1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor
文献类型：期刊论文
| 作者 | Gu WG1,3; Ip DTM1; Liu SJ1; Chan JH1; Wang Y1; Zhang X2; Zheng YT2; Wan DCC[*]1 |
| 刊名 | CHEMICO-BIOLOGICAL INTERACTIONS
 |
| 出版日期 | 2014 |
| 卷号 | 213期号:X页码:21-27 |
| 关键词 | HIV-1 integrase Lens epithelium-derived growth factor (LEDGF/P75 Molecular docking |
| 通讯作者 | chicheongwan@cuhk.edu.hk |
| 英文摘要 | Translocation of viral integrase (IN) into the nucleus is a critical precondition of integration during the life cycle of HIV, a causative agent of Acquired Immunodeficiency Syndromes (AIDS). As the first discovered cellular factor to interact with IN, Lens epithelium-derived growth factor (LEDGF/p75) plays an important role in the process of integration. Disruption of the LEDGF/p75-IN interaction has provided a great interest for anti-HIV agent discovery. In this work, we reported that one small molecular compound, 1,4-bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene(Compound 15), potently inhibit the IN-LEDGF/ p75 interaction and affect the HIV-1 IN nuclear distribution at 1 mu M. The putative binding mode of Compound 15 was constructed by a molecular docking simulation to provide structural insights into the ligand-binding mechanism. Compound 15 suppressed viral replication by measuring p24 antigen production in HIV-1(IIIB) acute infected C8166 cells with EC50 value of 11.19 mu M. Compound 15 might supply useful structural information for further anti-HIV agent discovery. |
| 收录类别 | SCI |
| 资助信息 | This work was partially supported by the Research Fund for the Control of Infectious Diseases from Hong Kong to DCCW (08070152), the National Natural Science Foundation of China (81102483; 81001462; 81360503), 973 Program (2009CB522306) and the Key Scientific and Technological Program of China (2012ZX10001-006, 2012ZX10001-007) and Yunnan (2010GA001). |
| 语种 | 英语 |
| WOS记录号 | WOS:000335281200003 |
| 公开日期 | 2014-10-15 |
| 源URL | [http://159.226.149.42:8088/handle/152453/8051]  |
| 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.School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, SAR, China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, China 3.Department of Immunology, Zunyi Medical College, Zunyi, China |
| 推荐引用方式 GB/T 7714 | Gu WG,Ip DTM,Liu SJ,et al. 1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor[J]. CHEMICO-BIOLOGICAL INTERACTIONS,2014,213(X):21-27. |
| APA | Gu WG.,Ip DTM.,Liu SJ.,Chan JH.,Wang Y.,...&Wan DCC[*].(2014).1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor.CHEMICO-BIOLOGICAL INTERACTIONS,213(X),21-27. |
| MLA | Gu WG,et al."1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor".CHEMICO-BIOLOGICAL INTERACTIONS 213.X(2014):21-27. |
入库方式： OAI收割
来源：昆明动物研究所
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