Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic
文献类型：期刊论文
| 作者 | Liu, Peihong2; Du, Yongli2; Song, Lianhua2; Shen, Jingkang3; Li, Qunyi1 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-11-01 |
| 卷号 | 23期号:21页码:7079-7088 |
| 关键词 | Type 2 diabetes mellitus PTP1B Inhibitor Structure-activity relationships |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.09.024 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) which plays an important role in the negative regulation of insulin and leptin pathway has emerged as a novel promising therapeutic target for the treatment of type 2 diabetes mellitus and obesity. Upon careful study, a series of novel scaffold and simple synthesis method inhibitors were discovered based on the analysis of X-ray crystal structures of PTP1B/inhibitor complexes and docking simulations. Among them, compound P7 exhibited high inhibitory activity (IC50 = 222 nM) with moderate selectivity (8-fold) over T-cell PTPase (TCPTP) through interacting with the A, B and C binding sites of PTP1B enzyme. Further studies on cellular activities revealed that compound P7 could enhance insulin-mediated in phosphorylation and insulin-stimulated glucose uptake. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PROTEIN-TYROSINE-PHOSPHATASE ; 1B INHIBITORS ; INSULIN SENSITIVITY ; GLUCOSE-UPTAKE ; MICE ; DISCOVERY ; OBESITY ; RECEPTOR ; DERIVATIVES ; INSIGHTS |
| 资助项目 | National Natural Science Foundation of China[81202389] ; National Natural Science Foundation of China[81302853] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000364437400031 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276344]  |
| 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 |
| 作者单位 | 1.Fudan Univ, Huashan Hosp, Clin Pharm Lab, Shanghai 200040, Peoples R China 2.Qilu Univ Technol, Sch Chem & Pharmaceut Engn, Jinan 250353, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Liu, Peihong,Du, Yongli,Song, Lianhua,et al. Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(21):7079-7088. |
| APA | Liu, Peihong,Du, Yongli,Song, Lianhua,Shen, Jingkang,&Li, Qunyi.(2015).Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic.BIOORGANIC & MEDICINAL CHEMISTRY,23(21),7079-7088. |
| MLA | Liu, Peihong,et al."Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic".BIOORGANIC & MEDICINAL CHEMISTRY 23.21(2015):7079-7088. |
入库方式： OAI收割
来源：上海药物研究所
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