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http://dx.doi.org/10.15207/JKCS.2017.8.1.115

The Impact of o-Toluidinyl Structure of 2-Methyl-4-(2-methylphenyldiazenyl)phenyl picolinamide on the AHR Antagonistic Activity  

Lee, Hyosung (Department of Pharmaceutical Science & Engineering, Seowon University)
Publication Information
Journal of the Korea Convergence Society / v.8, no.1, 2017 , pp. 115-121 More about this Journal
Abstract
AHR is a transcription factor activated by aryl hydrocarbons, regulating the expression of XMEs (xenobiotics Metabolizing Enzymes). Even though the role of AHR in human physiology has been intensively investigated for the past decades, our understandings are still largely limited due to the deficiency of adequate chemical agents. In addition, it has been demonstrated that AHR correlates to pathogeneses for some diseases. Furthermore, emerging data suggest that the study on the AHR may provide a valid therapeutic target. Classical antagonists in current use are reported to be partial agonistic whereas a pure antagonist is demanded. In this study, o-toluidinyl ring structure of 2-methyl-4-(2-methylphenyldiazenyl)phenyl picolinamide has been modified into various structures to optimize the AHR antagonistic activity by means of convergence study of organic synthesis and molecular biology.
Keywords
AHR (aryl hydrocarbon receptor); 2-methyl-4-(2-methylphenyldiazenyl)phenyl picolinamide; antagonist; therapeutic target; convergence study of organic synthesis and molecular biology;
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