A Proposed EPR Approach to Evaluating Agonist Binding Site of a Peptide Receptor

Autor:	Renata F. F. Vieira, Laerte Oliveira, Erick Fernando Poletti, Clovis R. Nakaie, Antonio C.M. Paiva, Shirley Schreier, Guita Nicolaewsky Jubilut, Douglas Duarte Lopes
Rok vydání:	2007
Předmět:	Agonist chemistry.chemical_classification Angiotensin II receptor type 1 Stereochemistry medicine.drug_class Chemistry Bioengineering Peptide Biochemistry Angiotensin II Transmembrane protein Analytical Chemistry Drug Discovery medicine Molecular Medicine Binding site Spin label Receptor
Zdroj:	International Journal of Peptide Research and Therapeutics. 14:121-126
ISSN:	1573-3904 1573-3149
DOI:	10.1007/s10989-007-9120-1
Popis:	Angiotensin II (Ang II) and its transmembrane AT1 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 (TOAC1-Ang II), as well as an inactive control (TOAC4-Ang II) analogs were mixed in solution with various synthesized AT1 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 AT1 molecule. Therefore, this combined EPR-TOAC approach shows promise as an alternative for use also in other applications related to specific intermolecular association processes.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::866dbbf2f331e9078688d038c8d8dfbe https://doi.org/10.1007/s10989-007-9120-1 Zobrazit plný text záznamu Full text from SpringerLink