Residues Val(254), His(256), and Phe(259) of the angiotensin II AT(1) receptor are not involved in ligand binding but participate in signal transduction

Residues Val(254), His(256), and Phe(259) of the angiotensin II AT(1) receptor are not involved in ligand binding but participate in signal transduction

Autor Han, Heliana Maria do Carmo Barbosa Autor UNIFESP Google Scholar
Shimuta, Suma Imura Autor UNIFESP Google Scholar
Kanashiro, Celia Akemi Autor UNIFESP Google Scholar
Oliveira, Laerte Autor UNIFESP Google Scholar
Han, Sang Won Autor UNIFESP Google Scholar
Paiva, Antonio Cechelli de Mattos Autor UNIFESP Google Scholar
Instituição Universidade Federal de São Paulo (UNIFESP)
Resumo The role of the external third of helix VI of the angiotensin II (AII) AT(1) receptor for the interaction with its ligand and for the subsequent signal transduction was investigated by individually replacing residues 252-256 by Ala, and residues 259 or 261 by Tyr, and permanently transfecting the resulting mutants to Chinese hamster ovary (CHO) cells, Binding experiments showed no great changes in affinity of any of the mutants for AII, [Sar(1)]-AII, or [Sar(1), Leu(8)]-AII, but the affinity for the nonpeptide antagonist DuP753 was significantly decreased. the inositol phosphate response to AII was remarkably decreased in mutants V254A, H256A, and F259Y. These results indicate that AT(1) residues Val(254), His(256), and Phe(259) are not involved in ligand binding but participate in signal transduction, Based in these results and in others from the literature, it is suggested that, in addition tea the His(256) imidazole ring, the Phe(259) aromatic ring interacts with the AII's Phe(8), thus contributing to the signal-triggering mechanism.
Idioma Inglês
Data de publicação 1998-06-01
Publicado em Molecular Endocrinology. Chevy Chase: Endocrine Soc, v. 12, n. 6, p. 810-814, 1998.
ISSN 0888-8809 (Sherpa/Romeo, fator de impacto)
Publicador Endocrine Soc
Extensão 810-814
Fonte http://dx.doi.org/10.1210/mend.12.6.0127
Direito de acesso Acesso aberto Open Access
Tipo Artigo
Web of Science WOS:000073891800004
Endereço permanente http://repositorio.unifesp.br/handle/11600/25899

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