The pregnane X receptor: from bench to bedside.
BACKGROUND
The pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved in the response of mammals to their chemical environment.


OBJECTIVE
To summarize the functions and clinical implications of PXR.


METHODS
In the current review, the clinical implications of PXR are discussed, and the use of genetically engineered PXR mouse models is highlighted.


CONCLUSIONS
Recent advances in mouse models, including Pxr-null and PXR-humanized mice, provide in vivo tools for evaluating the physiological functions of PXR and its role in controlling xenobiotic metabolism and transport. By using the PXR knockout and humanized mouse models, PXR was found to influence drug-drug interactions, hepatic steatosis, and the homeostasis of vitamin D, bile acids, and steroid hormones. PXR was also shown to influence inflammatory bowel diseases.
Ma
Xiaochao
X
National Cancer Institute, Laboratory of Metabolism, Center for Cancer Research, National Institutes of Health, Bethesda, MD 20892, USA.
Idle
Jeffrey R
JR
Gonzalez
Frank J
FJ
D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism; D004347:Drug Interactions; D006706:Homeostasis / Q000502:physiology; D006801:Humans; D043183:Irritable Bowel Syndrome / Q000235:genetics / Q000378:metabolism; D008107:Liver Diseases / Q000235:genetics / Q000378:metabolism; D051379:Mice; D018345:Mice, Knockout; D008822:Mice, Transgenic; D004364:Pharmaceutical Preparations / Q000378:metabolism; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000235:genetics* / Q000502:physiology*; D013256:Steroids / Q000378:metabolism; D014807:Vitamin D / Q000502:physiology
D001647:Bile Acids and Salts; C000625852:NR1I2 protein, human; C000625853:Nr1i2 protein, mouse; D004364:Pharmaceutical Preparations; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D013256:Steroids; D014807:Vitamin D