Top ▲

Liver X receptor-α

Click here for help

Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 602

Nomenclature: Liver X receptor-α

Systematic Nomenclature: NR1H3

Family: 1H. Liver X receptor-like receptors

Gene and Protein Information Click here for help
Species AA Chromosomal Location Gene Symbol Gene Name Reference
Human 447 11p11.2 NR1H3 nuclear receptor subfamily 1 group H member 3 46
Mouse 445 2 50.52 cM Nr1h3 nuclear receptor subfamily 1, group H, member 3 1
Rat 445 3q24 Nr1h3 nuclear receptor subfamily 1, group H, member 3 2
Previous and Unofficial Names Click here for help
RLD-1 | LXRα | Oxysterols receptor α | liver X receptor alpha | nuclear orphan receptor LXR-alpha | oxysterols receptor LXR-alpha | nuclear receptor subfamily 1
Database Links Click here for help
Alphafold
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Heteromeric complex of the ligand binding domain of hLXR-alpha receptor and hRXR-alpha
PDB Id:  1UHL
Ligand:  T0901317
Resolution:  2.9Å
Species:  Human
References:  41
Natural/Endogenous Ligands Click here for help
24(S), 25-epoxycholesterol
24(S)-hydroxycholesterol
27-hydroxycholesterol
22R-hydroxycholesterol
Comments: A series of oxysterols are natural ligands
Potency order (Human)
20S-hydroxycholesterol, 22R-hydroxycholesterol, 24(S)-hydroxycholesterol > 25-hydroxycholesterol, 27-hydroxycholesterol  [24]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists Click here for help
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-783483 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 7.9 pKd 31
pKd 7.9 [31]
AZ12260493 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 8.1 pKi 3
pKi 8.1 (Ki 7x10-9 M) [3]
desmosterol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 5.5 pKi 48
pKi 5.5 (Ki 2.9x10-6 M) [48]
acetyl-podocarpic dimer Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.0 pEC50 40
pEC50 9.0 [40]
T0901317 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Agonist 7.3 pEC50 37
pEC50 7.3 [37]
27-hydroxycholesterol Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Agonist 7.1 pEC50 11
pEC50 7.1 [11]
IMB-808 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 pEC50 25
pEC50 6.8 (EC50 1.5x10-7 M) [25]
Description: In a LXRα-GAL4 luciferase reporter assay using transfected HEK293T cells.
GW3965 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Agonist 6.7 pEC50 7
pEC50 6.7 [7]
24(S), 25-epoxycholesterol Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.4 – 6.5 pEC50 16,24,42
pEC50 5.4 – 6.5 [16,24,42]
paxilline Small molecule or natural product Hs Agonist 5.4 pEC50 4
pEC50 5.4 [4]
24(S)-hydroxycholesterol Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Agonist 5.4 pEC50 24
pEC50 5.4 [24]
22R-hydroxycholesterol Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.3 pEC50 17
pEC50 5.3 [17]
Agonist Comments
Other oxysterols were also identified as endogenous ligands by Janowski et al., including 20, 22-dihydroxycholesterol [17]. Activity of endogenous LXR agonists is compared in Janowski et al. [16]. Efficacy value for ligand 27-hydroxycholesterol was determined in vitro. Other endogenous agonist include cholic acid [42].
Antagonists Click here for help
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK2033 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pIC50 51
pIC50 7.0 [51]
SR9238 Small molecule or natural product Click here for species-specific activity table Mm Inverse agonist 6.7 pIC50 12
pIC50 6.7 (IC50 2.14x10-7 M) [12]
View species-specific antagonist tables
Antagonist Comments
Inverse agonist SR9243 induces interaction between Liver-X receptors and their corepressors, resulting in an inhibition of aerobic glycolysis and lipogenesis [10].
Immunopharmacology Comments
Liver X receptors (LXR) are involved in the regulation of lipid metabolism and inflammatory responses. As such they are novel drug targets for cholesterol homeostasis (hypercholesterolaemia), inflammation, and with potential therapeutic effects in neurodegenerative diseases [47]. Rgenix has a small molecule LXR agonist (RGX-104) in Phase 1 clinical trial as an immuno-oncology therapy (see NCT02922764). Rgenix's preclinical studies showed that RGX-104 reverses myeloid-derived suppressor cell (MDSC)-mediated immune evasion by tumour cells. This effect is produced via LXR agonist-generated depletion of MDSCs in the tumour microenvironment, which releases T cells and other immune cells to detect and destroy the cancerous cells.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling
DNA Binding Click here for help
Structure:  RXR partner
HRE core sequence:  AGGTCANNNNAGGTCA
Response element:  DR4, Other - see comments
DNA Binding Comments
RXR binds the 5’ half-site while LXR binds the 3’ half-site of DR4 HREs.
Co-binding Partners Click here for help
Name Interaction Effect Reference
Retinoid X receptor-α Physical, Functional Required for transactivation 46
SHP Physical, Functional Represses transactivation 5
LRH-1 Functional Competence factor 30
Main Co-regulators Click here for help
Name Activity Specific Ligand dependent AF-2 dependent Comments References
EP300 Co-activator No Yes No Overexpression increased transactivation of the ABCA1 promoter 15
NCOA1 Co-activator No Yes No p160 family: Overexpression increased transactivation of the ABCA1 promoter 15
TRRAP Co-activator No Yes No Overexpression increased transactivation of LXRE, RNAi decreased expression of LXR regulated genes 43
NCOA2 Co-activator No Yes No Interaction determined by affinity pull-down 39
PPARGC1A Co-activator No Yes No Overexpression increased transactivation of the CETP promoter 32
PPARGC1B Co-activator No Yes No Overexpression increased transactivation of LXRE Viral transduction increased expression of LXR genes 26
NCOR1 Co-repressor No Yes No Interaction determined in mammalian two-hybrid LXR alpha>beta. Overexpression decreased transactivation of LXRE 13
NCOR2 Co-repressor No Yes No Interaction determined in mammalian two-hybrid LXR alpha>beta 13
Main Target Genes Click here for help
Name Species Effect Technique Comments References
APOE Human Activated Transient transfection, EMSA Cholesterol transport 23
APOD Human Activated Transient transfection, EMSA 14
CETP Human Activated Transient transfection, EMSA 29
LPL Human Activated Transient transfection, EMSA 50
PLTP Human Activated Transient transfection, EMSA 6,21
NR1H3 Human Activated Transient transfection, EMSA 22
SREBF1 Human Activated Transient transfection, EMSA Fatty acid and triglycerides synthesis 35
ApoCI/IV/II Human Activated Transient transfection 30
Vegfa Mouse Activated Angiogenesis and neovascularization 45
Cyp7a1 Mouse Activated Transient transfection, EMSA Cholesterol to bile acid conversion 24
ABCA1 Human Activated Transient transfection, EMSA Reverse cholesterol transport efflux 8,35
ABCG1 Human Activated Transient transfection, EMSA Reverse cholesterol transport efflux 20,44
Scd1 Mouse Activated Unsaturated fatty acid synthesis
SLC2A4 Human Activated Transient transfection, EMSA Insulin stimulated glucose uptake 9
Abcg5 Mouse Activated Intestinal cholesterol efflux 34
Mylip Mouse Activated Induces lipoprotein receptor (LDLR) degradation, the receptor responsible for cholesterol uptake 49
Npc1l1 Mouse Repressed Intestinal cholesterol absorption 27
Abcg8 Mouse Activated Intestinal cholesterol efflux 34
FASN Human Activated Transient transfection, EMSA Fatty acid synthesis 18
Tissue Distribution Click here for help
Liver, small intestine, kidney, adipose, macrophages, spleen, adrenal
Expression level:  High
Species:  Rat
Technique:  Northern blot
References:  46
Tissue Distribution Comments
Mouse expression determined by Northern blot in [28].
Physiological Consequences of Altering Gene Expression Click here for help
Knockout mice are resistant to obesity when challenged with a diet containing high fat and cholesterol.
Species:  Mouse
Tissue: 
Technique:  Knockout
References:  19
Knockout mice display an inability to tolerate dietary cholesterol; accumulation of hepatic cholesteryl esters resulting in hepatomegaly; accumulation of macrophage cholesterol; increased serum LDL; decreased serum HDL, VLDL, and triglycerides.
Species:  Mouse
Tissue: 
Technique:  Knockout
References:  33,36-38
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0002182 abnormal astrocyte morphology PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0005365 abnormal bile salt homeostasis PMID: 9630215 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0009278 abnormal bone marrow cell physiology PMID: 12193651 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0010152 abnormal brain ependyma morphology PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0004950 abnormal brain vasculature morphology PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000822 abnormal brain ventricle morphology PMID: 12368482 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0003191 abnormal cellular cholesterol metabolism PMID: 11238557 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0005537 abnormal cerebral aqueduct morphology PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0005278 abnormal cholesterol homeostasis PMID: 12368482 
Nr1h3tm1Dgen Nr1h3tm1Dgen/Nr1h3tm1Dgen
Not Specified
MGI:1352462  MP:0005278 abnormal cholesterol homeostasis PMID: 16614371 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000820 abnormal choroid plexus morphology PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002679 abnormal corpus luteum PMID: 19325005 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0001119 abnormal female reproductive system morphology PMID: 17166844 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0003699 abnormal female reproductive system physiology PMID: 17166844 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000828 abnormal fourth ventricle morphology PMID: 12368482 
Nr1h3tm1Dgen Nr1h3tm1Dgen/Nr1h3tm1Dgen
Not Specified
MGI:1352462  MP:0002139 abnormal hepatobiliary system physiology PMID: 16614371 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000823 abnormal lateral ventricle morphology PMID: 12368482 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002786 abnormal Leydig cell morphology PMID: 17341595 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0002118 abnormal lipid homeostasis PMID: 12368482 
Nr1h3tm1Dgen Nr1h3tm1Dgen/Nr1h3tm1Dgen
Not Specified
MGI:1352462  MP:0002118 abnormal lipid homeostasis PMID: 16614371 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002446 abnormal macrophage morphology PMID: 12193651 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0001145 abnormal male reproductive system morphology PMID: 17166844 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0003698 abnormal male reproductive system physiology PMID: 17166844 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0009229 abnormal median eminence morphology PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000920 abnormal myelination PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0003871 abnormal myelin sheath morphology PMID: 12368482 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0008256 abnormal myometrium morphology PMID: 17166844 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0003507 abnormal ovary physiology PMID: 19325005 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002907 abnormal parturition PMID: 17166844 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002216 abnormal seminiferous tubule morphology PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002784 abnormal Sertoli cell morphology PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002685 abnormal spermatogonia proliferation PMID: 17341595 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0009688 abnormal spinal cord central canal morphology PMID: 12368482 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000836 abnormal substantia nigra morphology PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0009648 abnormal superovulation PMID: 19325005 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0000826 abnormal third ventricle morphology PMID: 12368482 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0009671 abnormal uterus physiology PMID: 17166844 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0008934 absent choroid plexus PMID: 12368482 
Nr1h3tm1Djm|Tg(APPswe,PSEN1dE9)85Dbo Nr1h3tm1Djm/Nr1h3tm1Djm,Tg(APPswe,PSEN1dE9)85Dbo/0
involves: 129S6/SvEvTac * C3H * C57BL/6
MGI:1352462  MGI:3525178  MP:0003329 amyloid beta deposits PMID: 17563384 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0003354 astrocytosis PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002773 decreased circulating luteinizing hormone level PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002773 decreased circulating luteinizing hormone level PMID: 17341595 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002780 decreased circulating testosterone level PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002780 decreased circulating testosterone level PMID: 17341595 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0008948 decreased neuron number PMID: 12368482 
Nr1h3tm1Wexi Nr1h3tm1Wexi/Nr1h3tm1Wexi
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J
MGI:1352462  MP:0008734 decreased susceptibility to endotoxin shock PMID: 19717840 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0004852 decreased testis weight PMID: 17341595 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0000599 enlarged liver PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0004832 enlarged ovary PMID: 19325005 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002628 hepatic steatosis PMID: 9630215 
Nr1h3tm1Wexi Nr1h3tm1Wexi/Nr1h3tm1Wexi
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J
MGI:1352462  MP:0002628 hepatic steatosis PMID: 19717840 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0000755 hindlimb paralysis PMID: 17166844 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0000740 impaired smooth muscle contractility PMID: 17166844 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0002941 increased circulating alanine transaminase level PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002941 increased circulating alanine transaminase level PMID: 9630215 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0005343 increased circulating aspartate transaminase level PMID: 9630215 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0005178 increased circulating cholesterol level PMID: 9630215 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0005182 increased circulating estradiol level PMID: 19325005 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0000182 increased circulating LDL cholesterol level PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0000182 increased circulating LDL cholesterol level PMID: 9630215 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0001846 increased inflammatory response PMID: 19325005 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0010027 increased liver cholesterol level PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0010027 increased liver cholesterol level PMID: 9630215 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac
MGI:1352462  MGI:1352463  MP:0010027 increased liver cholesterol level PMID: 10968783 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002981 increased liver weight PMID: 9630215 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0004778 increased macrophage derived foam cell number PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 12524534 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 12524534 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002412 increased susceptibility to bacterial infection PMID: 12524534 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0002412 increased susceptibility to bacterial infection PMID: 12524534 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0003070 increased vascular permeability PMID: 19325005 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0001915 intracranial hemorrhage PMID: 12368482 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0003103 liver degeneration PMID: 9630215 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0008280 male germ cell apoptosis PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0008280 male germ cell apoptosis PMID: 17341595 
Nr1h2tm1.1Gstr|Nr1h3tm1.1Gstr Nr1h2tm1.1Gstr/Nr1h2tm1.1Gstr,Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MGI:1352463  MP:0003224 neuron degeneration PMID: 12368482 
Nr1h3tm1Gstr Nr1h3tm1Gstr/Nr1h3tm1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0002169 no abnormal phenotype detected PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0002016 ovary cysts PMID: 19325005 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0004834 ovary hemorrhage PMID: 19325005 
Nr1h3tm1.1Gstr Nr1h3tm1.1Gstr/Nr1h3tm1.1Gstr
involves: 129S1/Sv * 129X1/SvJ * C57BL/6
MGI:1352462  MP:0000603 pale liver PMID: 11238557 
Nr1h3tm1Djm Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MP:0000603 pale liver PMID: 9630215 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0008028 pregnancy-related premature death PMID: 17166844 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0001922 reduced male fertility PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0001154 seminiferous tubule degeneration PMID: 17341595 
Nr1h2tm1Djm|Nr1h3tm1Djm Nr1h2tm1Djm/Nr1h2tm1Djm,Nr1h3tm1Djm/Nr1h3tm1Djm
involves: 129S6/SvEvTac * C57BL/6
MGI:1352462  MGI:1352463  MP:0003205 testicular atrophy PMID: 17341595 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Amyotrophic lateral sclerosis
Disease Ontology: DOID:332
Orphanet: ORPHA803

References

Show »

1. Alberti S, Steffensen KR, Gustafsson JA. (2000) Structural characterisation of the mouse nuclear oxysterol receptor genes LXRalpha and LXRbeta. Gene, 243 (1-2): 93-103. [PMID:10675617]

2. Apfel R, Benbrook D, Lernhardt E, Ortiz MA, Salbert G, Pfahl M. (1994) A novel orphan receptor specific for a subset of thyroid hormone-responsive elements and its interaction with the retinoid/thyroid hormone receptor subfamily. Mol Cell Biol, 14 (10): 7025-35. [PMID:7935418]

3. AstraZeneca. AZ12260493. Accessed on 12/09/2014. Modified on 12/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/az12260493/

4. Bramlett KS, Houck KA, Borchert KM, Dowless MS, Kulanthaivel P, Zhang Y, Beyer TP, Schmidt R, Thomas JS, Michael LF, Barr R, Montrose C, Eacho PI, Cao G, Burris TP. (2003) A natural product ligand of the oxysterol receptor, liver X receptor. J Pharmacol Exp Ther, 307 (1): 291-6. [PMID:12893846]

5. Brendel C, Schoonjans K, Botrugno OA, Treuter E, Auwerx J. (2002) The small heterodimer partner interacts with the liver X receptor alpha and represses its transcriptional activity. Mol Endocrinol, 16 (9): 2065-76. [PMID:12198243]

6. Cao G, Beyer TP, Yang XP, Schmidt RJ, Zhang Y, Bensch WR, Kauffman RF, Gao H, Ryan TP, Liang Y, Eacho PI, Jiang XC. (2002) Phospholipid transfer protein is regulated by liver X receptors in vivo. J Biol Chem, 277 (42): 39561-5. [PMID:12177004]

7. Collins JL, Fivush AM, Watson MA, Galardi CM, Lewis MC, Moore LB, Parks DJ, Wilson JG, Tippin TK, Binz JG, Plunket KD, Morgan DG, Beaudet EJ, Whitney KD, Kliewer SA, Willson TM. (2002) Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem, 45 (10): 1963-6. [PMID:11985463]

8. Costet P, Luo Y, Wang N, Tall AR. (2000) Sterol-dependent transactivation of the ABC1 promoter by the liver X receptor/retinoid X receptor. J Biol Chem, 275 (36): 28240-5. [PMID:10858438]

9. Dalen KT, Ulven SM, Bamberg K, Gustafsson JA, Nebb HI. (2003) Expression of the insulin-responsive glucose transporter GLUT4 in adipocytes is dependent on liver X receptor alpha. J Biol Chem, 278 (48): 48283-91. [PMID:12970362]

10. Flaveny CA, Griffett K, El-Gendy Bel-D, Kazantzis M, Sengupta M, Amelio AL, Chatterjee A, Walker J, Solt LA, Kamenecka TM et al.. (2015) Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell, 28 (1): 42-56. [PMID:26120082]

11. Fu X, Menke JG, Chen Y, Zhou G, MacNaul KL, Wright SD, Sparrow CP, Lund EG. (2001) 27-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. J Biol Chem, 276 (42): 38378-87. [PMID:11504730]

12. Griffett K, Solt LA, El-Gendy Bel-D, Kamenecka TM, Burris TP. (2013) A liver-selective LXR inverse agonist that suppresses hepatic steatosis. ACS Chem Biol, 8 (3): 559-67. [PMID:23237488]

13. Hu X, Li S, Wu J, Xia C, Lala DS. (2003) Liver X receptors interact with corepressors to regulate gene expression. Mol Endocrinol, 17 (6): 1019-26. [PMID:12663743]

14. Hummasti S, Laffitte BA, Watson MA, Galardi C, Chao LC, Ramamurthy L, Moore JT, Tontonoz P. (2004) Liver X receptors are regulators of adipocyte gene expression but not differentiation: identification of apoD as a direct target. J Lipid Res, 45 (4): 616-25. [PMID:14703507]

15. Huuskonen J, Fielding PE, Fielding CJ. (2004) Role of p160 coactivator complex in the activation of liver X receptor. Arterioscler Thromb Vasc Biol, 24 (4): 703-8. [PMID:14764426]

16. Janowski BA, Grogan MJ, Jones SA, Wisely GB, Kliewer SA, Corey EJ, Mangelsdorf DJ. (1999) Structural requirements of ligands for the oxysterol liver X receptors LXRalpha and LXRbeta. Proc Natl Acad Sci USA, 96 (1): 266-71. [PMID:9874807]

17. Janowski BA, Willy PJ, Devi TR, Falck JR, Mangelsdorf DJ. (1996) An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha. Nature, 383 (6602): 728-31. [PMID:8878485]

18. Joseph SB, Laffitte BA, Patel PH, Watson MA, Matsukuma KE, Walczak R, Collins JL, Osborne TF, Tontonoz P. (2002) Direct and indirect mechanisms for regulation of fatty acid synthase gene expression by liver X receptors. J Biol Chem, 277 (13): 11019-25. [PMID:11790787]

19. Kalaany NY, Gauthier KC, Zavacki AM, Mammen PP, Kitazume T, Peterson JA, Horton JD, Garry DJ, Bianco AC, Mangelsdorf DJ. (2005) LXRs regulate the balance between fat storage and oxidation. Cell Metab, 1 (4): 231-44. [PMID:16054068]

20. Kennedy MA, Venkateswaran A, Tarr PT, Xenarios I, Kudoh J, Shimizu N, Edwards PA. (2001) Characterization of the human ABCG1 gene: liver X receptor activates an internal promoter that produces a novel transcript encoding an alternative form of the protein. J Biol Chem, 276 (42): 39438-47. [PMID:11500512]

21. Laffitte BA, Joseph SB, Chen M, Castrillo A, Repa J, Wilpitz D, Mangelsdorf D, Tontonoz P. (2003) The phospholipid transfer protein gene is a liver X receptor target expressed by macrophages in atherosclerotic lesions. Mol Cell Biol, 23 (6): 2182-91. [PMID:12612088]

22. Laffitte BA, Joseph SB, Walczak R, Pei L, Wilpitz DC, Collins JL, Tontonoz P. (2001) Autoregulation of the human liver X receptor alpha promoter. Mol Cell Biol, 21 (22): 7558-68. [PMID:11604492]

23. Laffitte BA, Repa JJ, Joseph SB, Wilpitz DC, Kast HR, Mangelsdorf DJ, Tontonoz P. (2001) LXRs control lipid-inducible expression of the apolipoprotein E gene in macrophages and adipocytes. Proc Natl Acad Sci USA, 98 (2): 507-12. [PMID:11149950]

24. Lehmann JM, Kliewer SA, Moore LB, Smith-Oliver TA, Oliver BB, Su JL, Sundseth SS, Winegar DA, Blanchard DE, Spencer TA, Willson TM. (1997) Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. J Biol Chem, 272 (6): 3137-40. [PMID:9013544]

25. Li N, Wang X, Xu Y, Lin Y, Zhu N, Liu P, Lu D, Si S. (2017) Identification of a Novel Liver X Receptor Agonist that Regulates the Expression of Key Cholesterol Homeostasis Genes with Distinct Pharmacological Characteristics. Mol Pharmacol, 91 (4): 264-276. [PMID:28087808]

26. Lin J, Yang R, Tarr PT, Wu PH, Handschin C, Li S, Yang W, Pei L, Uldry M, Tontonoz P, Newgard CB, Spiegelman BM. (2005) Hyperlipidemic effects of dietary saturated fats mediated through PGC-1beta coactivation of SREBP. Cell, 120 (2): 261-73. [PMID:15680331]

27. Lo Sasso G, Murzilli S, Salvatore L, D'Errico I, Petruzzelli M, Conca P, Jiang ZY, Calabresi L, Parini P, Moschetta A. (2010) Intestinal specific LXR activation stimulates reverse cholesterol transport and protects from atherosclerosis. Cell Metab, 12 (2): 187-93. [PMID:20674863]

28. Lu TT, Repa JJ, Mangelsdorf DJ. (2001) Orphan nuclear receptors as eLiXiRs and FiXeRs of sterol metabolism. J Biol Chem, 276 (41): 37735-8. [PMID:11459853]

29. Luo Y, Tall AR. (2000) Sterol upregulation of human CETP expression in vitro and in transgenic mice by an LXR element. J Clin Invest, 105 (4): 513-20. [PMID:10683381]

30. Mak PA, Laffitte BA, Desrumaux C, Joseph SB, Curtiss LK, Mangelsdorf DJ, Tontonoz P, Edwards PA. (2002) Regulated expression of the apolipoprotein E/C-I/C-IV/C-II gene cluster in murine and human macrophages. A critical role for nuclear liver X receptors alpha and beta. J Biol Chem, 277 (35): 31900-8. [PMID:12032151]

31. Menke JG, Macnaul KL, Hayes NS, Baffic J, Chao YS, Elbrecht A, Kelly LJ, Lam MH, Schmidt A, Sahoo S, Wang J, Wright SD, Xin P, Zhou G, Moller DE, Sparrow CP. (2002) A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a). Endocrinology, 143 (7): 2548-58. [PMID:12072387]

32. Oberkofler H, Schraml E, Krempler F, Patsch W. (2003) Potentiation of liver X receptor transcriptional activity by peroxisome-proliferator-activated receptor gamma co-activator 1 alpha. Biochem J, 371 (Pt 1): 89-96. [PMID:12470296]

33. Peet DJ, Turley SD, Ma W, Janowski BA, Lobaccaro JM, Hammer RE, Mangelsdorf DJ. (1998) Cholesterol and bile acid metabolism are impaired in mice lacking the nuclear oxysterol receptor LXR alpha. Cell, 93 (5): 693-704. [PMID:9630215]

34. Repa JJ, Berge KE, Pomajzl C, Richardson JA, Hobbs H, Mangelsdorf DJ. (2002) Regulation of ATP-binding cassette sterol transporters ABCG5 and ABCG8 by the liver X receptors alpha and beta. J Biol Chem, 277 (21): 18793-800. [PMID:11901146]

35. Repa JJ, Liang G, Ou J, Bashmakov Y, Lobaccaro JM, Shimomura I, Shan B, Brown MS, Goldstein JL, Mangelsdorf DJ. (2000) Regulation of mouse sterol regulatory element-binding protein-1c gene (SREBP-1c) by oxysterol receptors, LXRalpha and LXRbeta. Genes Dev, 14 (22): 2819-30. [PMID:11090130]

36. Repa JJ, Turley SD, Lobaccaro JA, Medina J, Li L, Lustig K, Shan B, Heyman RA, Dietschy JM, Mangelsdorf DJ. (2000) Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science, 289 (5484): 1524-9. [PMID:10968783]

37. Schultz JR, Tu H, Luk A, Repa JJ, Medina JC, Li L, Schwendner S, Wang S, Thoolen M, Mangelsdorf DJ, Lustig KD, Shan B. (2000) Role of LXRs in control of lipogenesis. Genes Dev, 14 (22): 2831-8. [PMID:11090131]

38. Schuster GU, Parini P, Wang L, Alberti S, Steffensen KR, Hansson GK, Angelin B, Gustafsson JA. (2002) Accumulation of foam cells in liver X receptor-deficient mice. Circulation, 106 (9): 1147-53. [PMID:12196343]

39. Song C, Kokontis JM, Hiipakka RA, Liao S. (1994) Ubiquitous receptor: a receptor that modulates gene activation by retinoic acid and thyroid hormone receptors. Proc Natl Acad Sci USA, 91 (23): 10809-13. [PMID:7971966]

40. Sparrow CP, Baffic J, Lam MH, Lund EG, Adams AD, Fu X, Hayes N, Jones AB, Macnaul KL, Ondeyka J, Singh S, Wang J, Zhou G, Moller DE, Wright SD, Menke JG. (2002) A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux. J Biol Chem, 277 (12): 10021-7. [PMID:11790770]

41. Svensson S, Ostberg T, Jacobsson M, Norström C, Stefansson K, Hallén D, Johansson IC, Zachrisson K, Ogg D, Jendeberg L. (2003) Crystal structure of the heterodimeric complex of LXRalpha and RXRbeta ligand-binding domains in a fully agonistic conformation. EMBO J, 22 (18): 4625-33. [PMID:12970175]

42. Theofilopoulos S, Wang Y, Kitambi SS, Sacchetti P, Sousa KM, Bodin K, Kirk J, Saltó C, Gustafsson M, Toledo EM et al.. (2013) Brain endogenous liver X receptor ligands selectively promote midbrain neurogenesis. Nat Chem Biol, 9 (2): 126-33. [PMID:23292650]

43. Unno A, Takada I, Takezawa S, Oishi H, Baba A, Shimizu T, Tokita A, Yanagisawa J, Kato S. (2005) TRRAP as a hepatic coactivator of LXR and FXR function. Biochem Biophys Res Commun, 327 (3): 933-8. [PMID:15649435]

44. Venkateswaran A, Repa JJ, Lobaccaro JM, Bronson A, Mangelsdorf DJ, Edwards PA. (2000) Human white/murine ABC8 mRNA levels are highly induced in lipid-loaded macrophages. A transcriptional role for specific oxysterols. J Biol Chem, 275 (19): 14700-7. [PMID:10799558]

45. Walczak R, Joseph SB, Laffitte BA, Castrillo A, Pei L, Tontonoz P. (2004) Transcription of the vascular endothelial growth factor gene in macrophages is regulated by liver X receptors. J Biol Chem, 279 (11): 9905-11. [PMID:14699103]

46. Willy PJ, Umesono K, Ong ES, Evans RM, Heyman RA, Mangelsdorf DJ. (1995) LXR, a nuclear receptor that defines a distinct retinoid response pathway. Genes Dev, 9 (9): 1033-45. [PMID:7744246]

47. Xu P, Li D, Tang X, Bao X, Huang J, Tang Y, Yang Y, Xu H, Fan X. (2013) LXR agonists: new potential therapeutic drug for neurodegenerative diseases. Mol Neurobiol, 48 (3): 715-28. [PMID:23625315]

48. Yang C, McDonald JG, Patel A, Zhang Y, Umetani M, Xu F, Westover EJ, Covey DF, Mangelsdorf DJ, Cohen JC et al.. (2006) Sterol intermediates from cholesterol biosynthetic pathway as liver X receptor ligands. J Biol Chem, 281 (38): 27816-26. [PMID:16857673]

49. Zelcer N, Hong C, Boyadjian R, Tontonoz P. (2009) LXR regulates cholesterol uptake through Idol-dependent ubiquitination of the LDL receptor. Science, 325 (5936): 100-4. [PMID:19520913]

50. Zhang Y, Repa JJ, Gauthier K, Mangelsdorf DJ. (2001) Regulation of lipoprotein lipase by the oxysterol receptors, LXRalpha and LXRbeta. J Biol Chem, 276 (46): 43018-24. [PMID:11562371]

51. Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA et al.. (2010) Discovery of tertiary sulfonamides as potent liver X receptor antagonists. J Med Chem, 53 (8): 3412-6. [PMID:20345102]

Contributors

Show »

How to cite this page