Nomenclature: Farnesoid X receptor

Systematic Nomenclature: NR1H4

Family: 1H. Liver X receptor-like receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

Gene and Protein Information
Species AA Chromosomal Location Gene Symbol Gene Name Reference
Human 472 12q23.1 NR1H4 nuclear receptor subfamily 1, group H, member 4 8
Mouse 488 10 50.0 cM Nr1h4 nuclear receptor subfamily 1, group H, member 4 34
Rat 469 7q13 Nr1h4 nuclear receptor subfamily 1, group H, member 4 8
Previous and Unofficial Names
FXR
RIP14
HRR1
HRR-1
FXRα
Bile acid receptor
MGC94878
RXR-interacting protein 14
farnesoid X activated receptor
farnesoid X-activated receptor
farnesol receptor HRR-1
nuclear receptor subfamily 1, group H, member 4
retinoid X receptor-interacting protein 14
Rxrip14
AI957360
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
NURSA Receptor
OMIM
Orphanet Gene
PharmGKB Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Bile Acid Receptor ligand binding domain - cocrystallised with agonist
PDB Id:  1OT7
Ligand:  chenodeoxycholic acid   This ligand is endogenous
Resolution:  2.9Å
Species:  Rat
References:  27
Natural/Endogenous Ligands
Comments: A series of bile acids are natural ligands
Potency order (Human)
chenodeoxycholic acid > lithocholic acid, deoxycholic acid  [25,28]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GW4064 Hs Agonist 7.8 pEC50 26
pEC50 7.8 [26]
ECDCA Hs Agonist 7.0 pEC50 29
pEC50 7.0 (EC50 9.9x10-8 M) [29]
fexaramine Hs Agonist 6.6 pEC50 7
pEC50 6.6 [7]
22R-hydroxycholesterol Hs Agonist 5.5 pEC50 6
pEC50 5.5 [6]
lithocholic acid N/A Agonist 5.3 pEC50 25,28,38
pEC50 5.3 [25,28,38]
chenodeoxycholic acid Hs Agonist 5.3 pEC50 28,38
pEC50 5.3 [28,38]
cholic acid N/A Agonist 5.0 – 4.0 pEC50 28,38
pEC50 5.0 – 4.0 [28,38]
deoxycholic acid N/A Agonist 4.0 pEC50 23,28,38
pEC50 4.0 [23,28,38]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
guggulsterone Mm Antagonist 5.0 pEC50 37
pEC50 5.0 [37]
guggulsterone Hs Antagonist 5.7 – 6.0 pIC50 39
pIC50 5.7 – 6.0 (IC50 2x10-6 – 1x10-6 M) [39]
View species-specific antagonist tables
DNA Binding
Structure:  RXR partner
HRE core sequence:  AGTTCAnTGAACT
Response element:  Other - see comments
DNA Binding Comments
FXR binds IR1
Main Co-regulators
Name Activity Specific Ligand dependent AF-2 dependent Comments References
PPARGC1A Co-activator No Yes Yes 16,33,40
NCOA1 Co-activator No Yes Yes 25,28
MED1 Co-activator No Yes Yes 30
CARM1 Co-activator No Yes Yes 1
PRMT1 Co-activator No Yes No 32
TRRAP Co-activator No Yes No 36
Main Target Genes
Name Species Effect Technique Comments References
VLDLR Human Activated 4
NR0B2 Human Activated Transient transfection, EMSA NR0B2 is a nuclear receptor also commonly known as short heterodimer partner (SHP) 10,22
ABCB11 Human Activated Transient transfection, EMSA progressive familial intrahepatic cholestasis 2, bile salt export pump 1
FABP6 Human Activated Transient transfection, EMSA Fatty acid binding protein 6, ileal 11
ABCB4 Human Activated Transient transfection, EMSA 5
FGF19 Human Activated Transient transfection, EMSA 12
ABCC2 Human Activated Transient transfection, EMSA multidrug resistance associated protein 2 (MRP2multidrug resistance associated protein 2 (MRP2) 24
SLCO1B3 Human Activated Transient transfection, EMSA solute carrier organic anion transporter family member 1B3 (OATP1B3; SLCO1B3) 15
SLC27A5 Human Activated Transient transfection, EMSA bile acid-CoA synthetase (BACS) 31
SLC3A1 Human Activated Transient transfection, EMSA bile acid-CoA: amino acid N-acetyltransferase (BAT) 31
APOAI Human Repressed Transient transfection, EMSA apolipoprotein A-I (APOAI): Repressed by FXR binding as a monomer to negative FXR response element. 4
APOC2 Human Repressed Transient transfection, EMSA apolipoprotein C-II (ApoCII) 17
APOE Human Activated APOE- apolipoprotein E. 24
C3 Human Activated Transient transfection, EMSA complement component 3 21
PDK4 Human Activated pyruvate dehydrogenase kinase, isozyme 4 33
PLTP Human Activated Transient transfection, EMSA phospholipid transfer protein 37
PPARA Human Activated Transient transfection, EMSA The mouse PPARa gene is not induced. 30
Fibrinogen Human Activated 2
KNG1 Human Activated Transient transfection, EMSA 5
SDC1 Human Activated Transient transfection, EMSA CD138, syndecan-1, SYND1 7
VIPR1 Human Activated 3
alpha-crystallin Human Activated Transient transfection, EMSA 20
organic solute transporter α-β Human Activated 9,19,42
Abcb4 Mouse Activated Transient transfection, EMSA 13-14
Apoc3 Mouse Repressed ChIP, Transient transfection, EMSA 4
Tissue Distribution
Liver, small intestine, colon, kidney and adrenal
Expression level:  High
Species:  Mouse
Technique:  In situ hybridisation,Q-PCR, Northern Blot.
References:  8,34,41
Physiological Consequences of Altering Gene Expression
FXR-null mice have elevated serum bile acids, cholesterol, and triglycerides, increased hepatic cholesterol and triglycerides, and a proatherogenic serum lipoprotein profile. The also have reduced bile acid pools and reduced fecal bile acid excretion, and are susceptible to cholesterol gallstone disease.
Species:  Mouse
Tissue:  Various
Technique:  Gene knockout
References:  18,35
Phenotypes, Alleles and Disease Models Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Nr1h4tm1Kok Nr1h4tm1Kok/Nr1h4tm1Kok
involves: 129P2/OlaHsd * C57BL/6J
MGI:1352464  MP:0004773 abnormal bile composition PMID: 12917447 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: 129X1/SvJ
MGI:1352464  MP:0004773 abnormal bile composition PMID: 17720959 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0005365 abnormal bile salt homeostasis PMID: 11030617 
Nr1h4tm1Kok Nr1h4tm1Kok/Nr1h4tm1Kok
involves: 129P2/OlaHsd * C57BL/6J
MGI:1352464  MP:0005365 abnormal bile salt homeostasis PMID: 12917447 
Nr1h4tm1.1Gonz|Tg(Vil-cre)997Gum Nr1h4tm1.1Gonz/Nr1h4tm1.1Gonz,Tg(Vil-cre)997Gum/0
involves: 129X1/SvJ * C57BL/6 * SJL
MGI:1352464  MGI:2446957  MP:0005365 abnormal bile salt homeostasis PMID: 17720959 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0004774 abnormal bile salt level PMID: 11030617 
Nr1h4tm1Kok Nr1h4tm1Kok/Nr1h4tm1Kok
involves: 129P2/OlaHsd * C57BL/6J
MGI:1352464  MP:0004772 abnormal bile secretion PMID: 12917447 
Nr1h4tm1Kok Nr1h4tm1Kok/Nr1h4tm1Kok
involves: 129P2/OlaHsd * C57BL/6J
MGI:1352464  MP:0009642 abnormal blood homeostasis PMID: 12917447 
Nr1h4tm1.2Auw Nr1h4tm1.2Auw/Nr1h4tm1.2Auw
involves: 129/Sv * C57BL/6J
MGI:1352464  MP:0000607 abnormal hepatocyte morphology PMID: 19815629 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0000598 abnormal liver morphology PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0005150 cachexia PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0005534 decreased body temperature PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0010182 decreased susceptibility to weight gain PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0002628 hepatic steatosis PMID: 11030617 
Nr1h4tm1Kok Nr1h4tm1Kok/Nr1h4tm1Kok
involves: 129P2/OlaHsd * C57BL/6J
MGI:1352464  MP:0004789 increased bile salt level PMID: 12917447 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: 129X1/SvJ
MGI:1352464  MP:0004789 increased bile salt level PMID: 17720959 
Nr1h4tm1.1Gonz|Tg(Vil-cre)997Gum Nr1h4tm1.1Gonz/Nr1h4tm1.1Gonz,Tg(Vil-cre)997Gum/0
involves: 129X1/SvJ * C57BL/6 * SJL
MGI:1352464  MGI:2446957  MP:0004789 increased bile salt level PMID: 17720959 
Nr1h4tm1.1Gonz|Tg(Alb1-cre)1Dlr Nr1h4tm1.1Gonz/Nr1h4tm1.1Gonz,Tg(Alb1-cre)1Dlr/0
involves: 129X1/SvJ * C57BL/6
MGI:1352464  MGI:2176944  MP:0004789 increased bile salt level PMID: 17720959 
Nr1h4tm1.2Auw Nr1h4tm1.2Auw/Nr1h4tm1.2Auw
involves: 129/Sv * C57BL/6J
MGI:1352464  MP:0004789 increased bile salt level PMID: 19815629 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
STOCK Nr1h4/J
MGI:1352464  MP:0002941 increased circulating alanine transaminase level PMID: 18820241 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
STOCK Nr1h4/J
MGI:1352464  MP:0005343 increased circulating aspartate transaminase level PMID: 18820241 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0005178 increased circulating cholesterol level PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: 129X1/SvJ
MGI:1352464  MP:0005178 increased circulating cholesterol level PMID: 17720959 
Nr1h4tm1.1Gonz|Tg(Alb1-cre)1Dlr Nr1h4tm1.1Gonz/Nr1h4tm1.1Gonz,Tg(Alb1-cre)1Dlr/0
involves: 129X1/SvJ * C57BL/6
MGI:1352464  MGI:2176944  MP:0005178 increased circulating cholesterol level PMID: 17720959 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
STOCK Nr1h4/J
MGI:1352464  MP:0005178 increased circulating cholesterol level PMID: 18820241 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0003980 increased circulating phospholipid level PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0001552 increased circulating triglyceride level PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: 129X1/SvJ
MGI:1352464  MP:0001552 increased circulating triglyceride level PMID: 17720959 
Nr1h4tm1.1Gonz|Tg(Alb1-cre)1Dlr Nr1h4tm1.1Gonz/Nr1h4tm1.1Gonz,Tg(Alb1-cre)1Dlr/0
involves: 129X1/SvJ * C57BL/6
MGI:1352464  MGI:2176944  MP:0001552 increased circulating triglyceride level PMID: 17720959 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
STOCK Nr1h4/J
MGI:1352464  MP:0001552 increased circulating triglyceride level PMID: 18820241 
Nr1h4tm1.2Auw Nr1h4tm1.2Auw/Nr1h4tm1.2Auw
involves: 129/Sv * C57BL/6J
MGI:1352464  MP:0003887 increased hepatocyte apoptosis PMID: 19815629 
Nr1h4tm1.2Auw Nr1h4tm1.2Auw/Nr1h4tm1.2Auw
involves: 129/Sv * C57BL/6J
MGI:1352464  MP:0003893 increased hepatocyte proliferation PMID: 19815629 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0010027 increased liver cholesterol level PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0009355 increased liver triglyceride level PMID: 11030617 
Nr1h4tm1Gonz Nr1h4tm1Gonz/Nr1h4tm1Gonz
involves: C57BL/6N
MGI:1352464  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 11030617 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Intrahepatic cholestasis of pregnancy
Orphanet:  69665
References: 
Mutations not determined

REFERENCES

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To cite this database page, please use the following:

1H. Liver X receptor-like receptors: Farnesoid X receptor. Last modified on 14/03/2014. Accessed on 30/10/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=603.

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