Function
History
Searchers suspected since 70s the existence of different angiotensin receptors. But it was only at the end of 80s that searchers had tools to identify these two distinct trans-membrane receptors (AT1R and AT2R)[1]. Three labs discovered in the same time these two receptors so they were some confusion about the nomenclature. So in 1991 a group of searchers met to define a coherent nomenclature. Finally, around 2015, researchers the crystal structure of the receptor in complex with its antagonist ZD7155 and with an inverse agonist olmesartan [2]. They used x-ray cryogenic-crystallography. They found similar conformation of the receptor when it is linked to the antagonist or to the inverse agonist. They also found conserved molecular recognition modes. So to complete the discovery, they realized some experiments with mutants to identify the different residues which interact with the ligand.
Structure (function relationship)
Primary and secondary structure
376 amino acids [3]
Ligand binding pocket
Application in the therapeutic field
Since angiotensin receptor is involved in the renin-angiotenisin system, it represents a target of choice to cure some diseases like hypertension or heart failure.
