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

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dc.contributor.authorLopes, Douglas Duarte [UNIFESP]
dc.contributor.authorPoletti, Erick Fernando [UNIFESP]
dc.contributor.authorVieira, Renata de Freitas Fischer [UNIFESP]
dc.contributor.authorJubilut, Guita Nicolaewsky [UNIFESP]
dc.contributor.authorOliveira, Laerte [UNIFESP]
dc.contributor.authorPaiva, Antonio Cechelli de Mattos [UNIFESP]
dc.contributor.authorSchreier, Shirley
dc.contributor.authorNakaie, Clovis Ryuichi [UNIFESP]
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.date.accessioned2016-01-24T13:51:25Z
dc.date.available2016-01-24T13:51:25Z
dc.date.issued2008-06-01
dc.description.abstractAngiotensin 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.en
dc.description.affiliationUniversidade Federal de São Paulo, Dept Biophys, BR-04044020 São Paulo, Brazil
dc.description.affiliationUniv São Paulo, Inst Chem, Dept Biochem, BR-05513870 São Paulo, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, Dept Biophys, BR-04044020 São Paulo, Brazil
dc.description.sourceWeb of Science
dc.format.extent121-126
dc.identifierhttps://dx.doi.org/10.1007/s10989-007-9120-1
dc.identifier.citationInternational Journal of Peptide Research and Therapeutics. New York: Springer, v. 14, n. 2, p. 121-126, 2008.
dc.identifier.doi10.1007/s10989-007-9120-1
dc.identifier.issn1573-3149
dc.identifier.urihttps://repositorio.unifesp.br/handle/11600/30692
dc.identifier.wosWOS:000255878700007
dc.language.isoeng
dc.publisherSpringer
dc.relation.ispartofInternational Journal of Peptide Research and Therapeutics
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rights.licensehttp://www.springer.com/open+access/authors+rights?SGWID=0-176704-12-683201-0
dc.subjectPeptideen
dc.subjectAngiotensin IIen
dc.subjectReceptoren
dc.subjectTOACen
dc.subjectEPRen
dc.subjectSpin labelen
dc.titleA proposed EPR approach to evaluating agonist binding site of a peptide receptoren
dc.typeinfo:eu-repo/semantics/article
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