Structure-Based Discovery of PDEs Inhibitors
文献类型：期刊论文
| 作者 | Li, Li; Chen, Wuyan; Chen, Tiantian; Ren, Jing; Xu, Yechun
|
| 刊名 | CURRENT TOPICS IN MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016 |
| 卷号 | 16期号:9页码:917-933 |
| 关键词 | Crystal structure Cyclic nucleotide signalling pathway Family-selective inhibitor Medicinal chemistry Phosphodiesterases Structure-based drug design |
| ISSN号 | 1568-0266 |
| DOI | 10.2174/1568026615666150825142134 |
| 文献子类 | Review |
| 英文摘要 | Phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and cGMP, thereby regulating the cyclic nucleotide signalling pathways and biological responses. PDEs inhibitors can be used clinically for treatment of several diseases including central nervous system disorders, erectile dysfunction, pulmonary hypertension, acute refractory cardiac failure, and inflammatory diseases such as chronic obstructive pulmonary disease. However, the unfavourable risk-benefit ratio and side-effect profiles of non-selective PDEs inhibitors have impeded their therapeutic success and therefore spurred the pharmaceutical industry to develop family-selective PDE inhibitors. Given the recent remarkable advances in structure-based drug design, this review will summarize developments and achievements in structure-based search, design and optimization of PDEs inhibitors, and highlight the challenges that need to be addressed. |
| WOS关键词 | PHOSPHODIESTERASE 10A PDE10A ; STRUCTURE-BASED DESIGN ; SELECTIVE INHIBITORS ; IN-VIVO ; BIOLOGICAL EVALUATION ; CRYSTAL-STRUCTURE ; BENZIMIDAZOLE DERIVATIVES ; ERECTILE DYSFUNCTION ; ATOPIC-DERMATITIS ; TOPICAL TREATMENT |
| 资助项目 | CAS-NovoNordisk Great Wall Professorship[00000000] ; National Natural Science Foundation of China[21172233] ; National Natural Science Foundation of China[81422047] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000365467700004 |
| 出版者 | BENTHAM SCIENCE PUBL LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276277]  |
| 专题 | 药物发现与设计中心 上海药物代谢研究中心 |
| 通讯作者 | Xu, Yechun |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Li,Chen, Wuyan,Chen, Tiantian,et al. Structure-Based Discovery of PDEs Inhibitors[J]. CURRENT TOPICS IN MEDICINAL CHEMISTRY,2016,16(9):917-933. |
| APA | Li, Li,Chen, Wuyan,Chen, Tiantian,Ren, Jing,&Xu, Yechun.(2016).Structure-Based Discovery of PDEs Inhibitors.CURRENT TOPICS IN MEDICINAL CHEMISTRY,16(9),917-933. |
| MLA | Li, Li,et al."Structure-Based Discovery of PDEs Inhibitors".CURRENT TOPICS IN MEDICINAL CHEMISTRY 16.9(2016):917-933. |
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。