• Search Research Projects
  • Search Researchers
  • How to Use
  1. Back to project page

2015 Fiscal Year Final Research Report

Regulation mechanism of drug metabolism enzymes by SCARM and dual ligand of CAR/PXR

Research Project

  • PDF
Project/Area Number 25460175
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Environmental and hygienic pharmacy
Research InstitutionToho University

Principal Investigator

KANNO Yuichiro  東邦大学, 薬学部, 講師 (40453849)

Project Period (FY) 2013-04-01 – 2016-03-31
Keywords核内受容体 / 転写因子 / 遺伝子発現調節 / 生体外異物
Outline of Final Research Achievements

The CAR and PXR regulate various genes involved in xenobiotics and drug metabolism. In many cases, CAR/PXR share ligands termed dual ligands of CAR/PXR. First, we screened compound library to investigate dual ligand of CAR/PXR, we identified Nigramide J and T0901317, as a dual ligand of CAR/PXR. In this study, we established a tetracycline-inducible human CAR and stably human PXR-overexpressing HepG2 cell line (HepTR/hCAR/hPXR) to examine CAR/PXR dual ligands. We investigated the regulation of cytochrome P450 (CYP) 2B6, CYP2C9, CYP3A4, and UDP-glucuronosyl transferase, which are target genes of CAR/PXR, by dual ligands of CAR/PXR in two transfectants. We show that dual ligands of CAR/PXR show distinct gene regulation patterns by crosstalk between CAR and PXR. Furthermore, the two newly established cell lines are useful tools to investigate dual ligands of CAR/PXR.

Free Research Field

薬学

URL: 

Published: 2017-05-10  

Information User Guide FAQ News Terms of Use Attribution of KAKENHI

Powered by NII kakenhi