ACE activity is modulated by kinin B2 receptor

Hypertension
Regiane A SabatiniJoão B Pesquero

Abstract

Angiotensin-converting enzyme (ACE) is an ectoprotein able to modulate the activity of a plethora of compounds, among them angiotensin I and bradykinin. Despite several decades of research, new aspects of the mechanism of action of ACE have been elucidated, expanding our understanding of its role not only in cardiovascular regulation but also in different areas. Recent findings have ascribed an important role for ACE/kinin B(2) receptor heterodimerization in the pharmacological properties of the receptor. In this work, we tested the hypothesis that this interaction also affects ACE enzymatic activity. ACE catalytic activity was analyzed in Chinese hamster ovary cell monolayers coexpressing the somatic form of the enzyme and the receptor coding region using as substrate the fluorescence resonance energy transfer peptide Abz-FRK(Dnp)P-OH. Results show that the coexpression of the kinin B(2) receptor leads to an augmentation in ACE activity. In addition, this effect could be blocked by the B(2) receptor antagonist icatibant. The hypothesis was also tested in endothelial cells, a more physiological system, where both proteins are naturally expressed. Endothelial cells from genetically ablated kinin B(2) receptor mice showed a decre...Continue Reading

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Citations

Jul 21, 2009·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·Vanessa F MerinoJoão B Pesquero
Nov 16, 2013·Journal of Medicinal Chemistry·Darius P ZlotosPaula A Witt-Enderby
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Jul 9, 2010·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·Aline Mourao HilzendegerJoão Bosco Pesquero
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Nov 1, 2020·Pharmaceuticals·Suhail HamidNour-Eddine Rhaleb
May 1, 2019·Life Sciences·Thássio Ricardo Ribeiro MesquitaSandra Lauton-Santos

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