Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site
文献类型：期刊论文
| 作者 | Du, Yongli1; Zhang, Yanhui1; Ling, Hao1; Li, Qunyi2; Shen, Jingkang3 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2018-01-20 |
| 卷号 | 144页码:692-700 |
| 关键词 | Protein tyrosine phosphatase 1B inhibitors N-(2,5-diethoxy-phenyl)-methane sulfonamide Type 2 diabetes mellitus PTP1B |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2017.12.064 |
| 文献子类 | Article |
| 英文摘要 | PTP1B serving as a key negative regulator of insulin signaling is a novel target for type 2 diabetes and obesity. Modification at ring B of N-(4-[(3-Phenyl-ureido)-methyl]-phenyl)-methane-sulfonamide template to interact with residues Arg47 and Lys41 in the C site of PTP1B by molecular docking aided design resulted in the discovery of a series of novel high potent and selective inhibitors of PTP1B. The structure activity relationship interacting with the C site of PTP1B was well illustrated. Compounds 8 and 18 were shown to be the high potent and most promising PTP1B inhibitors with cellular activity and great selectivity over the highly homologous TCPTP and other PTPs. (C) 2017 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; STRUCTURE-BASED DESIGN ; RECEPTOR ; OBESITY ; ACIDS |
| 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:000425198100052 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279951]  |
| 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.Qilu Univ Technol, Shandong Acad Sci, Sch Chem & Pharmaceut Engn, 3501 Daxue Rd, Jinan 250353, Shandong, Peoples R China; 2.Fudan Univ, Huashan Hosp, Clin Pharm Lab, 12 Wu Lu Mu Qi M Rd, Shanghai 200040, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Du, Yongli,Zhang, Yanhui,Ling, Hao,et al. Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,144:692-700. |
| APA | Du, Yongli,Zhang, Yanhui,Ling, Hao,Li, Qunyi,&Shen, Jingkang.(2018).Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,144,692-700. |
| MLA | Du, Yongli,et al."Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 144(2018):692-700. |
入库方式： OAI收割
来源：上海药物研究所
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