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
ISSN0036-8075
EISSN1095-9203
卷号332期号:6027页码:322-327
发表状态已发表
DOI10.1126/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.

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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
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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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