A review of mutagenesis studies of angiotensin II type 1 receptor, the three-dimensional receptor model in search of the agonist and antagonist binding site and the …

Y Inoue, N Nakamura, T Inagami - Journal of hypertension, 1997 - journals.lww.com
Y Inoue, N Nakamura, T Inagami
Journal of hypertension, 1997journals.lww.com
Objective To seek the mechanism whereby agonists, competitive antagonists and
insurmountable antagonists affect the receptor function differently, by reviewing recent
mutagenesis studies of angiotensin II type 1 receptor (AT 1) in which the binding of the
agonist and antagonists and receptor signaling were affected. AT1 receptor structure and
ligand binding sites We built a model of seven transmembrane spanning domains of the AT
1 receptors using bacteriorhodopsin as a template. The carboxy terminal of angiotensin II …
Objective To seek the mechanism whereby agonists, competitive antagonists and insurmountable antagonists affect the receptor function differently, by reviewing recent mutagenesis studies of angiotensin II type 1 receptor (AT 1) in which the binding of the agonist and antagonists and receptor signaling were affected.
AT1 receptor structure and ligand binding sites We built a model of seven transmembrane spanning domains of the AT 1 receptors using bacteriorhodopsin as a template. The carboxy terminal of angiotensin II binds to Lys 199 in transmembrane domain 5, whereas the guanidinium group of Arg 2 binds to Asp 281 in transmembrane domain 7. Results of studies using mutagenesis supporting proposed ligand-docking models are discussed.
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