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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.)

Current basis for discovery and development of aryl hydrocarbon receptor antagonists for experimental and therapeutic use in atherosclerosis

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Pernomian, Larissa [1] ; da Silva, Carlos H. T. P. [1]
Total Authors: 2
[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Computat Lab Pharmaceut Chem, BR-14040903 Ribeirao Preto, SP - Brazil
Total Affiliations: 1
Document type: Review article
Source: European Journal of Pharmacology; v. 764, p. 118-123, OCT 5 2015.
Web of Science Citations: 6

The important role played by aryl hydrocarbon receptor activation in the pathophysiology of atherosclerosis induced by cigarette smoke exposure has spurred the clinical interest in the development of aryl hydrocarbon receptor antagonists with atheroprotective efficacy. A few aryl hydrocarbon receptor antagonists were developed but the lack of structural information regarding the receptor ligand binding domain resulted in several limitations in the pharmacological properties of these compounds including partial agonism, allosterism, non-selectivity, cytotoxicity and susceptibility to bioactivation. These limitations make the progress of preclinical and clinical assays with the available aryl hydrocarbon receptor antagonists difficult. There is a great interest in developing pure, competitive, selective, nontoxic and resistant to bioactivation aryl hydrocarbon receptor antagonists. Current technology permits he development of pharmacologically ideal antagonists based on the chemical features of the aryl hydrocarbon receptor ligand binding domain. According to these characteristics, chlorinated derivatives of trans-stilbene mew-substituted with electrophilic aromatic directing groups would be effective prototypes for pure, competitive, selective, nontoxic and resistant to bioactivation antagonists for such receptor. (C) 2015 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 13/08216-2 - CRID - Center for Research in Inflammatory Diseases
Grantee:Fernando de Queiroz Cunha
Support type: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 14/17740-0 - Planning, development ánd pharmacological evaluation of new aryl hydrocarbon receptors (AhR) antagonists that are candidates for atheroprotective drugs
Grantee:Larissa Pernomian
Support type: Scholarships in Brazil - Post-Doctorate