Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity
文献类型：期刊论文
| 作者 | Chen, Shuai; Zhao, Xuemei; Tan, Jinzhi; Lu, Hong; Qi, Zhi; Huang, Qiang; Zeng, Xianzhuo; Zhang, Mingjun; Jiang, Shibo; Jiang, Hualiang
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| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 2007-06-22 |
| 卷号 | 565期号:1-3页码:54-59 |
| 关键词 | cyclophilin A cyclosporin A human immunodeficiency virus peptidyl-prolyl cis-trans isomerase |
| ISSN号 | 0014-2999 |
| DOI | 10.1016/j.ejphar.2007.03.023 |
| 文献子类 | Article |
| 英文摘要 | Cyclophilin A acts as protein folding chaperones and intracellular transports in many cellular processes. Previous studies have shown that cyclophilin A can interact with HIV-1 (human immunodeficiency virus type 1) gag protein and enhance viral infectivity. Many cyclophilin A inhibitors such as cyclosporin A can inhibit HIV-1 replication in vitro. Here, we report a structure-based identification of novel non-peptidic cyclophilin A inhibitors as anti-HIV lead compounds. Following a computer-aided virtual screening and subsequent surface plasmon resonance (SPR) analysis, 12 low molecular weight cyclophilin A ligands were selected for further evaluation of their in vitro inhibition of peptidyl-prolyl cis-trans isomerase (PPlase) activity of cyclophilin A and HIV-1 replication. Five of these compounds (FD5, FD8, FD9, FD10 and FD12) exhibited inhibition against both PPlase activity and HIV-1 infection. These active compounds will be used as leads for structure and activity relationship (SAR) and optimization studies in order to design more effective anti-HIV-1 therapeutics, and as probes for investigating the effect of cyclophilins on HIV-1 replication. (c) 2007 Elsevier B.V. All rights reserved. |
| WOS关键词 | IMMUNODEFICIENCY-VIRUS TYPE-1 ; HIGHLY INHIBITORY-ACTIVITY ; CYCLOSPORINE-A ; BIOLOGICAL EVALUATION ; BINDING-PROTEIN ; HIV-1 VIRIONS ; SITE ; INFECTIVITY ; CALCINEURIN ; ISOMERASE |
| 资助项目 | NIAID NIH HHS[R01 AI046221] ; NIAID NIH HHS[AI46221] ; NIAID NIH HHS[R01 AI046221-04] ; NIAID NIH HHS[R21 AI046221] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000247336500007 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273222]  |
| 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 | Jiang, Hualiang |
| 作者单位 | 1.Fudan Univ, Sch Life Sci, Inst Genet, State Key Lab Genet Engn, Shanghai, Peoples R China 2.Chinese Acad Sci, Drug Discovery & Design Ctr, State Key Lab Drug Res, Beijing 100864, Peoples R China 3.New York Blood Ctr, Lindsley F Kimball Res Inst, Lab Viral Immunol, New York, NY 10021 USA |
| 推荐引用方式 GB/T 7714 | Chen, Shuai,Zhao, Xuemei,Tan, Jinzhi,et al. Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2007,565(1-3):54-59. |
| APA | Chen, Shuai.,Zhao, Xuemei.,Tan, Jinzhi.,Lu, Hong.,Qi, Zhi.,...&Yu, Long.(2007).Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity.EUROPEAN JOURNAL OF PHARMACOLOGY,565(1-3),54-59. |
| MLA | Chen, Shuai,et al."Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity".EUROPEAN JOURNAL OF PHARMACOLOGY 565.1-3(2007):54-59. |
入库方式： OAI收割
来源：上海药物研究所
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