Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors
文献类型：期刊论文
| 作者 | Liu, Qiufeng2,3; Chen, Xinde1; Chen, Wuyan2; Yuan, Xiaojing2; Su, Haixia2; Shen, Jianhua1 ; Xu, Yechun2
|
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016-05-26 |
| 卷号 | 59期号:10页码:5115-5120 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.6b00282 |
| 文献子类 | Article |
| 英文摘要 | Lipoprotein-associated phospholipase A2 (Lp-PLA2) represents a promising therapeutic target for atherosclerosis and Alzheimer's disease. Here we reported the first crystal structures of Lp-PLA2 bound with reversible inhibitors and the thermodynamic characterization of complexes. High rigidity of Lp-PLA2 structure and similar binding modes of inhibitors with completely different scaffolds are revealed. It not only provides the molecular basis for inhibitory activity but also sheds light on the essential features of Lp-PLA2 recognition with reversible inhibitors. |
| WOS关键词 | ACTIVATING-FACTOR-ACETYLHYDROLASE ; DIABETIC MACULAR EDEMA ; LP-PLA(2) INHIBITORS ; A(2) ; DARAPLADIB ; POTENT ; DERIVATIVES ; DISCOVERY ; SYSTEM ; SERIES |
| 资助项目 | CAS-Novo Nordisk[00000000] ; National Natural Science Foundation of China[81422047] ; National Natural Science Foundation of China[81402850] ; National Natural Science Foundation of China[81502987] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000376840600055 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276035]  |
| 专题 | 药物发现与设计中心 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 | Xu, Yechun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 3.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Qiufeng,Chen, Xinde,Chen, Wuyan,et al. Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2016,59(10):5115-5120. |
| APA | Liu, Qiufeng.,Chen, Xinde.,Chen, Wuyan.,Yuan, Xiaojing.,Su, Haixia.,...&Xu, Yechun.(2016).Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,59(10),5115-5120. |
| MLA | Liu, Qiufeng,et al."Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 59.10(2016):5115-5120. |
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。