Recently, Liu Qingsong and Liu Jing, researchers of the Strong Magnetic Field Science Center of the Chinese Academy of Sciences, collaborated with Wei Wei, a professor at Anhui Medical University, to develop a new type of BTK kinase inhibitor CHMFL-BTK-11 for the treatment of rheumatoid arthritis. Related research results are published in the journal Scientific Reports.
Liu Qingsong told reporters that rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by persistent damage to the joints and other tissues of the immune system, which can cause irreversible joint damage, deformity, and even disability. Among them, the incidence of rheumatoid arthritis in China is 0.28%.
Liu Qingsong said: "With the deep understanding of the key mechanisms of action of various kinases in immune activation and inflammatory signaling pathways, selective kinase inhibitors have become a new strategy for the treatment of rheumatoid arthritis."
Bruton's tyrosine kinase (BTK) is a non-receptor tyrosine kinase that plays an extremely important role in the B cell receptor signaling pathway. The B cells here are an important immune cell that affects the development of many immune diseases. "Because of the immune activation of B cell sustained activation can lead to rheumatoid arthritis, BTK kinase is considered to be an effective drug target for the treatment of rheumatoid arthritis." Liu Jing said.
This study found a novel BTK kinase irreversible inhibitor CHMFL-BTK-11, which can effectively inhibit the excessive activation of human primary B cells and the secretion of inflammatory factor TNFα in peripheral blood mononuclear cells. In the mouse arthritis model, CHMFL-BTK-11 can effectively suppress the immune response by blocking the proliferation of over-activated B cells, reduce the production of inflammatory factors IgG1, IgG2, IgM, IL-6, and stimulate anti-inflammatory factors. Secretion of IL-10. Liu Qingsong pointed out: "The high activity and high selectivity of CHMFL-BTK-11 make it a potential new drug for the treatment of rheumatoid arthritis."
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