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靶向 Syk:脾酪氨酸激酶作为治疗靶点。

Getting Syk: spleen tyrosine kinase as a therapeutic target.

机构信息

Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, Hansen Life Sciences Research Building, 210 South University Street, West Lafayette, IN 47907, USA.

出版信息

Trends Pharmacol Sci. 2014 Aug;35(8):414-22. doi: 10.1016/j.tips.2014.05.007. Epub 2014 Jun 26.

Abstract

Spleen tyrosine kinase (Syk) is a cytoplasmic protein tyrosine kinase well known for its ability to couple immune cell receptors to intracellular signaling pathways that regulate cellular responses to extracellular antigens and antigen-immunoglobulin (Ig) complexes of particular importance to the initiation of inflammatory responses. Thus, Syk is an attractive target for therapeutic kinase inhibitors designed to ameliorate the symptoms and consequences of acute and chronic inflammation. Its more recently recognized role as a promoter of cell survival in numerous cancer cell types ranging from leukemia to retinoblastoma has attracted considerable interest as a target for a new generation of anticancer drugs. This review discusses the biological processes in which Syk participates that have made this kinase such a compelling drug target.

摘要

脾酪氨酸激酶(Syk)是一种细胞质蛋白酪氨酸激酶,以其能够将免疫细胞受体与细胞内信号通路偶联的能力而闻名,这些信号通路调节细胞对外源抗原和抗原-免疫球蛋白(Ig)复合物的反应,这对于启动炎症反应尤为重要。因此,Syk 是治疗性激酶抑制剂的一个有吸引力的靶点,旨在改善急性和慢性炎症的症状和后果。其最近被认为在从白血病到视网膜母细胞瘤的多种癌细胞类型中作为促进细胞存活的促进因子,这使其成为新一代抗癌药物的一个有吸引力的靶点。本文综述了 Syk 参与的生物学过程,这些过程使这种激酶成为一个引人注目的药物靶点。

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