7XBD

Cryo-EM structure of human galanin receptor 2

7XBD の概要

• エントリーDOI: 10.2210/pdb7xbd/pdb
• EMDBエントリー: 33103
• 分子名称: Galanin receptor type 2, Guanine nucleotide-binding protein G(q) subunit alpha, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... (6 entities in total)
• 機能のキーワード: gpcr, membrane protein, galanin
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 6
• 化学式量合計: 145743.01

構造登録者

Ishimoto, N.,Kita, S.,Park, S.Y. (登録日: 2022-03-21, 公開日: 2022-07-13, 最終更新日: 2024-11-06)

主引用文献

Heo, Y.,Ishimoto, N.,Jeon, Y.E.,Yun, J.H.,Ohki, M.,Anraku, Y.,Sasaki, M.,Kita, S.,Fukuhara, H.,Ikuta, T.,Kawakami, K.,Inoue, A.,Maenaka, K.,Tame, J.R.H.,Lee, W.,Park, S.Y.
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.
Plos Biol., 20:e3001714-e3001714, 2022

PubMed Abstract: 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.

PubMed: 35913979
DOI: 10.1371/journal.pbio.3001714

実験手法

ELECTRON MICROSCOPY (3.11 Å)