Key advances in the development of reversible covalent inhibitors.
作者信息
Zheng Jiyue, Zhang Guiping, Li Jie Jack
机构信息
Center for Drug Design and Development, Suzhou Genhouse Bio Co., Ltd., Suzhou, Jiangsu, China.
出版信息
Future Med Chem. 2025 Feb;17(4):389-392. doi: 10.1080/17568919.2025.2453407. Epub 2025 Jan 19.
Abstract
摘要
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Key advances in the development of reversible covalent inhibitors.
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本文引用的文献
1
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Nat Commun. 2024 Oct 4;15(1):8606. doi: 10.1038/s41467-024-52573-2.
2
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3
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