alexa Molecular Mechanism of Attenuated Inverse Agonism of ARBs for Active-State of AT1 receptor

Research & Reviews: Journal of Hospital and Clinical Pharmacy
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Review Article

Molecular Mechanism of Attenuated Inverse Agonism of ARBs for Active-State of AT1 receptor

Takanobu Takezako1,2*, Hamiyet Unal3, Sadashiva S Karnik4 and Koichi Node5

Department of Advanced Heart Research, Saga University, Saga, Japan

Department of Biosignal Pathophysiology, Kobe University Graduate School of Medicine, Kobe, Japan

Department of Basic Sciences, Faculty of Pharmacy and Betul Ziya Eren Genome and Stem Cell Center, Erciyes University, Kayseri, Turkey

Department of Molecular Cardiology, Lerner Research Institute, Cleveland Clinic Foundation Cleveland, Ohio, USA

Department of Cardiovascular Medicine, Saga University, Japan

*Corresponding Author:
Takanobu Takezako
Department of Biosignal Pathophysiology
Kobe University Graduate School of Medicine, 1-1 Rokkodai-cho
Nada-ku, Kobe 657- 8501, Japan
Tel: +81-78-881-1212
Fax: +81-78- 803-5254
E-mail: [email protected]

Received: 01/09/2015 Accepted: 11/09/2015 Published: 15/09/2015



Typically AngII the octapeptide hormone produced by the renin angiotensin system binds to angiotensin II type 1 receptor (AT1R) and activates its functions which can be competitively inhibited by AT1R blockers (ARBs). However several studies have demonstrated ligandindependently activated AT1R in clinical setting such as mechanical stretch and auto-antibodies as well as receptor mutations. Clinically used ARBs prevent ligand-independent activation of the AT1R by inverse agonistic effect with variable efficacies. Ligand-independent transition of AT1R to activated state is known to attenuate inverse agonistic efficacy of the ARBs but the molecular mechanism is unknown. Therefore, identifying the molecular basis of reduced inverse agonist efficacy of ARBs for the active-state of the AT1R provided a fundamental insight for application of ARBs in treatment of diseases as well as for future drug development. Since AT1R is an extensively studied member of G-protein coupled receptor superfamily encoded in human genome the new regulatory mechanisms of inverse agonist function we describe is relevant to disorders caused by other members of this superfamily. In this review, we focus on the molecular mechanism of attenuated inverse agonism of the ARBs.


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