Structure-based development of potent and selective type-II kinase inhibitors of RIPK1.

"sd 4 9 coordinates and structure factors for the co-crystal structure of ripk1 kinase domain (1-294 c34a c127a c233a c240a) and 20 have been deposited in the protein data bank with the accession number 8i2n."

"Conflicts of interest Li Tan, Ying Li, Ying Qin, Chunting Qi, and Huaijiang Xiang are inventors on patent applications relating to this work, owned by SIOC, CAS."

"We thank Prof. Junying Yuan (IRCBC of CAS, Shanghai, China) and Dr. Jidong Zhu (Etern Therapeutics, Shanghai, China) for their generous help on this work, Dr. Sudan He (ISM of CAMS, Suzhou, China) for providing RIPK3-FKBP NIH/3T3 cells, and National Facility for Protein Science in Shanghai (China) for the help in animal studies. This work was supported by grants from the 10.13039/501100001809National Natural Science Foundation of China (Grants Nos. 21837004, 82151212, and 32170755), the Strategic Priority Research Program of the 10.13039/501100002367Chinese Academy of Sciences (XDB39050500, China), Shanghai Municipal Science and Technology Major Project (Grant No.2019SHZDZX02, China). Conceptualization: Li Tan and Ying Li; Methodology: Li Tan, Ying Li, Ying Qin, Lifeng Pan, Zheng Zhang and, Yechun Xu; Investigation and Formal Analysis: Ying Qin, Dekang Li, Chunting Qi, Huaijiang Xiang, Huyan Meng, Jingli Liu, Shaoqing Zhou, Xinyu Gong, Ying Li, Guifang Xu, Rui Zu, Hang Xie, and Gang Xu; Software: Huaijiang Xiang, Xinyu Gong, and Lifeng Pan; Resources: Shi Chen; Writing-Original Draft: Li Tan, Ying Li, Ying Qin, and Dekang Li; Writing-Review & Editing: All the authors; Supervision: Li Tan, Ying Li, Lifeng Pan, Shi Chen, Zheng Zhang, and Yechun Xu; Funding acquisition: Li Tan, Ying Li, and Zheng Zhang."