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布鲁顿酪氨酸激酶作为药物研发靶点

Bruton's tyrosine kinase as a drug discovery target.

作者信息

Pan Zhengying

机构信息

Alpharetta, Georgia, USA.

出版信息

Drug News Perspect. 2008 Sep;21(7):357-62. doi: 10.1358/dnp.2008.21.7.1255308.

Abstract

Bruton's tyrosine kinase (Btk) is an important mediator in multiple signal transduction pathways. Fifteen years of research have revealed a complex role for Btk in hematopoietic cells. These studies suggest that Btk may be a promising target for therapeutic intervention for several complicated diseases. Inhibitors targeting the Btk kinase domain have been developed and show clear beneficial effects in animal models of rheumatoid arthritis, lymphoma and other diseases. Here, an overview of these studies is presented with an emphasis on results stemming from medicinal chemistry research.

摘要

布鲁顿酪氨酸激酶(Btk)是多种信号转导途径中的重要介质。十五年的研究揭示了Btk在造血细胞中的复杂作用。这些研究表明,Btk可能是几种复杂疾病治疗干预的一个有前景的靶点。针对Btk激酶结构域的抑制剂已被开发出来,并在类风湿性关节炎、淋巴瘤和其他疾病的动物模型中显示出明显的有益效果。在此,对这些研究进行综述,重点介绍药物化学研究的结果。

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