中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Progress in Studies of Structure, Mechanism and Antagonists Interaction of GPCR Co-Receptors for HIV

文献类型:期刊论文

作者Zhong, Bing1; Zhen, Yunmei2; Qin, Guangrong1; Yang, Huaiyu1; Jiang, Hualiang1; Chen, Guanghui2; Yu, Kunqian1
刊名CURRENT PHARMACEUTICAL BIOTECHNOLOGY
出版日期2014
卷号15期号:10页码:938-950
关键词CCR5 computational methods crystal structure CXCR4 HIV small molecular antagonists
ISSN号1389-2010
DOI10.2174/1389201015666141031120836
文献子类Article
英文摘要Chemokine receptors are G protein-coupled receptors that contain seven trans-membrane domains. CXCR4 and CCR5 as major co-receptors for HIV-1 entry into host cells are implicated in cancer and inflammation. They have been attractive targets for the pharmaceutical industry basing on their roles in HIV disease. Homology modeling, molecular docking, molecular dynamics, Molecular Mechanics/Generalized Born Surface Area and many other computational methods are applied to illustrate the structure, function and binding site of GPCR. Moreover, the high resolution crystal structures of CXCR4 and CCR5 have provided extremely valuable structural information and receptor activation mechanisms, enable structure-based drug discovery for the treatment of HIV-1 infection. We also describe the recent progress about the small molecule antagonists of CXCR4 and CCR5 and the interaction between GPCR and their ligands predicted by molecular docking and molecular dynamics methods. Future research questions and further investigations are outlined to highlight some researches that may be relevant to the advancement of therapies targeting the important receptor related with HIV.
WOS关键词IMMUNODEFICIENCY-VIRUS TYPE-1 ; SMALL-MOLECULE CCR5 ; SELECTIVE ANTI-HIV-1 ACTIVITY ; PROTEIN-COUPLED RECEPTOR ; CXCR4 CHEMOKINE RECEPTOR ; 2ND EXTRACELLULAR LOOP ; ENTRY INHIBITORS ; BINDING-SITES ; POTENT INHIBITORS ; HIGHLY POTENT
资助项目National High Technology Research and Development Program of China (863 Program)[2012AA020301] ; National High Technology Research and Development Program of China (863 Program)[2012AA01A305] ; Chinese Academy of Sciences Project[KSZD-EW-L09-4] ; National Natural Science Foundation of China[81230076] ; National Natural Science Foundation of China[21210003] ; National Science and Technology Major Project "Key New Drug Creation and Manufacturing Program"[2013ZX09507001]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000345277000005
出版者BENTHAM SCIENCE PUBL LTD
源URL[http://119.78.100.183/handle/2S10ELR8/277255]  
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Yu, Kunqian
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
2.Shantou Univ, Dept Biol, Shantou 515063, Guangdong, Peoples R China
推荐引用方式
GB/T 7714
Zhong, Bing,Zhen, Yunmei,Qin, Guangrong,et al. Progress in Studies of Structure, Mechanism and Antagonists Interaction of GPCR Co-Receptors for HIV[J]. CURRENT PHARMACEUTICAL BIOTECHNOLOGY,2014,15(10):938-950.
APA Zhong, Bing.,Zhen, Yunmei.,Qin, Guangrong.,Yang, Huaiyu.,Jiang, Hualiang.,...&Yu, Kunqian.(2014).Progress in Studies of Structure, Mechanism and Antagonists Interaction of GPCR Co-Receptors for HIV.CURRENT PHARMACEUTICAL BIOTECHNOLOGY,15(10),938-950.
MLA Zhong, Bing,et al."Progress in Studies of Structure, Mechanism and Antagonists Interaction of GPCR Co-Receptors for HIV".CURRENT PHARMACEUTICAL BIOTECHNOLOGY 15.10(2014):938-950.

入库方式: OAI收割

来源:上海药物研究所

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