Ligand binding to a G protein-coupled receptor captured in a mass spectrometer
文献类型：期刊论文
| 作者 | Yen, Hsin-Yung2; Hopper, Jonathan T. S.3; Liko, Idlir2,3; Allison, Timothy M.2; Zhu, Ya4; Wang, Dejian4,5; Stegmann, Monika1,6,7; Mohammed, Shabaz6,7; Wu, Beili4,5 ; Robinson, Carol V.2
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| 刊名 | SCIENCE ADVANCES
 |
| 出版日期 | 2017-06 |
| 卷号 | 3期号:6 |
| ISSN号 | 2375-2548 |
| DOI | 10.1126/sciadv.1701016 |
| 文献子类 | Article |
| 英文摘要 | G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptors belong to the largest family of membrane-embedded cell surface proteins and are involved in a diverse array of physiological processes. Despite progress in the mass spectrometry of membrane protein complexes, G protein-coupled receptors have remained intractable because of their low yield and instability after extraction from cell membranes. We established conditions in the mass spectrometer that preserve noncovalent ligand binding to the human purinergic receptor P2Y(1). Results established differing affinities for nucleotides and the drug MRS2500 and link antagonist binding with the absence of receptor phosphorylation. Overall, therefore, our results are consistent with drug binding, preventing the conformational changes that facilitate downstream signaling. More generally, we highlight opportunities for mass spectrometry to probe effects of ligand binding on G protein-coupled receptors. |
| WOS关键词 | HUMAN P2Y(1) RECEPTOR ; MACROMOLECULAR ASSEMBLIES ; PURINERGIC RECEPTORS ; ANTAGONIST ; KINASES ; ATP ; ASTROCYTES ; ACTIVATION ; ARRESTINS |
| 资助项目 | European Research Council ENABLE[695511] ; Medical Research Council[G1000819] ; Wellcome Trust Investigator Award[104633/Z/14/Z] |
| WOS研究方向 | Science & Technology - Other Topics |
| 语种 | 英语 |
| WOS记录号 | WOS:000406370700081 |
| 出版者 | AMER ASSOC ADVANCEMENT SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272624]  |
| 专题 | 药物靶标结构与功能中心 |
| 通讯作者 | Robinson, Carol V. |
| 作者单位 | 1.UCB Celltech, 216 Bath Rd, Slough SL1 3WE, Berks, England 2.Univ Oxford, Chem Res Lab, South Parks Rd, Oxford OX1 3QZ, England; 3.OMass Technol Ltd, Ctr Innovat & Enterprise, Begbroke Sci Pk,Woodstock Rd, Oxford OX5 1PF, England; 4.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 5.ShanghaiTech Univ, Sch Life Sci & Technol, 99 Haike Rd, Shanghai 201203, Peoples R China; 6.Univ Oxford, Dept Chem, Oxford OX1 3QU, England; 7.Univ Oxford, Dept Biochem, Oxford OX1 3QU, England; |
| 推荐引用方式 GB/T 7714 | Yen, Hsin-Yung,Hopper, Jonathan T. S.,Liko, Idlir,et al. Ligand binding to a G protein-coupled receptor captured in a mass spectrometer[J]. SCIENCE ADVANCES,2017,3(6). |
| APA | Yen, Hsin-Yung.,Hopper, Jonathan T. S..,Liko, Idlir.,Allison, Timothy M..,Zhu, Ya.,...&Robinson, Carol V..(2017).Ligand binding to a G protein-coupled receptor captured in a mass spectrometer.SCIENCE ADVANCES,3(6). |
| MLA | Yen, Hsin-Yung,et al."Ligand binding to a G protein-coupled receptor captured in a mass spectrometer".SCIENCE ADVANCES 3.6(2017). |
入库方式： OAI收割
来源：上海药物研究所
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