6JOD

Angiotensin II type 2 receptor with ligand

6JOD の概要

• エントリーDOI: 10.2210/pdb6jod/pdb
• 関連するPDBエントリー: 5XLI
• 分子名称: Type-2 angiotensin II receptor, Angiotensin II, Soluble cytochrome b562,Soluble cytochrome b562, ... (5 entities in total)
• 機能のキーワード: g protein-coupled receptor, regulator of blood pressure, signaling protein
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 5
• 化学式量合計: 92571.89

構造登録者

Asada, H.,Iwata, S.,Hirata, K.,Shimamura, T. (登録日: 2019-03-20, 公開日: 2020-01-15, 最終更新日: 2024-10-23)

主引用文献

Asada, H.,Inoue, A.,Ngako Kadji, F.M.,Hirata, K.,Shiimura, Y.,Im, D.,Shimamura, T.,Nomura, N.,Iwanari, H.,Hamakubo, T.,Kusano-Arai, O.,Hisano, H.,Uemura, T.,Suno, C.,Aoki, J.,Iwata, S.
The Crystal Structure of Angiotensin II Type 2 Receptor with Endogenous Peptide Hormone.
Structure, 28:418-, 2020

PubMed Abstract: Angiotensin II (AngII) is a peptide hormone that plays a key role in regulating blood pressure, and its interactions with the G protein-coupled receptors, AngII type-1 receptor (ATR) and AngII type-2 receptor (ATR), are central to its mechanism of action. We solved the crystal structure of human ATR bound to AngII and its specific antibody at 3.2-Å resolution. AngII (full agonist) and [Sar, Ile]-AngII (partial agonist) interact with ATR in a similar fashion, except at the bottom of the ATR ligand-binding pocket. In particular, the residues including Met128, which constitute the deep end of the cavity, play important roles in angiotensin receptor (ATR) activation upon AngII binding. These differences that occur upon endogenous ligand binding may contribute to a structural change in ATR, leading to normalization of the non-canonical coordination of helix 8. Our results will inform the design of more effective ligands for ATRs.

PubMed: 31899086
DOI: 10.1016/j.str.2019.12.003

実験手法

X-RAY DIFFRACTION (3.2 Å)