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Article

International Union of Pharmacology. LXII. The NR1H and NR1I Receptors: Constitutive Androstane Receptor, Pregnene X Receptor, Farnesoid X Receptor , Farnesoid X Receptor , Liver X Receptor , Liver X Receptor , and Vitamin D Receptor

Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, Texas (D.D.M., R.X.); The Institute of Molecular and Cellular Biosciences, The University of Tokyo, Tokyo, Japan (S.K.); Center for Pharmacogenetics, University of Pittsburgh, Pittsburgh, Pennsylvania (W.X.); Howard Hughes Medical Institute, Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas (D.J.M., D.R.S.); and Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas (D.J.M., D.R.S., S.A.K.)

Abstract

Introduction

Structures

LXRalpha and beta

FXRalpha

VDR

CAR

PXR

Endogenous Ligands

LXRalpha and beta

FXRalpha

VDR

PXR and CAR

Synthetic Ligands and Selective Modulators

LXRalpha and beta

FXRalpha

VDR

PXR and CAR

Genetics

LXRalpha and beta

FXRalpha and beta

VDR

PXR and CAR

The nuclear receptors of the NR1H and NR1I subgroups include the constitutive androstane receptor, pregnane X receptor, farnesoid X receptors, liver X receptors, and vitamin D receptor. The newly emerging functions of these related receptors are under the control of metabolic pathways, including metabolism of xenobiotics, bile acids, cholesterol, and calcium. This review summarizes results of structural, pharmacologic, and genetic studies of these receptors.

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