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2016 ; 1859
(9
): 1141-1154
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Small-molecule modulators of PXR and CAR
#MMPMID26921498
Chai SC
; Cherian MT
; Wang YM
; Chen T
Biochim Biophys Acta
2016[Sep]; 1859
(9
): 1141-1154
PMID26921498
show ga
Two nuclear receptors, the pregnane X receptor (PXR) and the constitutive
androstane receptor (CAR), participate in the xenobiotic detoxification system by
regulating the expression of drug-metabolizing enzymes and transporters in order
to degrade and excrete foreign chemicals or endogenous metabolites. This review
aims to expand the perceived relevance of PXR and CAR beyond their established
role as master xenosensors to disease-oriented areas, emphasizing their
modulation by small molecules. Structural studies of these receptors have
provided much-needed insight into the nature of their binding promiscuity and the
important elements that lead to ligand binding. Reports of species- and
isoform-selective activation highlight the need for further scrutiny when
extrapolating from animal data to humans, as animal models are at the forefront
of early drug discovery. This article is part of a Special Issue entitled:
Xenobiotic nuclear receptors: New Tricks for An Old Dog, edited by Dr. Wen Xie.
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