RDN-009(RDN-009) - 药物靶点：ZAP70_在研适应症：银屑病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

ZAP70

作用机制

ZAP70 inhibitors(Zap70 tyrosine kinase inhibitors)

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病

在研适应症

银屑病

非在研适应症-

原研机构

中国科学院

在研机构

中国科学院大学

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)药物发现

特殊审评-

结构

分子式C24H24ClN7O4

InChIKeyLRSSMJXTQUVHEA-UHFFFAOYSA-N

CAS号2839429-24-0

关联

100 项与 RDN-009 相关的临床结果

登录后查看更多信息

100 项与 RDN-009 相关的转化医学

登录后查看更多信息

100 项与 RDN-009 相关的专利（医药）

登录后查看更多信息

1

项与 RDN-009 相关的文献（医药）

2021-07-01·European Journal of Medicinal Chemistry1区 · 医学

Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor

1区 · 医学

Article

作者: Sun, Yaoliang ; Ren, Xuelian ; Xu, Shilin ; Li, Heng ; Huang, He ; Rao, Danni ; Zheng, Mingyue ; Wen, Cuiyun ; Tang, Wei

ZAP-70 (zeta-chain associated protein kinase 70 kDa) signaling pathway and its functions have been involved in the development and adaptive immune signaling of T cell. It thus represents a promising target for autoimmune diseases. Although reversible ZAP-70 kinase domain inhibitors have been developed, they are either weak or nonselective. We report herein the structure-guided development of the first potent and covalent inhibitor of ZAP-70 kinase domain. In particular, compound 18 (RDN009) showed good selectivity for ZAP-70 over structurally related Syk, and displayed potent inhibitory effects on T cell proliferation, activation, and inflammatory cytokine production. A mass spectrometry analysis further confirmed the covalent linkage between the inhibitor and ZAP-70 protein at C346. Overall, the covalent inhibitor RDN009 represents a potent and selective probe of ZAP-70 for further development for treatment of autoimmune diseases.

100 项与 RDN-009 相关的药物交易

登录后查看更多信息