Author: "Yang, Yiqing" / Journal: journal of medicinal chemistry - Searchworks@Jio Institute Digital Library Search Results

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Start Over Author "Yang, Yiqing" Journal journal of medicinal chemistry

Author: Yang, Yiqing, primary, Gao, Hongying, additional, Sun, Xiuyun, additional, Sun, Yonghui, additional, Qiu, Yueping, additional, Weng, Qinjie, additional, and Rao, Yu, additional
Published: 2020
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Author: Li, Mei-Xin, primary, Yang, Yiqing, additional, Zhao, Qiuye, additional, Wu, Yue, additional, Song, Lei, additional, Yang, Haiyan, additional, He, Ming, additional, Gao, Hongying, additional, Song, Bao-Liang, additional, Luo, Jie, additional, and Rao, Yu, additional
Published: 2020
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Author: Yang, Yiqing, primary, Cao, Lin, additional, Gao, Hongying, additional, Wu, Yue, additional, Wang, Yaxin, additional, Fang, Fang, additional, Lan, Tianlong, additional, Lou, Zhiyong, additional, and Rao, Yu, additional
Published: 2019
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Author: Yang, Yiqing, primary, Yu, You, additional, Li, Xiaolu, additional, Li, Jing, additional, Wu, Yue, additional, Yu, Jie, additional, Ge, Jingpeng, additional, Huang, Zhenghui, additional, Jiang, Lubin, additional, Rao, Yu, additional, and Yang, Maojun, additional
Published: 2017
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Author: Kaneshige, Atsunori, Yang, Yiqing, Bai, Longchuan, Wang, Mi, Xu, Renqi, Mallik, Leena, Chinnaswamy, Krishnapriya, Metwally, Hoda, Wang, Yu, McEachern, Donna, Tošović, Jelena, Yang, Chao-Yie, Kirchhoff, Paul D., Meagher, Jennifer L., Stuckey, Jeanne A., and Wang, Shaomeng
Abstract: STAT6 is an attractive therapeutic target for human cancers and other human diseases. Starting from a STAT6 ligand with Ki= 3.5 μM binding affinity, we obtained AK-068 with Ki= 6 nM to STAT6 and at least >85-fold binding selectivity over STAT5. Using AK-068 and cereblon ligands, we discovered AK-1690 as the first, potent and selective PROTAC STAT6 degrader. AK-1690 effectively induces degradation of STAT6 protein in cells with DC50values of as low as 1 nM while showing minimal effect on other STAT members up to 10 μM. A single dose of AK-1690 effectively depletes STAT6 in mouse tissues. Determination of the first cocrystal structure of STAT6 in complex with AK-1690 provides a structural basis for their interactions. AK-1690 is a powerful tool with which to investigate the roles of STAT6 in human diseases and biological processes and a promising lead compound for further optimization.
Published: 2024
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