淋巴特异性酪氨酸磷酸酶抑制剂的研究进展
发布时间：2018-10-21 09:38
【摘要】：淋巴特异性酪氨酸磷酸酶(lymphoid-specific tyrosine phosphatase,LYP)主要分布于淋巴系统,是由PTPn22基因编码的非受体蛋白酪氨酸磷酸酶。正常生理条件下,该酶与CSK结合后,可抑制T细胞受体信号传导并维持免疫系统自身稳定。病理条件下,该酶会发生突变而无法正常结合CSK,导致其功能亢进并诱发各种免疫疾病。因此淋巴特异性酪氨酸磷酸酶也被认为是治疗I型糖尿病、风湿性关节炎以及格雷夫斯病等自身免疫疾病的新型靶标。本文将综述其研究进展,并总结已报道的抑制剂的结构类型及活性。
[Abstract]:Lymphoid specific tyrosine phosphatase (lymphoid-specific tyrosine phosphatase,LYP), mainly distributed in the lymphatic system, is a non-receptor protein tyrosine phosphatase encoded by PTPn22 gene. Under normal physiological conditions, the enzyme could inhibit the signal transduction of T cell receptor and maintain the autostability of immune system after binding with CSK. Under pathological conditions, the enzyme mutates and fails to bind to CSK, normally, which leads to hyperfunction and induces various immune diseases. Therefore, lymphoid-specific tyrosine phosphatase is also considered as a new target for autoimmune diseases such as type I diabetes, rheumatoid arthritis and Graves disease. This paper will review the progress of its research, and summarize the structural types and activities of the reported inhibitors.
【作者单位】： 山东大学药学院药物化学研究所;
【基金】：山东省自然科学基金杰出青年基金资助项目(JQ201319) 山东大学自主创新基金资助项目(2016JC018)
【分类号】：R976
本文编号：2284715
[Abstract]:Lymphoid specific tyrosine phosphatase (lymphoid-specific tyrosine phosphatase,LYP), mainly distributed in the lymphatic system, is a non-receptor protein tyrosine phosphatase encoded by PTPn22 gene. Under normal physiological conditions, the enzyme could inhibit the signal transduction of T cell receptor and maintain the autostability of immune system after binding with CSK. Under pathological conditions, the enzyme mutates and fails to bind to CSK, normally, which leads to hyperfunction and induces various immune diseases. Therefore, lymphoid-specific tyrosine phosphatase is also considered as a new target for autoimmune diseases such as type I diabetes, rheumatoid arthritis and Graves disease. This paper will review the progress of its research, and summarize the structural types and activities of the reported inhibitors.
【作者单位】： 山东大学药学院药物化学研究所;
【基金】：山东省自然科学基金杰出青年基金资助项目(JQ201319) 山东大学自主创新基金资助项目(2016JC018)
【分类号】：R976
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