Conformational switch of angiotensin II type 1 receptor underlying mechanical stress-induced activation.

@article{Yasuda2008ConformationalSO,
  title={Conformational switch of angiotensin II type 1 receptor underlying mechanical stress-induced activation.},
  author={Noritaka Yasuda and Shin-ichiro Miura and Hiroshi Akazawa and Toshimasa Tanaka and Yingjie Qin and Yoshihiro Kiya and Satoshi Imaizumi and Masahiro Fujino and Kaoru Ito and Yunzeng Zou and Shigetomo Fukuhara and Satoshi Kunimoto and Koichi Fukuzaki and Toshiaki Sato and Junbo Ge and Naoki Mochizuki and Haruaki Nakaya and Keijiro Saku and Issei Komuro},
  journal={EMBO reports},
  year={2008},
  volume={9 2},
  pages={
          179-86
        }
}
The angiotensin II type 1 (AT(1)) receptor is a G protein-coupled receptor that has a crucial role in the development of load-induced cardiac hypertrophy. Here, we show that cell stretch leads to activation of the AT(1) receptor, which undergoes an anticlockwise rotation and a shift of transmembrane (TM) 7 into the ligand-binding pocket. As an inverse agonist, candesartan suppressed the stretch-induced helical movement of TM7 through the bindings of the carboxyl group of candesartan to the… CONTINUE READING

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