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Structure of an Agonist-Bound Human A(2A) Adenosine Receptor | |
Xu, Fei; Wu, Huixian; Katritch, Vsevolod; Han, Gye Won; Jacobson, Kenneth A.; Gao, Zhan-Guo; Cherezov, Vadim; Stevens, Raymond C. | |
2011 | |
发表期刊 | SCIENCE |
ISSN | 0036-8075 |
EISSN | 1095-9203 |
卷号 | 332期号:6027页码:322-327 |
发表状态 | 已发表 |
DOI | 10.1126/science.1202793 |
摘要 | Activation of G protein-coupled receptors upon agonist binding is a critical step in the signaling cascade for this family of cell surface proteins. We report the crystal structure of the A(2A) adenosine receptor (A(2A)AR) bound to an agonist UK-432097 at 2.7 angstrom resolution. Relative to inactive, antagonist-bound A(2A)AR, the agonist-bound structure displays an outward tilt and rotation of the cytoplasmic half of helix VI, a movement of helix V, and an axial shift of helix III, resembling the changes associated with the active-state opsin structure. Additionally, a seesaw movement of helix VII and a shift of extracellular loop 3 are likely specific to A(2A)AR and its ligand. The results define the molecule UK-432097 as a "conformationally selective agonist" capable of receptor stabilization in a specific active-state configuration. |
URL | 查看原文 |
收录类别 | SCI |
WOS研究方向 | Science & Technology - Other Topics |
WOS类目 | Multidisciplinary Sciences |
WOS记录号 | WOS:000289516600036 |
WOS关键词 | CRYSTAL-STRUCTURE ; ALLOSTERIC MODULATION ; SUBTYPE-SELECTIVITY ; BINDING-SITE ; IDENTIFICATION ; DOMAINS ; GPCR |
原始文献类型 | Article |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/120266 |
专题 | 个人在本单位外知识产出 |
通讯作者 | Stevens, Raymond C. |
作者单位 | 1.Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA 2.Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, La Jolla, CA 92093 USA 3.Univ Calif San Diego, San Diego Supercomp Ctr, La Jolla, CA 92093 USA 4.NIDDKD, Bioorgan Chem Lab, Bethesda, MD 20892 USA |
推荐引用方式 GB/T 7714 | Xu, Fei,Wu, Huixian,Katritch, Vsevolod,et al. Structure of an Agonist-Bound Human A(2A) Adenosine Receptor[J]. SCIENCE,2011,332(6027):322-327. |
APA | Xu, Fei.,Wu, Huixian.,Katritch, Vsevolod.,Han, Gye Won.,Jacobson, Kenneth A..,...&Stevens, Raymond C..(2011).Structure of an Agonist-Bound Human A(2A) Adenosine Receptor.SCIENCE,332(6027),322-327. |
MLA | Xu, Fei,et al."Structure of an Agonist-Bound Human A(2A) Adenosine Receptor".SCIENCE 332.6027(2011):322-327. |
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