淋巴特异性酪氨酸磷酸酶抑制剂的研究进展  

Progress of lymphoid-specific tyrosine phosphatase inhibitors

作　　者：朱鹏举[1] 侯旭奔[1] 方浩[1] 

机构地区：[1]山东大学药学院,药物化学研究所,山东济南250012

出　　处：《药学学报》2017年第5期699-705,共7页Acta Pharmaceutica Sinica

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)

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。Lymphoid-specific tyrosine phosphatase （LYP） is a phosphatase that is encoded by protein tyrosine phosphatase non-receptor type 22 and is mainly distributed in lymphoid. In psychological condition, LYP inhibits T-cell receptor （TCR） signaling in association with C-terminal kinase （CSK）. While in pathological condition, mutant LYP dissociates with CSK, which augments the inhibition of TCR signaling and leads to autoimmune diseases. Consequently, LYP is now considered as a new target of type I diabetes, rheumatic arthritis and Graves disease and some other autoimmune disorders. This review mainly focuses on the development of LYP inhibitors in their structures and activities.

关 键 词：淋巴特异性酪氨酸磷酸酶 自身免疫病 抑制剂 

分 类 号：R916[医药卫生—药学]