide-alkyne "click" reaction. A range of azides can be used to provide peptides with different hydrophobicities. The resulting 18F radiopharmaceutical tracers (see scheme) maintain their high affinity for the targeted receptor in vitro in human prostate cancer cells. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码:11117 / 11120
页数:4
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