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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board Member: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Sies, Helmut / Turk, Boris / Wittinghofer, Alfred

SCImago Journal Rank (SJR) 2015: 1.607
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Impact per Publication (IPP) 2015: 2.609

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A role for transmembrane domains V and VI in ligand binding and maturation of the angiotensin II AT1 receptor

Graciela C. Pignatari1 / Raphael Rozenfeld2 / Emer S. Ferro3 / Laerte Oliveira4 / Antonio C.M. Paiva5 / Lakshmi A. Devi6







Corresponding authors ;

Citation Information: Biological Chemistry. Volume 387, Issue 3, Pages 269–276, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: 10.1515/BC.2006.036, March 2006

Publication History

September 13, 2005
December 16, 2005
Published Online:


Several studies have proposed that angiotensin II (Ang II) binds to its receptor AT1 through interactions with residues in helices V and VI, suggesting that the distance between these helices is crucial for ligand binding. Based on a 3D model of AT1 in which the C-terminus of Ang II is docked, we identified the hydrophobic residues of TM V and VI pointing towards the external face of the helices, which may play a role in the structure of the binding pocket and in the structural integrity of the receptor. We performed a systematic mutagenesis study of these residues and examined the binding, localization, maturation, and dimerization of the mutated receptors. We found that mutations of hydrophobic residues to alanine in helix V do not alter binding, whereas mutations to glutamate lead to loss of binding without a loss in cell surface expression, suggesting that the external face of helix V may not directly participate in binding, but may rather contribute to the structure of the binding pocket. In contrast, mutations of hydrophobic residues to glutamate in helix VI lead to a loss in cell surface expression, suggesting that the external surface of helix VI plays a structural role and ensures correct folding of the receptor.

Keywords: dimerization; folding; GPCR; maturation; site-directed mutagenesis

Citing Articles

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P. Balakumar and G. Jagadeesh
Journal of Molecular Endocrinology, 2014, Volume 53, Number 2, Page R71
Silvana A.A. Correa, Graciela C. Pignatari, Emer S. Ferro, Nelson A.S. Pacheco, Claudio M. Costa-Neto, João B. Pesquero, Laerte Oliveira, Antonio C.M. Paiva, and Suma I. Shimuta
Regulatory Peptides, 2006, Volume 134, Number 2-3, Page 132
Edson L. Santos, Kely de Picoli Souza, Elena Cibrián-Uhalte, Suzana M. Oliveira, Michael Bader, Claudio M. Costa-Neto, Laerte Oliveira, and João B. Pesquero
International Immunopharmacology, 2008, Volume 8, Number 2, Page 282
Raphael Rozenfeld, Achla Gupta, Khatuna Gagnidze, Maribel P Lim, Ivone Gomes, Dinah Lee-Ramos, Natalia Nieto, and Lakshmi A Devi
The EMBO Journal, 2011, Volume 30, Number 12, Page 2350
Renan Paulo Martin, Eliete da Silva Rodrigues, Silvana Aparecida Alves Correa, Suzana Macedo Oliveira, Renato Arruda Mortara, Laerte Oliveira, Clovis Ryuichi Nakaie, and Suma Imura Shimuta
Biological Chemistry, 2010, Volume 391, Number 10

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