One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation
文献类型：期刊论文
| 作者 | Li, Jian; Chen, Jing ; Zhang, Li; Wang, Feng; Gui, Chunshan; Qin, Yu; Xu, Qiang; Liu, Hong; Nan, Fajun; Shen, Jingkang
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2006-08-15 |
| 卷号 | 14期号:16页码:5527-5534 |
| 关键词 | cyclophilin A inhibitor quinoxaline surface plasmon resonance fluorescence titration |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2006.04.026 |
| 文献子类 | Article |
| 英文摘要 | Cyclophilin A (CypA) is a ubiquitous cellular enzyme playing critical roles in many biological processes, and its inhibitor has been reported to have potential immunosuppressive activity. In this work, we reported a novel quinoxaline derivative, 2,3-di(furan-2-yl)-6-(3-N,N-diethylcarbamoyl-piperidino)carbonylamino quinoxaline (DC838, 3), which was confirmed to be a potent inhibitor against human CypA. By using the surface plasmon resonance (SPR) and fluorescence titration techniques, the kinetic analysis of CypA/DC838 interaction was quantitatively performed. CypA peptidyl prolyl cis-trans isomerase (PPIase) activity inhibition assay showed that DC838 demonstrated highly CypA PPIase inhibitory activity. In vivo assay results showed that DC838 could inhibit mouse spleen cell proliferation induced by concanavalin A (Con A). Molecular docking simulation further elucidated the specific DC838 binding to CypA at the atomic level. The current work should provide useful information in the discovery of immunosuppressor based on CypA inhibitor. (c) 2006 Elsevier Ltd. All rights reserved. |
| WOS关键词 | CIS-TRANS-ISOMERASE ; VIRUS TYPE-1 HIV-1 ; CYCLOSPORINE-A ; PROTEIN-CYCLOPHILIN ; BINDING-PROTEIN ; GAG PROTEINS ; SDZ NIM-811 ; VIRIONS ; REPLICATION ; CALCINEURIN |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000239472700011 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273520]  |
| 专题 | 药理学第三研究室 药物发现与设计中心 |
| 通讯作者 | Shen, Xu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr,State Key Lab Drug Re, Shanghai 201203, Peoples R China 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 3.Nanjing Univ, Sch Life Sci, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jian,Chen, Jing,Zhang, Li,et al. One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2006,14(16):5527-5534. |
| APA | Li, Jian.,Chen, Jing.,Zhang, Li.,Wang, Feng.,Gui, Chunshan.,...&Jiang, Hualiang.(2006).One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation.BIOORGANIC & MEDICINAL CHEMISTRY,14(16),5527-5534. |
| MLA | Li, Jian,et al."One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation".BIOORGANIC & MEDICINAL CHEMISTRY 14.16(2006):5527-5534. |
入库方式： OAI收割
来源：上海药物研究所
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