A proposed EPR approach to evaluating agonist binding site of a peptide receptor

A proposed EPR approach to evaluating agonist binding site of a peptide receptor

Author Lopes, Douglas D. Autor UNIFESP Google Scholar
Poletti, Erick F. Autor UNIFESP Google Scholar
Vieira, Renata F. F. Autor UNIFESP Google Scholar
Jubilut, Guita N. Autor UNIFESP Google Scholar
Oliveira, Laerte Autor UNIFESP Google Scholar
Paiva, Antonio C. M. Autor UNIFESP Google Scholar
Schreier, Shirley Google Scholar
Nakaie, Clovis R. Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Abstract Angiotensin II (Ang II) and its transmembrane AT(1) receptor were selected in order to test an innovative strategy that might allow the assessment of the agonist binding site in the receptor molecule. With the use of the 2,2,6,6-tetramethylpiperidine-1-oxyl-4-amino-4-carboxylic acid (TOAC) paramagnetic probe, a biologically active agonist (TOAC(1)-Ang II), as well as an inactive control (TOAC(4)-Ang II) analogs were mixed in solution with various synthesized AT(1) fragments. Comparative intermolecular interactions, as estimated by analyzing the EPR spectra of solutions, suggested the existence of an agonist binding site containing a sequence composed of portions of the N-terminal (13-17) and the third extracellular loop (266-278) fragments of the AT(1) molecule. Therefore, this combined EPR-TOAC approach shows promise as an alternative for use also in other applications related to specific intermolecular association processes.
Keywords peptide
angiotensin II
receptor
TOAC
EPR
spin label
Language English
Date 2008-06-01
Published in International Journal of Peptide Research and Therapeutics. New York: Springer, v. 14, n. 2, p. 121-126, 2008.
ISSN 1573-3149 (Sherpa/Romeo, impact factor)
Publisher Springer
Extent 121-126
Origin http://dx.doi.org/10.1007/s10989-007-9120-1
Access rights Closed access
Type Article
Web of Science ID WOS:000255878700007
URI http://repositorio.unifesp.br/handle/11600/30692

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