Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake

doi:10.1016/j.bbagen.2006.05.009

	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; Hu, Li-hong ; Li, Jia
刊名	BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
	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.