Bisphenol A and its analogues activate human pregnane X receptor.

ABSTRACT:

Background

Bisphenol A (BPA) is a base chemical used extensively in many consumer products. BPA and its analogues are present in environmental and human samples. Many endocrine-disrupting chemicals, including BPA, have been shown to activate the pregnane X receptor (PXR), a nuclear receptor that functions as a master regulator of xenobiotic metabolism. However, the detailed mechanism by which these chemicals activate PXR remains unknown.

Objective

We investigated the mechanism by which BPA interacts with and activates PXR and examined selected BPA analogues to determine whether they bind to and activate PXR.

Methods

Cell-based reporter assays, in silico ligand-PXR docking studies, and site-directed mutagenesis were combined to study the interaction between BPA and PXR

SUBMITTER: Sui Y 

PROVIDER: S-EPMC3295358 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature