摘要
类风湿性关节炎(RA)是一种慢性自身免疫性疾病,并且成为残疾和劳动力丧失的主要原因之一。 大多数RA患者(主要是ACPA和RF)产生的异常B细胞和自身抗体的存在表明B细胞的功能参与RA疾病的发展。 因此,靶向B细胞的药物已成为RA治疗的热点。 研究表明,Bruton酪氨酸激酶(BTK)参与B细胞增殖和激活过程的调节。 一些小分子BTK抑制剂在生物活性分析和动物模型中显示出优异的抑制作用。 因此,本综述将简要介绍BTK及其在细胞信号传导中的作用,并概述用于RA治疗的BTK抑制剂的最新进展。
关键词: BTK抑制剂,RA,B细胞,活性,抗炎,结构。
Current Medicinal Chemistry
Title:Development of Bruton’s Tyrosine Kinase Inhibitors for Rheumatoid Arthritis
Volume: 25 Issue: 42
关键词: BTK抑制剂,RA,B细胞,活性,抗炎,结构。
摘要: Rheumatoid Arthritis (RA) is a chronic autoimmune disease and becomes one of the major causes of disability and work force loss. The presence of abnormal B cell and autoantibodies produced by most RA patients, primarily ACPA and RF, indicate that the function of B cell was involved in the development of RA disease. Accordingly, the drug targeting B cell has become a hot spot in the treatment of RA. Studies have shown that Bruton's tyrosine kinase (BTK) is involved in the regulation of B cell proliferation and activation process. Some small molecule BTK inhibitors have shown excellent inhibition in biological activity analysis and animal models. Therefore, this review will briefly introduce BTK and its role in cell signaling and overview recent progress of BTK inhibitors for RA treatment.
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Cite this article as:
Development of Bruton’s Tyrosine Kinase Inhibitors for Rheumatoid Arthritis, Current Medicinal Chemistry 2018; 25 (42) . https://dx.doi.org/10.2174/0929867325666180316121951
DOI https://dx.doi.org/10.2174/0929867325666180316121951 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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