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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

A fluorimetric binding assay for angiotensin II and kinin receptors

Full text
Author(s):
Martin, Renan P. [1] ; Filippelli-Silva, Rafael [1] ; Rodrigues, Eliete S. [1] ; Nakaie, Clovis R. [1] ; Shimuta, Suma I. [1]
Total Authors: 5
Affiliation:
[1] Univ Fed Sao Paulo, Dept Biophys, Rua Botucatu 862, BR-04023062 Sao Paulo - Brazil
Total Affiliations: 1
Document type: Journal article
Source: JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS; v. 79, p. 55-59, MAY-JUN 2016.
Web of Science Citations: 0
Abstract

Angiotensin II (AngII) and kinins (bradykinin (BK) and des-Arg9-bradykinin (DBK)), are potent agents involved in the maintenance of blood pressure and several biological activities, and their better understanding is important to produce new drugs aimed to control arterial blood pressure. Previous studies on ligand-receptor binding have been based on radioactive methods, which led us to study a new method based on the fluorimetric method. A lanthanide attached to the N-terminal segment of the peptide (AngII, BK and DBK), which produces a time-resolved-fluorescent ligand, was used in a binding test with CHO cells expressing the AT1, AT2, B1 or B2 receptors in comparison with the same cell line tested with the radioactive ligand. Our findings indicated that the nonradioactive-method provided a comparable result for the angiotensin receptors. On the other hand, the kinin receptors showed a slight reduction in the binding affinity, probably due to the linkage at the N-terminal segment and/or to the lower biological stability associated to the high temperature (37 degrees C) used for the fluorimetric method, while the radioactive one was at 4 degrees C. Wecan conclude that a time-resolved fluorescence assay would provide a sensitive method as an alternative tool for receptor studies. (C) 2016 Elsevier Inc. All rights reserved. (AU)

FAPESP's process: 07/56480-0 - Synthesis and studies of peptides and analogues involved principally in the renin-angiotensin and kallikrein-kinin system
Grantee:Clovis Ryuichi Nakaie
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 11/02208-2 - Structure-activity correlations between the angiotensin AT1 and AT2 receptors and the kinin B1 and B2 receptors in the light of chemokine CXCR4 receptor
Grantee:Suma Imura Shimuta
Support Opportunities: Regular Research Grants
FAPESP's process: 14/20965-3 - In silico study of genetic mutations causing hereditary angioedema
Grantee:Renan Paulo Martin
Support Opportunities: Scholarships in Brazil - Post-Doctoral