Article
Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model.
Scientific reports - 28 Mar 2017
Wu Hong, Huang Qiong, Qi Ziping, Chen Yongfei, Wang Aoli, Chen Cheng, Liang Qianmao, Wang Jinghua, Chen Wensheng, Dong Jin, Yu Kailin, Hu Chen, Wang Wenchao, Liu Xiaochuan, Deng Yuanxin, Wang Li, Wang Beilei, Li Xiaoxiang, Gray Nathanael S, Liu Jing, Wei Wei, Liu Qingsong
Abstract excerpt
BTK plays a critical role in the B cell receptor mediated inflammatory signaling in the rheumatoid arthritis (RA). Through a rational design approach we discovered a highly selective and potent BTK kinase inhibitor (CHMFL-BTK-11) which exerted its inhibitory efficacy through a covalent bond with BTK Cys481. CHMFL-BTK-11 potently blocked the anti-IgM stimulated BCR signaling in the Ramos cell lines and isolated...
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