Journal
HYPERTENSION RESEARCH
Volume 26, Issue 12, Pages 937-943Publisher
NATURE PUBLISHING GROUP
DOI: 10.1291/hypres.26.937
Keywords
angiotensin II type 1 receptor; G-protein-coupled receptors; structure and function
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Funding
- NATIONAL HEART, LUNG, AND BLOOD INSTITUTE [R01HL057470, R01HL064845] Funding Source: NIH RePORTER
- NHLBI NIH HHS [HL57470, R01 HL057470, HL64845, R01 HL064845] Funding Source: Medline
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The renin-angiotensin system hormone angiotensin II (Ang II) plays a central role in the pathophysiology of hypertension, cardiac hypertrophy, congestive heart failure, and coronary heart disease. Two distinct sub-types of Ang II receptor, type 1 (AT1) and type 2 (AT2), have been identified, and both have been shown to belong to the G-protein-coupled receptor superfamily (GPCRs). The recent Human Genome Project has revealed more than 1,000 transmembrane (TM) receptors that belong to this superfamily, and it has been estimated that 50% of all clinically used medicines modulate GPCRs activity. Recently, there have been many new insights regarding Ang II receptors and other GPCRs, such as on homo- and hetero-oligomerization, constitutive activation, movement of TM helices, internalization, desensitization and phosphorylation, trafficking, nuclear localization, intracellular protein-induced receptor activation, and receptor-associated proteins. Although AT1 receptor antagonists which prevent Ang II-induced signaling are already clinically available, we here summarize new findings regarding their structure and function, and the possibility of new therapeutic strategies for targeting Ang II receptors through molecular biological techniques.
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