Mechanochemical Activation of Class-B G-Protein-Coupled Receptor upon Peptide-Ligand Binding
文献类型：期刊论文
| 作者 | Lo Giudice, Cristina1; Zhang, Haonan2; Wu, Beili2 ; Alsteens, David1
|
| 刊名 | NANO LETTERS
 |
| 出版日期 | 2020-07-08 |
| 卷号 | 20期号:7页码:5575-5582 |
| 关键词 | Atomic force microscopy single-molecule force spectroscopy human glucagon receptor G-protein-coupled receptors mechanotransduction |
| ISSN号 | 1530-6984 |
| DOI | 10.1021/acs.nanolett.0c02333 |
| 通讯作者 | Alsteens, David(david.alsteens@uclouvain.be) |
| 英文摘要 | Glucagon binding to the class-B G-protein-coupled glucagon receptor (GCGR) triggers the release of glucose from the liver during fasting. Recently, GCGR crystal structures have highlighted the conformation and molecular details of inactive and active receptor states. However, the dynamics of the conformational changes accompanying GCGR activation remains unclear. Here, we use multiplex force-distance curve-based atomic force microscopy (FD-based AFM) to probe in situ glucagon binding to individual GCGRs and monitor dynamically the transition to the active conformer. After a "dock" step, in which glucagon is partially bound to the GCGR extracellular domain, further interactions of the N-terminus with the transmembrane domain trigger an increase in the stiffness of the complex, adopting a highly stable and rigid "lock" conformer. This mechanotransduction is key for G-protein recruitment. |
| WOS关键词 | GLUCAGON RECEPTOR ; INSIGHTS ; COMPLEX |
| 资助项目 | Universite' Catholique de Louvain ; Fonds National de la Recherche Scientifique (F.R.S.-FNRS)[PDR T.0090.15] ; European Molecular Biology Organization (EMBO)[ALTF 542-2018] |
| WOS研究方向 | Chemistry ; Science & Technology - Other Topics ; Materials Science ; Physics |
| 语种 | 英语 |
| WOS记录号 | WOS:000548893200115 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/292088]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Alsteens, David |
| 作者单位 | 1.Catholic Univ Louvain, Louvain Inst Biomol Sci & Technol, Louvain La Neuve, Belgium 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lo Giudice, Cristina,Zhang, Haonan,Wu, Beili,et al. Mechanochemical Activation of Class-B G-Protein-Coupled Receptor upon Peptide-Ligand Binding[J]. NANO LETTERS,2020,20(7):5575-5582. |
| APA | Lo Giudice, Cristina,Zhang, Haonan,Wu, Beili,&Alsteens, David.(2020).Mechanochemical Activation of Class-B G-Protein-Coupled Receptor upon Peptide-Ligand Binding.NANO LETTERS,20(7),5575-5582. |
| MLA | Lo Giudice, Cristina,et al."Mechanochemical Activation of Class-B G-Protein-Coupled Receptor upon Peptide-Ligand Binding".NANO LETTERS 20.7(2020):5575-5582. |
入库方式： OAI收割
来源：上海药物研究所
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