Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity
文献类型：期刊论文
| 作者 | Liu, Peihong2; Du, Yongli2; Song, Lianhua2; Shen, Jingkang1; Li, Qunyi3 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016-08-08 |
| 卷号 | 118页码:27-33 |
| 关键词 | Type 2 diabetes mellitus Methyl salicylate derivatives ABC type PTP1B inhibitor |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2016.04.014 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) as a key negative regulator of both insulin and leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus (T2DM) and obesity. With the goal of enhancing potency and selectivity of the PTP1B inhibitors, a series of methyl salicylate derivatives as ABC type PTP1B inhibitors (P1-P7) were discovered. More importantly, compound P6 exhibited high potent inhibitory activity (IC50 = 50 nM) for PTP1B with 15-fold selectivity over T-cell PTPase (TCPTP). Further studies on cellular activities revealed that compound P6 could enhance insulin-mediated insulin receptor beta (IR beta) phosphorylation and insulin-stimulated glucose uptake. (C) 2016 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | PROTEIN-TYROSINE-PHOSPHATASE ; INSULIN SENSITIVITY ; GLUCOSE-UPTAKE ; 1B INHIBITOR ; MICE ; RECEPTOR ; OBESITY ; ACID ; DERIVATIVES ; CELLS |
| 资助项目 | National Natural Science Foundation of China[81202389] ; National Natural Science Foundation of China[81302853] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000377312400004 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275929]  |
| 专题 | 药物化学研究室 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 |
| 通讯作者 | Du, Yongli; Li, Qunyi |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 2.Qilu Univ Technol, Sch Chem & Pharmaceut Engn, 3501 Daxue Rd, Jinan 250353, Peoples R China; 3.Fudan Univ, Huashan Hosp, Clin Pharm Lab, 12 Wu Lu Mu Qi M Rd, Shanghai 200040, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Peihong,Du, Yongli,Song, Lianhua,et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,118:27-33. |
| APA | Liu, Peihong,Du, Yongli,Song, Lianhua,Shen, Jingkang,&Li, Qunyi.(2016).Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,118,27-33. |
| MLA | Liu, Peihong,et al."Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 118(2016):27-33. |
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。