5XJM

Complex structure of angiotensin II type 2 receptor with Fab

5XJM の概要

• エントリーDOI: 10.2210/pdb5xjm/pdb
• 関連するPDBエントリー: 5XLI
• 分子名称: Type-2 angiotensin II receptor,Soluble cytochrome b562,Type-2 angiotensin II receptor, FabH, FabL, ... (4 entities in total)
• 機能のキーワード: class a gpcr, regulate human blood pressure, angiotensin receptors, signaling protein
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 95665.45

構造登録者

Asada, H.,Horita, S.,Shimamura, T.,Iwata, S. (登録日: 2017-05-02, 公開日: 2018-07-11, 最終更新日: 2024-11-13)

主引用文献

Asada, H.,Horita, S.,Hirata, K.,Shiroishi, M.,Shiimura, Y.,Iwanari, H.,Hamakubo, T.,Shimamura, T.,Nomura, N.,Kusano-Arai, O.,Uemura, T.,Suno, C.,Kobayashi, T.,Iwata, S.
Crystal structure of the human angiotensin II type 2 receptor bound to an angiotensin II analog
Nat. Struct. Mol. Biol., 25:570-576, 2018

PubMed Abstract: Angiotensin II (AngII) plays a central role in regulating human blood pressure, which is mainly mediated by interactions between AngII and the G-protein-coupled receptors (GPCRs) AngII type 1 receptor (ATR) and AngII type 2 receptor (ATR). We have solved the crystal structure of human ATR binding the peptide ligand [Sar, Ile]AngII and its specific antibody at 3.2-Å resolution. [Sar, Ile]AngII interacts with both the 'core' binding domain, where the small-molecule ligands of ATR and ATR bind, and the 'extended' binding domain, which is equivalent to the allosteric modulator binding site of muscarinic acetylcholine receptor. We generated an antibody fragment to stabilize the extended binding domain that functions as a positive allosteric modulator. We also identified a signature positively charged cluster, which is conserved among peptide-binding receptors, to locate C termini at the bottom of the binding pocket. The reported results should help with designing ligands for angiotensin receptors and possibly to other peptide GPCRs.

PubMed: 29967536
DOI: 10.1038/s41594-018-0079-8

実験手法

X-RAY DIFFRACTION (3.2 Å)