Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities
文献类型：期刊论文
| 作者 | Zhang, Yi-Nan2; Zhang, Wei1; Hong, Di2; Shi, Lei1; Shen, Qiang1; Li, Jing-Ya1 ; Li, Jia1; Hu, Li-Hong2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2008-09-15 |
| 卷号 | 16期号:18页码:8697-8705 |
| 关键词 | protein tyrosine phosphatase 1B oleanolic acid inhibitor SAR (structure-activity relationship) |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2008.07.080 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B is a key factor in the negative regulation of insulin pathway and a promising target for treatment of diabetes and obesity. Herein, a series of competitive inhibitors were optimized from oleanolic acid, a natural triterpenoid identified against PTP1B by screening libraries of traditional Chinese medicinal herbs. Modifying at 3 and 28 positions, we obtained compound 13 with a K(i) of 130 nM, which exhibited good selectivity between other phosphatases involved in insulin pathway except T-cell protein tyrosine phosphatase. Further evaluation in cell models illustrated that the derivatives enhanced insulin receptor phosphorylation in CHO/hIR cells and also stimulated glucose uptake in L6 myotubes with or addition of without insulin. (C) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | INSULIN-RECEPTOR PHOSPHORYLATION ; ISOPRENYLATED FLAVONOIDS ; PTP1B INHIBITORS ; ARDISIA-JAPONICA ; GLUCOSE-UPTAKE ; BINDING-SITE ; MICE ; SENSITIVITY ; DISCOVERY ; ERYTHRINA |
| 资助项目 | Chinese National Natural Science Foundation of China[30572241] ; Chinese National Natural Science Foundation of China[30623008] ; Shanghai Science and Technology Commission[04QMH1409] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000259173400043 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272810]  |
| 专题 | 国家新药筛选中心 上海中药现代化研究中心 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Yi-Nan,Zhang, Wei,Hong, Di,et al. Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(18):8697-8705. |
| APA | Zhang, Yi-Nan.,Zhang, Wei.,Hong, Di.,Shi, Lei.,Shen, Qiang.,...&Hu, Li-Hong.(2008).Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities.BIOORGANIC & MEDICINAL CHEMISTRY,16(18),8697-8705. |
| MLA | Zhang, Yi-Nan,et al."Oleanolic acid and its derivatives: New inhibitor of protein tyrosine phosphatase 1B with cellular activities".BIOORGANIC & MEDICINAL CHEMISTRY 16.18(2008):8697-8705. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。