Liver X receptor-α
Target has curated data in GtoImmuPdb
Target id: 602
Nomenclature: Liver X receptor-α
Systematic Nomenclature: NR1H3
Contents:
- Gene and Protein Information
- Previous and Unofficial Names
- Database Links
- Selected 3D Structures
- Natural/Endogenous Ligands
- Rank order lists
- Agonists
- Antagonists
- Immunopharmacology Comments
- DNA Binding
- Co-binding Partners
- Main Co-regulators
- Main Target Genes
- Tissue Distribution
- Physiological Consequences of Altering Gene Expression
- Phenotypes, Alleles and Disease Models
- Clinically-Relevant Mutations and Pathophysiology
- References
- Contributors
- How to cite this page
Gene and Protein Information  |
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| 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 |
| 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 |
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| Alphafold | Q13133 (Hs), Q9Z0Y9 (Mm), Q62685 (Rn) |
| CATH/Gene3D | 3.30.50.10 |
| ChEMBL Target | CHEMBL2808 (Hs), CHEMBL2189152 (Mm), CHEMBL4523336 (Rn) |
| Ensembl Gene | ENSG00000025434 (Hs), ENSMUSG00000002108 (Mm), ENSRNOG00000013172 (Rn) |
| Entrez Gene | 10062 (Hs), 22259 (Mm), 58852 (Rn) |
| Human Protein Atlas | ENSG00000025434 (Hs) |
| KEGG Gene | hsa:10062 (Hs), mmu:22259 (Mm), rno:58852 (Rn) |
| OMIM | 602423 (Hs) |
| Orphanet | ORPHA123908 (Hs) |
| Pharos | Q13133 (Hs) |
| RefSeq Nucleotide | NM_001130102 (Hs), NM_013839 (Mm), NM_001177730 (Mm), NM_031627 (Rn) |
| RefSeq Protein | NP_005684 (Hs), NP_038867 (Mm), NP_113815 (Rn) |
| SynPHARM |
6428 (in complex with GW3965) 6426 (in complex with L-783483) 6429 (in complex with T0901317) |
| UniProtKB | Q13133 (Hs), Q9Z0Y9 (Mm), Q62685 (Rn) |
| Wikipedia | NR1H3 (Hs) |
| Selected 3D Structures |
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| Natural/Endogenous Ligands |
| 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 
| Agonists |
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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 |
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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. |
| DNA Binding |
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| DNA Binding Comments | |||||||
| RXR binds the 5’ half-site while LXR binds the 3’ half-site of DR4 HREs. | |||||||
| Co-binding Partners |
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| 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 |
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| 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 |
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| 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
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| Tissue Distribution Comments | ||||||||||
| Mouse expression determined by Northern blot in [28]. | ||||||||||
| Physiological Consequences of Altering Gene Expression
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| Phenotypes, Alleles and Disease Models
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Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Clinically-Relevant Mutations and Pathophysiology
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References
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