| Structure-based development of potent and selective type-Ⅱ kinase inhibitors of RIPK1 |
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| 作者姓名： | Ying Qin Dekang Li Chunting Qi Huaijiang Xiang Huyan Meng Jingli Liu Shaoqing Zhou Xinyu Gong Ying Li Guifang Xu Rui Zu Hang Xie Yechun Xu Gang Xu Zheng Zhang Shi Chen Lifeng Pan Ying Li Li Tan |
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| 作者单位： | 1. Interdisciplinary Research Center on Biology and Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences;2. University of Chinese Academy of Sciences;3. State Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences;4. School of Chinese Materia Medica, Nanjing University of Chinese Medicine;5. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences;6. Institute of Hepatology, National Clinical Research Center for Infectious Disease, Shenzhen Third People's Hospital, the Second Affiliated Hospital, School of Medicine, Southern University of Science and Technology;7. Department of Burn and Plastic Surgery, Shenzhen Institute of Translational Medicine, Shenzhen University Medical School, Shenzhen Second People's Hospital, the First Affiliated Hospital of Shenzhen University |
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| 基金项目： | supported by grants from the National Natural Science Foundation of China (Grants Nos. 21837004, 82151212, and 32170755)；;the Strategic Priority Research Program of the Chinese Academy of Sciences (XDB39050500, China)； |
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| 摘 要： | Receptor-interacting serine/threonine-protein kinase 1(RIPK1) functions as a key regulator in inflammation and cell death and is involved in mediating a variety of inflammatory or degenerative diseases. A number of allosteric RIPK1 inhibitors(RIPK1i) have been developed, and some of them have already advanced into clinical evaluation. Recently, selective RIPK1i that interact with both the allosteric pocket and the ATP-binding site of RIPK1 have started to emerge. Here, we report the rational dev...
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