New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone-cycloalkyne click reaction

被引：24

作者：

Richard, Mylene ^{[1
]}

Truillet, Charles ^{[1
]}

Vu Long Tran ^{[1
]}

Liu, Hui ^{[2
]}

Porte, Karine ^{[2
]}

Audisio, Davide ^{[2
]}

Roche, Melanie ^{[1
]}

Jego, Benoit ^{[1
]}

Cholet, Sophie ^{[3
]}

Fenaille, Francois ^{[3
]}

Kuhnast, Bertrand ^{[1
]}

Taran, Frederic ^{[2
]}

Specklin, Simon ^{[1
]}

机构：

[1] Univ Paris Saclay, Univ Paris Sud, CNRS, INSERM,SHFJ,CEA,IMIV,UMR 1023, Orsay, France

[2] Univ Paris Saclay, CEA, SCBM, DRF,JOLIOT, F-91191 Gif Sur Yvette, France

[3] Univ Paris Saclay, JOLIOT, CEA, SPI,DRF, F-91191 Gif Sur Yvette, France

来源：

CHEMICAL COMMUNICATIONS | 2019年 / 55卷 / 70期

关键词：

IN-VIVO CHEMISTRY; IMMUNO-PET; ANTIBODY; CARCINOMA; STRATEGY;

D O I：

10.1039/c9cc05486c

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

We report the first pretargeting in vivo study using the Strain-Promoted Sydnone-Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M-1 s(-1), the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.

引用

页码：10400 / 10403

页数：4

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