Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex
Tan, Qiuxiang1; Zhu, Ya1; Li, Jian1; Chen, Zhuxi2; Han, Gye Won3; Kufareva, Irina4; Li, Tingting1; Ma, Limin1; Fenalti, Gustavo3; Li, Jing1; Zhang, Wenru1; Xie, Xin1; Yang, Huaiyu2; Jiang, Hualiang2; Cherezov, Vadim3; Liu, Hong1; Stevens, Raymond C.1,3,5; Zhao, Qiang1; Wu, Beili1
2013-09-20
Source PublicationSCIENCE
ISSN0036-8075
Volume341Issue:6152Pages:1387-1390
Status已发表
DOI10.1126/science.1241475
AbstractThe 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.
Indexed BySCI
Language英语
Funding Project[R01 GM071872]
WOS Research AreaScience & Technology - Other Topics
WOS SubjectMultidisciplinary Sciences
WOS IDWOS:000324597200045
PublisherAMER ASSOC ADVANCEMENT SCIENCE
WOS KeywordCRYSTAL-STRUCTURE ; SMALL-MOLECULE ; CORECEPTOR ; BINDING ; DISCOVERY ; TERMINUS ; ANTIBODY
Original Document TypeArticle
Citation statistics
Cited Times:386[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://kms.shanghaitech.edu.cn/handle/2MSLDSTB/2452
CollectioniHuman研究所_特聘教授组_Raymond Stevens组
iHuman研究所
生命科学与技术学院_特聘教授组_吴蓓丽组
Corresponding AuthorWu, Beili
Affiliation1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China
3.Scripps Res Inst, Dept Integrat Struct & Computat Biol, La Jolla, CA 92037 USA
4.Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, La Jolla, CA 92093 USA
5.ShanghaiTech Univ, iHuman Inst, Shanghai 201203, Peoples R China
Recommended Citation
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.
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