Date of Award

5-2009

Document Type

Thesis

Degree Name

Master of Science (MS)

Program

Biomedical Sciences

Track

Molecular Therapeutics and Cell Signaling

Research Advisor

Taosheng Chen, Ph.D.

Committee

David R. Nelson, Ph.D. Bing Yan, Ph.D. Xin Zhang, Ph.D.

Keywords

Antagonist; Human PXR; Reporter Gene Assay

Abstract

The pregnane X receptor (PXR or SXR; NR1I2) is a member of the nuclear receptor superfamily. It activates the transcription of a large network of genes including cytochrome P450 (CYP) and Mdr1 which play critical roles in chemicals metabolism and transportation. Induction of CYPs contributes to adverse drug-drug interactions. Non-toxic, PXR-specific antagonists will be valuable in attenuating the adverse drug-drug interaction which is the cause of many treatment failures in clinic. However, few hPXR antagonists were reported particularly the specific ones. In this thesis a reporter gene assay was used to study the specificity of hPXR antagonists from a panel of compounds that have been previously indentified as non-toxic hPXR antagonists.

DOI

10.21007/etd.cghs.2009.0179

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