Staurosporine as an agonist for induction of GLUT4 translocation, identified by a pH-sensitive fluorescent IRAP-mOrange2 probe
文献类型:期刊论文
作者 | Li, Yufeng1,2; Zheng, Li2; Wang, Dan2; Zhang, Xiang2; Li, Jia3![]() |
刊名 | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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出版日期 | 2016-11-25 |
卷号 | 480期号:4页码:534-538 |
关键词 | Diabetes pH-sensitive fluorescent probe GLUT4 translocation Staurosporine Insulin additive analogue |
ISSN号 | 0006-291X |
DOI | 10.1016/j.bbrc.2016.10.056 |
文献子类 | Article |
英文摘要 | Insulin-stimulated GLUT4 translocation from GLUT4 storage vesicles (GSVs) to the plasma membrane (PM) constitutes a key process for blood glucose control. Therefore, compounds that could promote GLUT4 translocation into the PM represent potential drugs for the treatment of diabetes. In this research, we screened for agonists that induce GLUT4 translocation by using a novel pH-sensitive fluorescent probe, insulin-regulated aminopeptidase (IRAP)-mOrange2. We identified as well as validated one agonist, staurosporine, from a 64,000 compound library. Staurosporine promotes GSVs translocation into the PM and increases glucose uptake through the AMP-activated protein kinase (AMPK) pathway, serving as an effective insulin additive analogue in L6 cells. Our work highlights the convenience and efficiency of this novel pH-sensitive fluorescent probe and reveals the new biological activity of staurosporine as an agonist for GLUT4 translocation and as an effective insulin additive analogue. (C) 2016 Elsevier Inc. All rights reserved. |
WOS关键词 | ACTIVATED PROTEIN-KINASE ; TYPE-2 DIABETES-MELLITUS ; RAT SKELETAL-MUSCLE ; INSULIN-RESISTANCE ; INHIBITOR SELECTIVITY ; METABOLIC SYNDROME ; COMPLEX-I ; CELLS ; MECHANISM ; TARGETS |
资助项目 | National Natural Science Foundation of China[81102456] ; National Natural Science Foundation of China[81373422] ; National Natural Science Foundation of China[30801416] ; National Natural Science Foundation of China[31300701] ; Knowledge Innovation Project of the Chinese Academy of Sciences[KSCX1-YW-02] ; National Key Laboratory of Biomacromolecules[00000000] |
WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
语种 | 英语 |
WOS记录号 | WOS:000389015400006 |
出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
源URL | [http://119.78.100.183/handle/2S10ELR8/275796] ![]() |
专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
通讯作者 | Zong, Hao; Xu, Xiaolan |
作者单位 | 1.Sichuan Normal Univ, Coll Life Sci, Chengdu 610101, Peoples R China; 2.Chinese Acad Sci, Inst Biophys, Natl Key Lab Biomacromol, Beijing 100101, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Drug Screening Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Li, Yufeng,Zheng, Li,Wang, Dan,et al. Staurosporine as an agonist for induction of GLUT4 translocation, identified by a pH-sensitive fluorescent IRAP-mOrange2 probe[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2016,480(4):534-538. |
APA | Li, Yufeng.,Zheng, Li.,Wang, Dan.,Zhang, Xiang.,Li, Jia.,...&Xu, Xiaolan.(2016).Staurosporine as an agonist for induction of GLUT4 translocation, identified by a pH-sensitive fluorescent IRAP-mOrange2 probe.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,480(4),534-538. |
MLA | Li, Yufeng,et al."Staurosporine as an agonist for induction of GLUT4 translocation, identified by a pH-sensitive fluorescent IRAP-mOrange2 probe".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 480.4(2016):534-538. |
入库方式: OAI收割
来源:上海药物研究所
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