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Your search keyword '"Chen, Shuaishuai"' showing total 4 results
Start Over Author "Chen, Shuaishuai" Journal journal of medicinal chemistry
4 results on '"Chen, Shuaishuai"'

1. Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2

Author

Guo, Yunhang, primary, Xue, Hai, additional, Hu, Nan, additional, Liu, Ye, additional, Sun, Hanzi, additional, Yu, Desheng, additional, Qin, Ling, additional, Shi, Gongyin, additional, Wang, Fan, additional, Xin, Lei, additional, Sun, Weihua, additional, Zhang, Fan, additional, Song, Xiaomin, additional, Li, Shuran, additional, Wei, Qiang, additional, Guo, Ying, additional, Li, Yong, additional, Liu, Xiaoxin, additional, Chen, Shuaishuai, additional, Zhang, Taichang, additional, Wu, Yue, additional, Su, Dan, additional, Zhu, Yutong, additional, Xu, Aiying, additional, Xu, Haipeng, additional, Yang, Shasha, additional, Zheng, Zhijun, additional, Liu, Junhua, additional, Yang, Xuefei, additional, Yuan, Xi, additional, Hong, Yuan, additional, Sun, Xuebing, additional, Guo, Yin, additional, Zhou, Changyou, additional, Liu, Xuesong, additional, Wang, Lai, additional, and Wang, Zhiwei, additional

Published
2024
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2. Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases

Author

Guo, Yunhang, primary, Hu, Nan, additional, Liu, Ye, additional, Zhang, Wei, additional, Yu, Desheng, additional, Shi, Gongyin, additional, Zhang, Bo, additional, Yin, Longbo, additional, Wei, Min, additional, Yuan, Xi, additional, Luo, Lusong, additional, Wang, Fan, additional, Song, Xiaomin, additional, Xin, Lei, additional, Wei, Qiang, additional, Li, Yong, additional, Guo, Ying, additional, Chen, Shuaishuai, additional, Zhang, Taichang, additional, Zhang, Shuo, additional, Zhou, Xing, additional, Zhang, Cuining, additional, Su, Dan, additional, Liu, Junhua, additional, Cheng, Zhenzhen, additional, Zhang, Jiye, additional, Xing, Haimei, additional, Sun, Hanzi, additional, Li, Xin, additional, Zhao, Yuan, additional, He, Min, additional, Wu, Yue, additional, Guo, Yin, additional, Sun, Xuebing, additional, Tian, Alice, additional, Zhou, Changyou, additional, Young, Steve, additional, Liu, Xuesong, additional, Wang, Lai, additional, and Wang, Zhiwei, additional

Published
2023
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3. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

Author

Guo, Yunhang, primary, Liu, Ye, additional, Hu, Nan, additional, Yu, Desheng, additional, Zhou, Changyou, additional, Shi, Gongyin, additional, Zhang, Bo, additional, Wei, Min, additional, Liu, Junhua, additional, Luo, Lusong, additional, Tang, Zhiyu, additional, Song, Huipeng, additional, Guo, Yin, additional, Liu, Xuesong, additional, Su, Dan, additional, Zhang, Shuo, additional, Song, Xiaomin, additional, Zhou, Xing, additional, Hong, Yuan, additional, Chen, Shuaishuai, additional, Cheng, Zhenzhen, additional, Young, Steve, additional, Wei, Qiang, additional, Wang, Haisheng, additional, Wang, Qiuwen, additional, Lv, Lei, additional, Wang, Fan, additional, Xu, Haipeng, additional, Sun, Hanzi, additional, Xing, Haimei, additional, Li, Na, additional, Zhang, Wei, additional, Wang, Zhongbo, additional, Liu, Guodong, additional, Sun, Zhijian, additional, Zhou, Dongping, additional, Li, Wei, additional, Liu, Libin, additional, Wang, Lai, additional, and Wang, Zhiwei, additional

Published
2019
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4. Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

Author

Guo, Yunhang, Liu, Ye, Hu, Nan, Yu, Desheng, Zhou, Changyou, Shi, Gongyin, Zhang, Bo, Wei, Min, Liu, Junhua, Luo, Lusong, Tang, Zhiyu, Song, Huipeng, Guo, Yin, Liu, Xuesong, Su, Dan, Zhang, Shuo, Song, Xiaomin, Zhou, Xing, Hong, Yuan, Chen, Shuaishuai, Cheng, Zhenzhen, Young, Steve, Wei, Qiang, Wang, Haisheng, Wang, Qiuwen, Lv, Lei, Wang, Fan, Xu, Haipeng, Sun, Hanzi, Xing, Haimei, Li, Na, Zhang, Wei, Wang, Zhongbo, Liu, Guodong, Sun, Zhijian, Zhou, Dongping, Li, Wei, Liu, Libin, Wang, Lai, and Wang, Zhiwei

Abstract

Aberrant activation of Bruton’s tyrosine kinase (BTK) plays an important role in pathogenesis of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of hematological malignancies. The discovery of a more selective on-target covalent BTK inhibitor is of high value. Herein, we disclose the discovery and preclinical characterization of a potent, selective, and irreversible BTK inhibitor as our clinical candidate by using in vitro potency, selectivity, pharmacokinetics (PK), and in vivo pharmacodynamic for prioritizing compounds. Compound BGB-3111(31a, Zanubrutinib) demonstrates (i) potent activity against BTK and excellent selectivity over other TEC, EGFR and Src family kinases, (ii) desirable ADME, excellent in vivo pharmacodynamic in mice and efficacy in OCI-LY10 xenograft models.

Published
2024
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