Ontology highlight
ABSTRACT:
SUBMITTER: Nagiri C
PROVIDER: S-EPMC6588608 | biostudies-literature | 2019
REPOSITORIES: biostudies-literature
Nagiri Chisae C Shihoya Wataru W Inoue Asuka A Kadji Francois Marie Ngako FMN Aoki Junken J Nureki Osamu O
Communications biology 20190621
Endothelin receptors (ET<sub>A</sub> and ET<sub>B</sub>) are G-protein-coupled receptors activated by endothelin-1 and are involved in blood pressure regulation. IRL2500 is a peptide-mimetic of the C-terminal tripeptide of endothelin-1, and has been characterized as a potent ET<sub>B</sub>-selective antagonist, which has preventive effects against brain edema. Here, we report the crystal structure of the human ET<sub>B</sub> receptor in complex with IRL2500 at 2.7 Å-resolution. The structure rev ...[more]