Date of Award
Master of Science (MS)
Molecular Therapeutics and Cell Signaling
Taosheng Chen, Ph.D.
David R. Nelson, Ph.D. Bing Yan, Ph.D. Xin Zhang, Ph.D.
Antagonist; Human PXR; Reporter Gene Assay
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.
Lei, Fang , "Studying the Specificity of hPXR Antagonists Using a Panel of Cell-based Assays" (2009). Theses and Dissertations (ETD). Paper 143. http://dx.doi.org/10.21007/etd.cghs.2009.0179.