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Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

文献类型：期刊论文

作者Tan, Qiuxiang1; Zhu, Ya1; Li, Jian1; Chen, Zhuxi5; Han, Gye Won2; Kufareva, Irina3; Li, Tingting1; Ma, Limin1; Fenalti, Gustavo2; Li, Jing1
刊名SCIENCE
出版日期2013-09-20
卷号341期号:6152页码:1387-1390
ISSN号0036-8075
DOI10.1126/science.1241475
文献子类Article
英文摘要The CCR5 chemokine receptor acts as a co-receptor for HIV-1 viral entry. Here we report the 2.7 angstrom-resolution crystal structure of human CCR5 bound to the marketed HIV drug maraviroc. The structure reveals a ligand-binding site that is distinct from the proposed major recognition sites for chemokines and the viral glycoprotein gp120, providing insights into the mechanism of allosteric inhibition of chemokine signaling and viral entry. A comparison between CCR5 and CXCR4 crystal structures, along with models of co-receptor-gp120-V3 complexes, suggests that different charge distributions and steric hindrances caused by residue substitutions may be major determinants of HIV-1 co-receptor selectivity. These high-resolution insights into CCR5 can enable structure-based drug discovery for the treatment of HIV-1 infection.
WOS关键词PROTEIN-COUPLED RECEPTOR ; CRYSTAL-STRUCTURE ; SMALL-MOLECULE ; V3 LOOP ; CORECEPTOR ; ANTAGONIST ; BINDING ; DISCOVERY ; TERMINUS ; ANTIBODY
资助项目National Basic Research Program of China[2012CB518000] ; National Basic Research Program of China[2012CB910400] ; NIH[R01 AI100604] ; NIH[U54 GM094618] ; National Science Foundation of China[31270766] ; National Science Foundation of China[81161120425] ; National Science Foundation of China[81025017] ; Shanghai Science and Technology Committee[11JC1414800] ; Shanghai Science and Technology Committee[12PJ1410500] ; [U01 GM094612] ; [R01 GM071872]
WOS研究方向Science & Technology - Other Topics
语种英语
WOS记录号WOS:000324597200045
出版者AMER ASSOC ADVANCEMENT SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/277457]  
专题药物靶标结构与功能中心
通讯作者Wu, Beili
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
2.Scripps Res Inst, Dept Integrat Struct & Computat Biol, La Jolla, CA 92037 USA;
3.Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, La Jolla, CA 92093 USA;
4.ShanghaiTech Univ, iHuman Inst, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Tan, Qiuxiang,Zhu, Ya,Li, Jian,et al. Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex[J]. SCIENCE,2013,341(6152):1387-1390.
APA Tan, Qiuxiang.,Zhu, Ya.,Li, Jian.,Chen, Zhuxi.,Han, Gye Won.,...&Wu, Beili.(2013).Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex.SCIENCE,341(6152),1387-1390.
MLA Tan, Qiuxiang,et al."Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex".SCIENCE 341.6152(2013):1387-1390.

入库方式： OAI收割

来源：上海药物研究所

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