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Annu Rev Pharmacol Toxicol. 2016;56:605-626. doi: 10.1146/annurev-pharmtox-010715-103209.

Nuclear Receptors as Therapeutic Targets in Liver Disease: Are We There Yet?

Author information

1
Department of Physiology and Neurobiology and The Institute for Systems Genomics, University of Connecticut, Storrs, Connecticut 06269.
2
Veterans Affairs Connecticut Healthcare System, West Haven, Connecticut 06516.
3
Department of Internal Medicine, Section of Digestive Diseases, Yale University, New Haven, Connecticut 06520.
#
Contributed equally

Abstract

Nuclear receptors (NR) are ligand-modulated transcription factors that play diverse roles in cell differentiation, development, proliferation, and metabolism and are associated with numerous liver pathologies such as cancer, steatosis, inflammation, fibrosis, cholestasis, and xenobiotic/drug-induced liver injury. The network of target proteins associated with NRs is extremely complex, comprising coregulators, small noncoding microRNAs, and long noncoding RNAs. The importance of NRs as targets of liver disease is exemplified by the number of NR ligands that are currently used in the clinics or in clinical trials with promising results. Understanding the regulation by NR during pathophysiological conditions, and identifying ligands for orphan NR, points to a potential therapeutic approach for patients with liver diseases. An overview of complex NR metabolic networks and their pharmacological implications in liver disease is presented here.

KEYWORDS:

cholestatic liver disease; drug-induced liver injury; hepatocellular cancer; liver inflammation and fibrosis; nonalcoholic fatty liver; viral hepatitis infection

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