Service de Chimie Bio-organique et Marquage, DRF-JOLIOT-SCBM, CEA, Université Paris-Saclay, 91191, Gif-sur-Yvette, France.
Service d'Ingénierie Moléculaire des Protéines, DRF-JOLIOT-SIMOPRO, CEA, Université Paris-Saclay, 91191, Gif-sur-Yvette, France.
Angew Chem Int Ed Engl. 2017 Dec 4;56(49):15612-15616. doi: 10.1002/anie.201708790. Epub 2017 Nov 10.
We report the discovery of a new bioorthogonal click-and-release reaction involving iminosydnones and strained alkynes. This transformation leads to two products resulting from the ligation and fragmentation of iminosydnones under physiological conditions. Optimized iminosydnones were successfully used to design innovative cleavable linkers for protein modification, thus opening up new areas in the fields of drug release and target-fishing applications. This click-and-release technology offers the possibility of exchanging tags on proteins for functionalized cyclooctynes under mild and bioorthogonal conditions.
我们报告了一种新的生物正交点击-释放反应的发现，涉及亚氨基喋呤和张力炔烃。这种转化导致了两种产物，它们是在生理条件下亚氨基喋呤的连接和断裂产生的。优化的亚氨基喋呤被成功地用于设计用于蛋白质修饰的创新可裂解连接子，从而在药物释放和目标捕捞应用领域开辟了新的领域。这种点击-释放技术提供了在温和和生物正交条件下用功能化环辛炔交换蛋白质上标签的可能性。
