6JOD

Angiotensin II type 2 receptor with ligand

Summary for 6JOD

• Entry DOI: 10.2210/pdb6jod/pdb
• Related: 5XLI
• Descriptor: Type-2 angiotensin II receptor, Angiotensin II, Soluble cytochrome b562,Soluble cytochrome b562, ... (5 entities in total)
• Functional Keywords: g protein-coupled receptor, regulator of blood pressure, signaling protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 5
• Total formula weight: 92571.89

Authors

Asada, H.,Iwata, S.,Hirata, K.,Shimamura, T. (deposition date: 2019-03-20, release date: 2020-01-15, Last modification date: 2024-10-23)

Primary citation

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

Experimental method

X-RAY DIFFRACTION (3.2 Å)