In the field of molecular biology, nuclear receptors are a class of proteins found within cells that are responsible for sensing steroid and thyroid hormones and certain other molecules. In response, these receptors work with other proteins to regulate the expression of specific genes, thereby controlling the development, homeostasis, and metabolism of the organism.
Nuclear receptors have the ability to directly bind to DNA and regulate the expression of adjacent genes, hence these receptors are classified as transcription factors. The regulation of gene expression by nuclear receptors generally only happens when a ligand is present. More specifically, ligand binding to a nuclear receptor results in a conformational change in the receptor, which, in turn, activates the receptor, resulting in up- or down-regulation of gene expression.
A unique property of nuclear receptors that differentiates them from other classes of receptors is their ability to directly interact with and control the expression of genomic DNA. As a consequence, nuclear receptors play key roles in both embryonic development and adult homeostasis. As discussed below, nuclear receptors may be classified according to either mechanism or homology.
[From Wikipedia, the free encyclopedia]
b7a
c91
fc2
f4a
db8
cd6
a2e
db8
cd6
cd6
a7b
feb
d2d
a2e
a7b
a7b
cd6
a2e
is not affected in human
cd6
e72
e72
a7b
d2d
d2d
d93
a7b
a7b
c02
a9d
inhibition
fc2
a7b
a9d
ed4
db8
feb
c2d
inhibition
c52
cd6
a7b
during fasting
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a10
feb
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fc2
d93
a7b
cd6
cd6
db8
ed4
cd6
cd6
b04
bdd
d52
a7b
cd6
a7b
feb
a7b
cd6
feb
a9d
a9d
cc6
aca
a2e
a7b
plays a role in translocation of CAR
a2e
a7b
cd6
a2e
ed4
a7b
e65
cd6
be4
a7b
a2e
ef9
feb
feb
feb
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ef9
e72
fc2
a7b
a2e
ef9
fc2
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e35
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feb
dc0
feb
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ef9
e72
fc2
d47
c85
feb
fc2
ef9
a2e
e72
Omeprazole, TCDD, PCB
Omeprazole, TCDD, PCB
Omeprazole, TCDD, PCB
a7b
b04
in mice (possibly also in humans?)
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b04
b04
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b04
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dfc
df0
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a2e
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a2e
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bdd
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f4a
cb1
f4a
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bdd
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cd6
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aca
bdd
d52
db8
db8
db8
db8
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a2e
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c02
cd6
cd6
cd6
df0
f65
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d93
d93
d93
d93
regulatory pathway
PW:0000004
Pathway Ontology
transcription factor mediated signaling pathway
PW:0000716
Pathway Ontology
17284330
PubMed
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Steroids
2007
Timsit YE
Negishi M
12120277
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PXR, CAR and drug metabolism.
Nat Rev Drug Discov
2002
Willson TM
Kliewer SA
15501915
PubMed
Chromatin immunoprecipitation (ChIP) scanning identifies primary glucocorticoid receptor target genes.
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2004
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Derynck MK
Nonaka DF
Khodabakhsh DB
Haqq C
Yamamoto KR
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Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
J Biol Chem
2003
Maglich JM
Parks DJ
Moore LB
Collins JL
Goodwin B
Billin AN
Stoltz CA
Kliewer SA
Lambert MH
Willson TM
Moore JT
19321346
PubMed
NRF2 and KEAP1 mutations: permanent activation of an adaptive response in cancer.
Trends Biochem Sci
2009
Hayes JD
McMahon M
19129222
PubMed
Identification of pregnane-X receptor target genes and coactivator and corepressor binding to promoter elements in human hepatocytes.
Nucleic Acids Res
2009
Hariparsad N
Chu X
Yabut J
Labhart P
Hartley DP
Dai X
Evers R
11991950
PubMed
Expression of CYP3A4, CYP2B6, and CYP2C9 is regulated by the vitamin D receptor pathway in primary human hepatocytes.
J Biol Chem
2002
Drocourt L
Ourlin JC
Pascussi JM
Maurel P
Vilarem MJ
12573484
PubMed
The expression of CYP2B6, CYP2C9 and CYP3A4 genes: a tangle of networks of nuclear and steroid receptors.
Biochim Biophys Acta
2003
Pascussi JM
Gerbal-Chaloin S
Drocourt L
Maurel P
Vilarem MJ
17901129
PubMed
Genome-wide identification of estrogen receptor alpha-binding sites in mouse liver.
Mol Endocrinol
2008
Gao H
Faelt S
Sandelin A
Gustafsson JA
Dahlman-Wright K
20619336
PubMed
Involvement of aryl hydrocarbon receptor in basal and 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced expression of target genes in primary human hepatocytes.
Toxicol In Vitro
2010
Le Vee M
Jouan E
Fardel O
20399894
PubMed
Bile acids and their nuclear receptor FXR: Relevance for hepatobiliary and gastrointestinal disease.
Biochim Biophys Acta
2010
Gadaleta RM
van Mil SW
Oldenburg B
Siersema PD
Klomp LW
van Erpecum KJ
15581595
PubMed
Regulatory network of lipid-sensing nuclear receptors: roles for CAR, PXR, LXR, and FXR.
Arch Biochem Biophys
2005
Handschin C
Meyer UA
18288955
PubMed
Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues.
Curr Drug Metab
2008
Pavek P
Dvorak Z
21420387
PubMed
From differential induction of UDP-glucuronosyltransferases in rat liver to characterization of responsible ligand-activated transcription factors, and their multilevel crosstalk in humans.
Biochem Pharmacol
2011
Bock KW
12573486
PubMed
Functional role of AhR in the expression of toxic effects by TCDD.
Biochim Biophys Acta
2003
Mimura J
Fujii-Kuriyama Y
16289099
PubMed
Over-production of IFN-gamma and IL-12 in AhR-null mice.
FEBS Lett
2005
Rodriguez-Sosa M
Elizondo G
Lopez-Duran RM
Rivera I
Gonzalez FJ
Vega L
15598615
PubMed
Subchronic exposure to TCDD, PeCDF, PCB126, and PCB153: effect on hepatic gene expression.
Environ Health Perspect
2004
Vezina CM
Walker NJ
Olson JR
17595319
PubMed
The xenobiotic-sensing nuclear receptors pregnane X receptor, constitutive androstane receptor, and orphan nuclear receptor hepatocyte nuclear factor 4alpha in the regulation of human steroid-/bile acid-sulfotransferase.
Mol Endocrinol
2007
Echchgadda I
Song CS
Oh T
Ahmed M
De La Cruz IJ
Chatterjee B
21908933
PubMed
Crosstalk of thyroid hormone receptor and liver X receptor in lipid metabolism and beyond [Review].
Endocr J
2011
Hashimoto K
Mori M
19106115
PubMed
Mechanism of vitamin D receptor inhibition of cholesterol 7alpha-hydroxylase gene transcription in human hepatocytes.
Drug Metab Dispos
2009
Han S
Chiang JY
15923610
PubMed
The GI-GPx gene is a target for Nrf2.
Mol Cell Biol
2005
Banning A
Deubel S
Kluth D
Zhou Z
Brigelius-Flohé R
15004031
PubMed
The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction.
J Biol Chem
2004
Maglich JM
Watson J
McMillen PJ
Goodwin B
Willson TM
Moore JT
21189866
PubMed
Nrf2 target genes are induced under marginal selenium-deficiency.
Genes Nutr
2010
Mueller M
Banning A
Brigelius-FlohÃÆâ€â„ÃÃÆâ€Ã