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• W2045208022 abstract "Type 1 angiotensin II (AT1) receptor has a critical role in the development of load-induced cardiac hypertrophy. Recently, we showed that mechanical stretching of cells activates the AT1 receptor without the involvement of angiotensin II (AngII) and that this AngII-independent activation is inhibited by the inverse agonistic activity of the AT1 receptor blocker (ARB), candesartan. Although the inverse agonist activity of ARBs has been studied in terms of their action on constitutively active AT1 receptors, the structure–function relationship of the inverse agonism they exert against stretch-induced AT1 receptor activation has not been fully elucidated. Assays evaluating c-fos gene expression and phosphorylated extracellular signal-regulated protein kinases (ERKs) have shown that olmesartan has strong inverse agonist activities against the constitutively active AT1 receptor and the stretch-induced activation of AT1 receptor, respectively. Ternary drug–receptor interactions, which occur between the hydroxyl group of olmesartan and Tyr113 and between the carboxyl group of olmesartan and Lys199 and His256, were essential for the potent inverse agonist action olmesartan exerts against stretch-induced ERK activation and the constitutive activity of the AT1-N111G mutant receptor. Furthermore, the inverse agonist activity olmesartan exerts against stretch-induced ERK activation requires an additional drug–receptor interaction involving the tetrazole group of olmesartan and Gln257 of the AT1 receptor. These results suggest that multivalent interactions between an inverse agonist and the AT1 receptor are required to stabilize the receptor in an inactive conformation in response to the distinct processes that lead to an AngII-independent activation of the AT1 receptor." @default.
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• W2045208022 date "2009-08-07" @default.
• W2045208022 modified "2023-10-10" @default.
• W2045208022 title "Multivalent ligand–receptor interactions elicit inverse agonist activity of AT1 receptor blockers against stretch-induced AT1 receptor activation" @default.
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• W2045208022 doi "https://doi.org/10.1038/hr.2009.117" @default.
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