IUPHAR DATABASE | 1H. Liver X receptor-like receptors

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Farnesoid X receptor

Systematic Nomenclature: NR1H4

Family: 1H. Liver X receptor-like receptors

Contents:

Gene and Protein Information

Previous and Unofficial Names

Database Links

Selected 3D Structures

Physiological Consequences of Altering Gene Expression

Phenotypes, Alleles and Disease Models

References

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

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	11180 (Hs)
DrugBank Target	3233 (Hs)
Ensembl	ENSG00000012504 (Hs), ENSMUSG00000047638 (Mm), ENSRNOG00000007197 (Rn)
Entrez Gene	9971 (Hs), 20186 (Mm), 60351 (Rn)
GeneCards	NR1H4 (Hs)
GenitoUrinary Development Molecular Anatomy Project	Nr1h4 (Mm)
HomoloGene	3760 (Hs)
Human Protein Reference Database	04827 (Hs)
InterPro	Q96RI1 (Hs), Q3V1T8 (Mm), Q62735 (Rn)
KEGG Gene	hsa:9971 (Hs), mmu:20186 (Mm), rno:60351 (Rn)
NURSA Receptor	1H4
OMIM	603826 (Hs)
PharmGKB Gene	PA31752 (Hs)
PhosphoSitePlus	Q96RI1 (Hs), Q60641 (Mm), Q62735 (Rn)
RefSeq Nucleotide	NM_005123 (Hs), NP_001157172 (Mm), NM_021745 (Rn)
RefSeq Protein	NP_005114 (Hs), NP_001156976 (Mm), NP_001157172 (Mm), NP_033134 (Mm), NP_068513 (Rn)
TreeFam	ENSG00000012504 (Hs), ENSMUSG00000047638 (Mm), ENSRNOG00000007197 (Rn)
UniProt	Q96RI1 (Hs), Q3V1T8 (Mm), Q62735 (Rn)
	1H. Liver X receptor-like receptors

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
Resolution:	2.9Å
Species:	Rat
References:	27

Search for other structures on the PDB

Search by keyword: Farnesoid X receptor

Search by accession number: Q96RI1, Q62735, Q3V1T8

Natural/Endogenous Ligand(s)
Comments: A series of bile acids are natural ligands

Potency order (Human)
chenodeoxycholic acid > lithocholic acid, deoxycholic acid [25,28]

Potency order (Human)

chenodeoxycholic acid > lithocholic acid, deoxycholic acid [25,28]

Agonists

Key to terms and symbols

View all chemical structures

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Ligand	Sp.	Action	Affinity	Units	Reference
GW4064	Hs	Agonist	7.82	pEC₅₀	26
ECDCA	Hs	Agonist	7.0	pEC₅₀	29
fexaramine	Hs	Agonist	6.6	pEC₅₀	7
22R-hydroxycholesterol	Hs	Agonist	5.5	pEC₅₀	6
chenodeoxycholic acid	?	Agonist	5.31	pEC₅₀	23,28,38
lithocholic acid	?	Agonist	5.3	pEC₅₀	25,28,38
cholic acid	?	Agonist	5.0 – 4.0	pEC₅₀	28,38
deoxycholic acid	?	Agonist	4.0	pEC₅₀	23,28,38

View species-specific agonist tables

Antagonists

Key to terms and symbols

View all chemical structures

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Ligand					Sp.	Action	Affinity	Units	Reference
guggulsterone					Mm	Antagonist	5.0	pEC₅₀	37
guggulsterone					Hs	Antagonist	5.7 – 6.0	pIC₅₀	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
KNG1	Human	Activated	Transient transfection, EMSA		5
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
VLDLR	Human	Activated			4
Fibrinogen	Human	Activated			2
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

Click here to show/hide data

Allele	Composition & genetic background	Accession	Phenotype Id	Phenotype	Reference
Nr1h4^tm1Kok	Nr1h4^tm1Kok/Nr1h4^tm1Kok involves: 129P2/OlaHsd * C57BL/6J	MGI:1352464	MP:0004773	abnormal bile composition	PMID: 12917447
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: 129X1/SvJ	MGI:1352464	MP:0004773	abnormal bile composition	PMID: 17720959
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0005365	abnormal bile salt homeostasis	PMID: 11030617
Nr1h4^tm1Kok	Nr1h4^tm1Kok/Nr1h4^tm1Kok involves: 129P2/OlaHsd * C57BL/6J	MGI:1352464	MP:0005365	abnormal bile salt homeostasis	PMID: 12917447
Nr1h4^tm1.1Gonz\|Tg(Vil-cre)997Gum	Nr1h4^tm1.1Gonz/Nr1h4^tm1.1Gonz,Tg(Vil-cre)997Gum/0 involves: 129X1/SvJ * C57BL/6 * SJL	MGI:1352464 MGI:2446957	MP:0005365	abnormal bile salt homeostasis	PMID: 17720959
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0004774	abnormal bile salt level	PMID: 11030617
Nr1h4^tm1Kok	Nr1h4^tm1Kok/Nr1h4^tm1Kok involves: 129P2/OlaHsd * C57BL/6J	MGI:1352464	MP:0004772	abnormal bile secretion	PMID: 12917447
Nr1h4^tm1Kok	Nr1h4^tm1Kok/Nr1h4^tm1Kok involves: 129P2/OlaHsd * C57BL/6J	MGI:1352464	MP:0009642	abnormal blood homeostasis	PMID: 12917447
Nr1h4^tm1.2Auw	Nr1h4^tm1.2Auw/Nr1h4^tm1.2Auw involves: 129/Sv * C57BL/6J	MGI:1352464	MP:0000607	abnormal hepatocyte morphology	PMID: 19815629
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0000598	abnormal liver morphology	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0005150	cachexia	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0005534	decreased body temperature	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0010182	decreased susceptibility to weight gain	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0002628	hepatic steatosis	PMID: 11030617
Nr1h4^tm1Kok	Nr1h4^tm1Kok/Nr1h4^tm1Kok involves: 129P2/OlaHsd * C57BL/6J	MGI:1352464	MP:0004789	increased bile salt level	PMID: 12917447
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: 129X1/SvJ	MGI:1352464	MP:0004789	increased bile salt level	PMID: 17720959
Nr1h4^tm1.1Gonz\|Tg(Vil-cre)997Gum	Nr1h4^tm1.1Gonz/Nr1h4^tm1.1Gonz,Tg(Vil-cre)997Gum/0 involves: 129X1/SvJ * C57BL/6 * SJL	MGI:1352464 MGI:2446957	MP:0004789	increased bile salt level	PMID: 17720959
Nr1h4^tm1.1Gonz\|Tg(Alb1-cre)1Dlr	Nr1h4^tm1.1Gonz/Nr1h4^tm1.1Gonz,Tg(Alb1-cre)1Dlr/0 involves: 129X1/SvJ * C57BL/6	MGI:1352464 MGI:2176944	MP:0004789	increased bile salt level	PMID: 17720959
Nr1h4^tm1.2Auw	Nr1h4^tm1.2Auw/Nr1h4^tm1.2Auw involves: 129/Sv * C57BL/6J	MGI:1352464	MP:0004789	increased bile salt level	PMID: 19815629
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz STOCK Nr1h4/J	MGI:1352464	MP:0002941	increased circulating alanine transaminase level	PMID: 18820241
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz STOCK Nr1h4/J	MGI:1352464	MP:0005343	increased circulating aspartate transaminase level	PMID: 18820241
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0005178	increased circulating cholesterol level	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: 129X1/SvJ	MGI:1352464	MP:0005178	increased circulating cholesterol level	PMID: 17720959
Nr1h4^tm1.1Gonz\|Tg(Alb1-cre)1Dlr	Nr1h4^tm1.1Gonz/Nr1h4^tm1.1Gonz,Tg(Alb1-cre)1Dlr/0 involves: 129X1/SvJ * C57BL/6	MGI:1352464 MGI:2176944	MP:0005178	increased circulating cholesterol level	PMID: 17720959
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz STOCK Nr1h4/J	MGI:1352464	MP:0005178	increased circulating cholesterol level	PMID: 18820241
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0003980	increased circulating phospholipid level	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0001552	increased circulating triglyceride level	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: 129X1/SvJ	MGI:1352464	MP:0001552	increased circulating triglyceride level	PMID: 17720959
Nr1h4^tm1.1Gonz\|Tg(Alb1-cre)1Dlr	Nr1h4^tm1.1Gonz/Nr1h4^tm1.1Gonz,Tg(Alb1-cre)1Dlr/0 involves: 129X1/SvJ * C57BL/6	MGI:1352464 MGI:2176944	MP:0001552	increased circulating triglyceride level	PMID: 17720959
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz STOCK Nr1h4/J	MGI:1352464	MP:0001552	increased circulating triglyceride level	PMID: 18820241
Nr1h4^tm1.2Auw	Nr1h4^tm1.2Auw/Nr1h4^tm1.2Auw involves: 129/Sv * C57BL/6J	MGI:1352464	MP:0003887	increased hepatocyte apoptosis	PMID: 19815629
Nr1h4^tm1.2Auw	Nr1h4^tm1.2Auw/Nr1h4^tm1.2Auw involves: 129/Sv * C57BL/6J	MGI:1352464	MP:0003893	increased hepatocyte proliferation	PMID: 19815629
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0010027	increased liver cholesterol level	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0009355	increased liver triglyceride level	PMID: 11030617
Nr1h4^tm1Gonz	Nr1h4^tm1Gonz/Nr1h4^tm1Gonz involves: C57BL/6N	MGI:1352464	MP:0009763	increased sensitivity to induced morbidity/mortality	PMID: 11030617

REFERENCES

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1. Ananthanarayanan, M; Li, S; Balasubramaniyan, N; Suchy, FJ; Walsh, MJ. (2004) Ligand-dependent activation of the farnesoid X-receptor directs arginine methylation of histone H3 by CARM1. J. Biol. Chem., 279 (52): 54348-57. [PMID:15471871]

2. Anisfeld, AM; Kast-Woelbern, HR; Lee, H; Zhang, Y; Lee, FY; Edwards, PA. (2005) Activation of the nuclear receptor FXR induces fibrinogen expression: a new role for bile acid signaling. J. Lipid Res., 46 (3): 458-68. [PMID:15604525]

3. Chignard, N; Mergey, M; Barbu, V; Finzi, L; Tiret, E; Paul, A; Housset, C. (2005) VPAC1 expression is regulated by FXR agonists in the human gallbladder epithelium. Hepatology, 42 (3): 549-57. [PMID:16037943]

4. Claudel, T; Sturm, E; Duez, H; Torra, IP; Sirvent, A; Kosykh, V; Fruchart, JC; Dallongeville, J; Hum, DW; Kuipers, F; Staels, B. (2002) Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element. J. Clin. Invest., 109 (7): 961-71. [PMID:11927623]

5. Cui, J; Huang, L; Zhao, A; Lew, JL; Yu, J; Sahoo, S; Meinke, PT; Royo, I; Pelaez, F; Wright, SD. (2003) Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump. J. Biol. Chem., 278 (12): 10214-20. [PMID:12525500]

6. Deng, R; Yang, D; Yang, J; Yan, B. (2006) Oxysterol 22(R)-hydroxycholesterol induces the expression of the bile salt export pump through nuclear receptor farsenoid X receptor but not liver X receptor. J. Pharmacol. Exp. Ther., 317 (1): 317-25. [PMID:16371446]

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12. Holt, JA; Luo, G; Billin, AN; Bisi, J; McNeill, YY; Kozarsky, KF; Donahee, M; Wang, DY; Mansfield, TA; Kliewer, SA; Goodwin, B; Jones, SA. (2003) Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesis. Genes Dev., 17 (13): 1581-91. [PMID:12815072]

13. Inagaki, T; Choi, M; Moschetta, A; Peng, L; Cummins, CL; McDonald, JG; Luo, G; Jones, SA; Goodwin, B; Richardson, JA; Gerard, RD; Repa, JJ; Mangelsdorf, DJ; Kliewer, SA. (2005) Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis. Cell Metab., 2 (4): 217-25. [PMID:16213224]

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15. Jung, D; Podvinec, M; Meyer, UA; Mangelsdorf, DJ; Fried, M; Meier, PJ; Kullak-Ublick, GA. (2002) Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor. Gastroenterology, 122 (7): 1954-66. [PMID:12055601]

16. Kanaya, E; Shiraki, T; Jingami, H. (2004) The nuclear bile acid receptor FXR is activated by PGC-1alpha in a ligand-dependent manner. Biochem. J., 382 (Pt 3): 913-21. [PMID:15202934]

17. Kast, HR; Nguyen, CM; Sinal, CJ; Jones, SA; Laffitte, BA; Reue, K; Gonzalez, FJ; Willson, TM; Edwards, PA. (2001) Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids. Mol. Endocrinol., 15 (10): 1720-8. [PMID:11579204]

18. Kok, T; Hulzebos, CV; Wolters, H; Havinga, R; Agellon, LB; Stellaard, F; Shan, B; Schwarz, M; Kuipers, F. (2003) Enterohepatic circulation of bile salts in farnesoid X receptor-deficient mice: efficient intestinal bile salt absorption in the absence of ileal bile acid-binding protein. J. Biol. Chem., 278 (43): 41930-7. [PMID:12917447]

19. Landrier, JF; Eloranta, JJ; Vavricka, SR; Kullak-Ublick, GA. (2006) The nuclear receptor for bile acids, FXR, transactivates human organic solute transporter-alpha and -beta genes. Am. J. Physiol. Gastrointest. Liver Physiol., 290 (3): G476-85. [PMID:16269519]

20. Lee, FY; Kast-Woelbern, HR; Chang, J; Luo, G; Jones, SA; Fishbein, MC; Edwards, PA. (2005) Alpha-crystallin is a target gene of the farnesoid X-activated receptor in human livers. J. Biol. Chem., 280 (36): 31792-800. [PMID:16012168]

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24. Mak, PA; Kast-Woelbern, HR; Anisfeld, AM; Edwards, PA. (2002) Identification of PLTP as an LXR target gene and apoE as an FXR target gene reveals overlapping targets for the two nuclear receptors. J. Lipid Res., 43 (12): 2037-41. [PMID:12454263]

25. Makishima, M; Okamoto, AY; Repa, JJ; Tu, H; Learned, RM; Luk, A; Hull, MV; Lustig, KD; Mangelsdorf, DJ; Shan, B. (1999) Identification of a nuclear receptor for bile acids. Science, 284 (5418): 1362-5. [PMID:10334992]

26. Maloney, PR; Parks, DJ; Haffner, CD; Fivush, AM; Chandra, G; Plunket, KD; Creech, KL; Moore, LB; Wilson, JG; Lewis, MC; Jones, SA; Willson, TM. (2000) Identification of a chemical tool for the orphan nuclear receptor FXR. J. Med. Chem., 43 (16): 2971-4. [PMID:10956205]

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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 01/04/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=603.

1H. Liver X receptor-like receptors
	Introduction
	Contributors
	References
	Farnesoid X receptor
	Farnesoid X receptor-β
	Liver X receptor-α
	Liver X receptor-β