Pregnane X receptor and drug-induced liver injury

Wang, YM; Chai, SC; Brewer, CT; Chen, T

HERO ID

5077975

Reference Type

Journal Article

Subtype

Review

Year

2014

Language

English

PMID

25252616

HERO ID 5077975
Material Type Review
In Press No
Year 2014
Title Pregnane X receptor and drug-induced liver injury
Authors Wang, YM; Chai, SC; Brewer, CT; Chen, T
Journal Expert Opinion on Drug Metabolism & Toxicology
Volume 10
Issue 11
Page Numbers 1521-1532
Abstract <strong>INTRODUCTION: </strong>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.<br /><br /><strong>AREAS COVERED: </strong>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.<br /><br /><strong>EXPERT OPINION: </strong>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.
Doi 10.1517/17425255.2014.963555
Pmid 25252616
Is Certified Translation No
Dupe Override No
Comments PMC access to author manuscript: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4198438/
Is Public Yes
Language Text English