Ontology highlight
ABSTRACT:
SUBMITTER: Miura S
PROVIDER: S-EPMC3375280 | biostudies-literature | 2012
REPOSITORIES: biostudies-literature
Miura Shin-ichiro S Kiya Yoshihiro Y Hanzawa Hiroyuki H Nakao Naoki N Fujino Masahiro M Imaizumi Satoshi S Matsuo Yoshino Y Yanagisawa Hiroaki H Koike Hiroyuki H Komuro Issei I Karnik Sadashiva S SS Saku Keijiro K
PloS one 20120614 6
Small differences in the chemical structures of ligands can be responsible for agonism, neutral antagonism or inverse agonism toward a G-protein-coupled receptor (GPCR). Although each ligand may stabilize the receptor conformation in a different way, little is known about the precise conformational differences. We synthesized the angiotensin II type 1 receptor blocker (ARB) olmesartan, R239470 and R794847, which induced inverse agonism, antagonism and agonism, respectively, and then investigated ...[more]