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Developing Isoxazole as a Native Photo-Cross-Linker for Photoaffinity Labeling and Chemoproteomics
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-09-23 , DOI: 10.1002/anie.202209947
Ke Cheng 1, 2 , Junyang Qi 2 , Xiaojie Ren 1 , Jie Zhang 1 , Huangxu Li 1 , Hanyue Xiao 1 , Rui Wang 3 , Zhiyang Liu 1 , Lingkuan Meng 1 , Nan Ma 4, 5 , Hongyan Sun 1
Affiliation  

Isoxazole is an essential pharmacophore in drug discovery. In this study, we investigated the photochemistry of isoxazole with biomolecules and developed it as a natively embedded photo-cross-linker for chemoproteomics and drug discovery. With this strategy, two isoxazole-containing drugs were successfully applied to chemoproteomic platforms to uncover their cellular targets and interactions.

中文翻译:

开发异恶唑作为用于光亲和标记和化学蛋白质组学的天然光交联剂

异恶唑是药物发现中必不可少的药效团。在这项研究中,我们研究了异恶唑与生物分子的光化学,并将其开发为一种天然嵌入的光交联剂,用于化学蛋白质组学和药物发现。通过这种策略,两种含异恶唑的药物成功应用于化学蛋白质组学平台,以揭示它们的细胞靶点和相互作用。
更新日期:2022-09-23
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