Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design
文献类型：期刊论文
| 作者 | Du, Yongli2; Ling, Hao2; Zhang, Meng1; Shen, Jingkang3; Li, Qunyi4 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-08-01 |
| 卷号 | 23期号:15页码:4891-4898 |
| 关键词 | Protein tyrosine phosphatase 1B inhibitor N-(2,5-Diethoxy-phenyl)-methanesulfonamide Type 2 diabetes mellitus Insulin signaling |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.05.032 |
| 文献子类 | Article |
| 英文摘要 | Fragment-docking-oriented de novel design for both the catalytic site and the C phosphotyrosine binding site led to the discovery of novel scaffold and chemical easy N-(2,5-diethoxy-phenyl)-methanesulfonamide based phosphotyrosine mimetics that when incorporated into ureas are high potent and selective inhibitors of protein tyrosine phosphatase 1B. Among them, compound 15 was shown to be the most potent PTP1B inhibitor with great selectivity over the highly homologous T-cell protein tyrosine phosphatase. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; PHOSPHOTYROSINE BINDING-SITE ; PROTEIN ; GLUCOSE ; OBESITY ; PROTEIN-TYROSINE-PHOSPHATASE-1B ; IDENTIFICATION ; STRATEGY ; RECEPTOR ; ACIDS |
| 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:000358440000081 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276455]  |
| 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.Brunswick Labs China, Suzhou 215021, 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; 4.Fudan Univ, Huashan Hosp, Clin Pharm Lab, Shanghai 200040, Peoples R China |
| 推荐引用方式 GB/T 7714 | Du, Yongli,Ling, Hao,Zhang, Meng,et al. Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(15):4891-4898. |
| APA | Du, Yongli,Ling, Hao,Zhang, Meng,Shen, Jingkang,&Li, Qunyi.(2015).Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design.BIOORGANIC & MEDICINAL CHEMISTRY,23(15),4891-4898. |
| MLA | Du, Yongli,et al."Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design".BIOORGANIC & MEDICINAL CHEMISTRY 23.15(2015):4891-4898. |
入库方式： OAI收割
来源：上海药物研究所
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