D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75
文献类型：期刊论文
| 作者 | Du L1; Chen JX2; Chen J1; Yang LM3; Zheng YT3; Tang Y[*]2; Shen X[*]1,2; Jiang HL1,2 |
| 刊名 | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
 |
| 出版日期 | 2008 |
| 卷号 | 375期号:1页码:139-144 |
| 关键词 | HIV-1 integrase Lens epithelium-derived growth factor (LEDGF/p75) yeast two-hybrid assay surface plasmon resonance (SPR) molecular docking site-directed mutagenesis |
| ISSN号 | 0006-291X |
| 通讯作者 | ytang234@ecust.edu.cn ; xshen@mail.shcnc.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | Integration of viral-DNA into host chromosome mediated by the viral protein HIV-1 integrase (IN) is an essential step in the HIV-1 life cycle. In this process, Lens epithelium-derived growth factor (LEDGF/p75) is discovered to function as a cellular co-factor for integration. Since LEDGF/p75 plays an important role in HIV integration, disruption of the LEDGF/p75 interaction with IN has provided a special interest for anti-HIV agent discovery. in this work, we reported that a benzoic acid derivative, 4-[(5-bromo-4-{[2,4-dioxo-3-(2-oxo-2-phenylethyl)-1,3-thiazolidin-5-ylidene]methyl)-2-ethoxyphenoxy)methyl] benzoic acid (D77) could potently inhibit the IN-LEDGF/p75 interaction and affect the HIV-1 IN nuclear distribution thus exhibiting antiretroviral activity. Molecular docking with site-directed mutagenesis analysis and Surface plasmon resonance (SPR) binding assays has clarified possible binding mode of D77 against HIV-1 integrase. As the firstly discovered small molecular compound targeting HIV-1 integrase interaction with LEDGF/p75, D77 might Supply useful structural information for further anti-HIV agent discovery. |
| 收录类别 | 其他 |
| 资助信息 | This work was finan- cially supported by the National Natural Science Foundation of China (Grants Nos. 30525024, 20472095, 20572023), the National ‘‘863” project of China 2006AA609Z447 and 2006AA609Z41), Shanghai Pujiang Program No. 05PJ14034), Shanghai Key Basic Research Project (Grants Nos. 06JC14080, 05JC14092), the State Key Program of Basic Research of China (Grants Nos. 2004CB58905, 2006AA09Z447), and the grant from CAS (Grant No. KSCX2-YW-R-18). |
| 原文出处 | 2008375139.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4627]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China 2.School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China 3.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China |
| 推荐引用方式 GB/T 7714 | Du L,Chen JX,Chen J,et al. D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2008,375(1):139-144. |
| APA | Du L.,Chen JX.,Chen J.,Yang LM.,Zheng YT.,...&Jiang HL.(2008).D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,375(1),139-144. |
| MLA | Du L,et al."D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 375.1(2008):139-144. |
入库方式： OAI收割
来源：昆明动物研究所
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