Molecular analysis of angiontensin II receptor inactivation by inverse agonists

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Angiotensin II (AngII) type 1 (AT_1) receptor physically interacts with other mechanosensitive molecules, which implicates functional relevance of the mutual interactions in mechanosensation by AT_1 receptor. Multivalent interactions between an inverse agonist and the AT_1 receptor cooperate to stabilize the receptor in an inactive conformation in response to the distinct processes of AngII-independent activation. Constitutive activity of AT_1 receptor contributes to cardiac remodeling independently of AngII even in vivo, when AT_1 receptor is up-regulalted in the heart, and inverse agonism of AT_1 receptor blockers provides therapeutic effects in the prevention of cardiac remodeling induced by constitutive activity of AT_1 receptor.