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Study on the Effects of Phenyldiazenylanilines on the Activation of Arylhydrocarbon Receptor

Phenyldiazenylaniline 유도체가 방향족탄화수소 수용체의 활성에 미치는 영향

Lee, Hyosung
이효성

  • Received : 2018.11.15
  • Accepted : 2019.01.20
  • Published : 2019.01.28

Abstract

AHR regulates the expression of xenobiotics metabolizing enzymes (XMEs) as a transcription fact upon binding of ligands that are mainly aryl hydrocarbons. The role of AHR in human physiology has been intensively investigated for the past decades, however our understanding on AHR yet to be elucidated largely due to the lack of proper chemical agents. It has been demonstrated that AHR correlates to pathogenesis for some diseases in recent studies suggesting that the study on the AHR may provide a valid therapeutic target. Classical antagonists in current use are reported to be partially agonistic whereas a pure antagonist is yet to be found. In this study, phenyldiazenylaniline has been designed based on the structure of two known AHR antagonist, Resveratrol and CH223191. The derivatives of phenyldiazenylaniline have been prepared and subjected to assessment as an AHR antagonist in order to optimize the AHR antagonistic activity of the designed structure by means of convergence study of organic synthesis and molecular biology.

Keywords

AHR (aryl hydrocarbon receptor);antagonist;phenyldiazenylanline;proper chemical agent;phenyldiazenylaniline;convergence study of chemical structure and biological activity