WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors)(WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors)) - 药物靶点：GRIN3A x GluN1_在研适应症：神经系统疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

作用机制

GRIN3A antagonists(glutamate ionotropic receptor NMDA type subunit 3A antagonists)、GluN1抑制剂(glutamate ionotropic receptor NMDA type subunit 1 inhibitors)

治疗领域

神经系统疾病

在研适应症

神经系统疾病

非在研适应症-

原研机构

中国科学院上海药物研究所

在研机构

中国科学院上海药物研究所

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

结构

分子式C20H13FO6

InChIKeyFRSWCCBXIHFKKY-UHFFFAOYSA-N

CAS号1223397-11-2

关联

100 项与 WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors) 相关的临床结果

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100 项与 WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors) 相关的转化医学

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100 项与 WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors) 相关的专利（医药）

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1

项与 WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors) 相关的文献（医药）

Cell Communication and Signaling

GLUT1 promotes cell proliferation via binds and stabilizes phosphorylated EGFR in lung adenocarcinoma

Article

作者: Li, Yu ; Zhao, Huijie ; Xie, Zhangrong ; Zeng, Xiaofei ; Chen, Sijie ; Du, Yuhui ; Shi, Yuxuan ; Zhou, Zhiqing ; Liu, Yue ; Chen, Guoan ; Lin, Xiangyi

AbstractBackgroundWhile previous studies have primarily focused on Glucose transporter type 1 (GLUT1) related glucose metabolism signaling, we aim to discover if GLUT1 promotes tumor progression through a non-metabolic pathway.MethodsThe RNA-seq and microarray data were comprehensively analyzed to evaluate the significance of GLUT1 expression in lung adenocarcinoma (LUAD). The cell proliferation, colony formation, invasion, and migration were used to test GLUT1 ‘s oncogenic function. Co-immunoprecipitation and mass spectrum (MS) were used to uncover potential GLUT1 interacting proteins. RNA-seq, DIA-MS, western blot, and qRT-PCR to probe the change of gene and cell signaling pathways.ResultsWe found that GLUT1 is highly expressed in LUAD, and higher expression is related to poor patient survival. GLUT1 knockdown caused a decrease in cell proliferation, colony formation, migration, invasion, and induced apoptosis in LUAD cells. Mechanistically, GLUT1 directly interacted with phosphor-epidermal growth factor receptor (p-EGFR) and prevented EGFR protein degradation via ubiquitin-mediated proteolysis. The GLUT1 inhibitor WZB117 can increase the sensitivity of LUAD cells to EGFR-tyrosine kinase inhibitors (TKIs) Gefitinib.ConclusionsGLUT1 expression is higher in LUAD and plays an oncogenic role in lung cancer progression. Combining GLUT1 inhibitors and EGFR-TKIs could be a potential therapeutic option for LUAD treatment.

100 项与 WZB117(Inhibitor of GluN1/GluN3 NMDA Receptors) 相关的药物交易

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