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

doi:10.1021/acs.jmedchem.4c00027

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Article

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

Journal of medicinal chemistry - 23 May 2024

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

Abstract excerpt

The approval of venetoclax, a B-cell lymphoma-2 (Bcl-2) selective inhibitor, for the treatment of chronic lymphocytic leukemia demonstrated that the antiapoptotic protein Bcl-2 is a druggable target for B-cell malignancies. However, venetoclax's limited potency cannot produce a strong, durable clinical benefit in other Bcl-2-mediated malignancies (e.g., diffuse large B-cell lymphomas) and multiple recurrent Bcl-2...

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PMID: 38695063
DOI: 10.1021/acs.jmedchem.4c00027
PMCID: PMC11129194

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Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.PMID 38695063Read ↗

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