7KNT

CryoEM structure of the apo-CGRP receptor in a detergent micelle

7KNT の概要

• エントリーDOI: 10.2210/pdb7knt/pdb
• EMDBエントリー: 22962
• 分子名称: Receptor activity-modifying protein 1, Calcitonin gene-related peptide type 1 receptor (2 entities in total)
• 機能のキーワード: gpcr, cgrp receptor, apo receptor, membrane protein, signaling protein
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 73341.22

構造登録者

Belousoff, M.J.,Danev, R. (登録日: 2020-11-06, 公開日: 2021-02-24, 最終更新日: 2025-05-14)

主引用文献

Josephs, T.M.,Belousoff, M.J.,Liang, Y.L.,Piper, S.J.,Cao, J.,Garama, D.J.,Leach, K.,Gregory, K.J.,Christopoulos, A.,Hay, D.L.,Danev, R.,Wootten, D.,Sexton, P.M.
Structure and dynamics of the CGRP receptor in apo and peptide-bound forms.
Science, 372:-, 2021

PubMed Abstract: G protein-coupled receptors (GPCRs) are key regulators of information transmission between cells and organs. Despite this, we have only a limited understanding of the behavior of GPCRs in the apo state and the conformational changes upon agonist binding that lead to G protein recruitment and activation. We expressed and purified unmodified apo and peptide-bound calcitonin gene-related peptide (CGRP) receptors from insect cells to determine their cryo-electron microscopy (cryo-EM) structures, and we complemented these with analysis of protein conformational dynamics using hydrogen-deuterium exchange mass spectrometry and three-dimensional variance analysis of the cryo-EM data. Together with our previously published structure of the active, Gs-bound CGRP receptor complex, our work provides insight into the mechanisms of class B1 GPCR activation.

PubMed: 33602864
DOI: 10.1126/science.abf7258

実験手法

ELECTRON MICROSCOPY (3.15 Å)