A Proposed EPR Approach to Evaluating Agonist Binding Site of a Peptide Receptor |
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| Authors: | Douglas D Lopes Erick F Poletti Renata F F Vieira Guita N Jubilut Laerte Oliveira Antonio C M Paiva Shirley Schreier Clovis R Nakaie |
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| Institution: | (1) Department of Biophysics, Universidade Federal de Sao Paulo, Rua Três de Maio 100, Sao Paulo, 04044-020, Brazil;(2) Department of Biochemistry, Institute of Chemistry, Universidade de Sao Paulo, Sao Paulo , 05513-870, Brazil |
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| Abstract: | 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.
In memoriam of Professor Paiva. |
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| Keywords: | Peptide Angiotensin II Receptor TOAC EPR Spin label |
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