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Title: A proposed EPR approach to evaluating agonist binding site of a peptide receptor
Authors: Lopes, Douglas D. [UNIFESP]
Poletti, Erick F. [UNIFESP]
Vieira, Renata F. F. [UNIFESP]
Jubilut, Guita N. [UNIFESP]
Oliveira, Laerte [UNIFESP]
Paiva, Antonio C. M. [UNIFESP]
Schreier, Shirley
Nakaie, Clovis R. [UNIFESP]
Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Keywords: peptide
angiotensin II
spin label
Issue Date: 1-Jun-2008
Publisher: Springer
Citation: International Journal of Peptide Research and Therapeutics. New York: Springer, v. 14, n. 2, p. 121-126, 2008.
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.
ISSN: 1573-3149
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Appears in Collections:Em verificação - Geral

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