Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake | |
Zhang, Wei; Hong, Di; Zhou, Yueyang; Zhang, Yinan; Shen, Qiang; Li, Jing-ya![]() ![]() | |
刊名 | BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
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2006-10 | |
卷号 | 1760期号:10页码:1505-1512 |
关键词 | PTP1B inhibitor ursolic acid traditional Chinese medicinal herb derivative competitive insulin receptor glucose uptake |
ISSN号 | 0304-4165 |
DOI | 10.1016/j.bbagen.2006.05.009 |
文献子类 | Article |
英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) is a key element in the negative regulation of the insulin signaling pathway and may play an important role in diabetes and obesity. We identified ursolic acid, a natural pentacyclic triterpenoid that occurs widely in traditional Chinese medicinal herbs, as an inhibitor of PTP1B by screening an extract library of the traditional Chinese medicinal herbs used a diabetes clinic. By modifying urosolic acid, we designed and synthesized a derivative with a K-i of 283 nM. As competitive inhibitors of PTP1B, ursolic acid and its derivative also inhibit T-cell protein tyrosine phosphatase and src homology phosphatase-2 but not leucocyte antigen-related phosphatase or protein tyrosine phosphatase alpha and epsilon, which are all possibly involved in the insulin pathway. The ursolic acid derivative enhanced insulin receptor phosphorylation in CHO/hIR cells and stimulate glucose uptake in L6 myotubes. (c) 2006 Elsevier B.V. All rights reserved. |
WOS关键词 | ANTIGEN-RELATED PHOSPHATASE ; FAO HEPATOMA-CELLS ; SIGNAL-TRANSDUCTION ; MODULATION ; MACROPHAGES ; SENSITIVITY ; ACTIVATION ; EXPRESSION ; OBESITY ; TISSUE |
WOS研究方向 | Biochemistry & Molecular Biology ; Biophysics |
语种 | 英语 |
出版者 | ELSEVIER SCIENCE BV |
WOS记录号 | WOS:000241589800005 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/273475] ![]() |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Hu, Li-hong |
作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Zhang, Wei,Hong, Di,Zhou, Yueyang,et al. Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake[J]. BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS,2006,1760(10):1505-1512. |
APA | Zhang, Wei.,Hong, Di.,Zhou, Yueyang.,Zhang, Yinan.,Shen, Qiang.,...&Li, Jia.(2006).Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake.BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS,1760(10),1505-1512. |
MLA | Zhang, Wei,et al."Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake".BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS 1760.10(2006):1505-1512. |
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