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-Structure paper
| タイトル | Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface. |
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| ジャーナル・号・ページ | PLoS Biol, Vol. 20, Issue 8, Page e3001714, Year 2022 |
| 掲載日 | 2022年8月1日 |
著者 | Yunseok Heo / Naito Ishimoto / Ye-Eun Jeon / Ji-Hye Yun / Mio Ohki / Yuki Anraku / Mina Sasaki / Shunsuke Kita / Hideo Fukuhara / Tatsuya Ikuta / Kouki Kawakami / Asuka Inoue / Katsumi Maenaka / Jeremy R H Tame / Weontae Lee / Sam-Yong Park / ![]() |
| PubMed 要旨 | Galanin is a neuropeptide expressed in the central and peripheral nervous systems, where it regulates various processes including neuroendocrine release, cognition, and nerve regeneration. Three G- ...Galanin is a neuropeptide expressed in the central and peripheral nervous systems, where it regulates various processes including neuroendocrine release, cognition, and nerve regeneration. Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts to treat diseases including Alzheimer's disease, anxiety, and addiction. To understand the basis of the ligand preferences of the receptors and to assist structure-based drug design, we used cryo-electron microscopy (cryo-EM) to solve the molecular structure of GALR2 bound to galanin and a cognate heterotrimeric G-protein, providing a molecular view of the neuropeptide binding site. Mutant proteins were assayed to help reveal the basis of ligand specificity, and structural comparison between the activated GALR2 and inactive hβ2AR was used to relate galanin binding to the movements of transmembrane (TM) helices and the G-protein interface. |
リンク | PLoS Biol / PubMed:35913979 / PubMed Central |
| 手法 | EM (単粒子) |
| 解像度 | 3.11 Å |
| 構造データ | EMDB-33103, PDB-7xbd: |
| 由来 |
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キーワード | MEMBRANE PROTEIN / GPCR / GALANIN |
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homo sapiens (ヒト)
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