Dataset Information
Pregnane X receptor and drug-induced liver injury.
Ontology highlight
ABSTRACT: Introduction
The liver plays a central role in transforming and clearing foreign substances. The continuous exposure of the liver to xenobiotics sometimes leads to impaired liver function, referred to as drug-induced liver injury (DILI). The pregnane X receptor (PXR) tightly regulates the expression of genes in the hepatic drug-clearance system and its undesired activation plays a role in DILI.Areas covered
This review focuses on the recent progress in understanding PXR-mediated DILI and highlights the efforts made to assess and manage PXR-mediated DILI during drug development.Expert opinion
Future efforts are needed to further elucidate the mechanisms of PXR-mediated liver injury, including the epigenetic regulation and polymorphisms of PXR. Novel in vitro models containing functional PXR could improve our ability to predict and assess DILI during drug development. PXR inhibitors may provide chemical tools to validate the potential of PXR as a therapeutic target and to develop drugs to be used in the clinic to manage PXR-mediated DILI.
SUBMITTER: Wang YM
PROVIDER: S-EPMC4198438 | biostudies-literature | 2014 Nov
REPOSITORIES: biostudies-literature
Publications
Pregnane X receptor and drug-induced liver injury.
Expert opinion on drug metabolism & toxicology 20140925 11
<h4>Introduction</h4>The liver plays a central role in transforming and clearing foreign substances. The continuous exposure of the liver to xenobiotics sometimes leads to impaired liver function, referred to as drug-induced liver injury (DILI). The pregnane X receptor (PXR) tightly regulates the expression of genes in the hepatic drug-clearance system and its undesired activation plays a role in DILI.<h4>Areas covered</h4>This review focuses on the recent progress in understanding PXR-mediated ...[more]
