Tchem NR1H3 Oxysterols receptor LXR-alpha

Protein Summary

Description

Nuclear receptor that exhibits a ligand-dependent transcriptional activation activity (PubMed:19481530, PubMed:25661920). Interaction with retinoic acid receptor (RXR) shifts RXR from its role as a silent DNA-binding partner to an active ligand-binding subunit in mediating retinoid responses through target genes defined by LXRES (By similarity). LXRES are DR4-type response elements characterized by direct repeats of two similar hexanuclotide half-sites spaced by four nucleotides (By similarity). Plays an important role in the regulation of cholesterol homeostasis, regulating cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (PubMed:19481530). Interplays functionally with RORA for the regulation of genes involved in liver metabolism (By similarity). The protein encoded by this gene belongs to the NR1 subfamily of the nuclear receptor superfamily. The NR1 family members are key regulators of macrophage function, controlling transcriptional programs involved in lipid homeostasis and inflammation. This protein is highly expressed in visceral organs, including liver, kidney and intestine. It forms a heterodimer with retinoid X receptor (RXR), and regulates expression of target genes containing retinoid response elements. Studies in mice lacking this gene suggest that it may play an important role in the regulation of cholesterol homeostasis. Alternatively spliced transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Oct 2011]

Uniprot Accession IDs

• Q13133
• A8K3J9
• D3DQR1
• Q8IW13
• Q96H87

Gene Name

• NR1H3

Ensembl ID

• ENST00000395397
• ENSP00000378793
• ENSG00000025434
• ENST00000405853
• ENSP00000384745
• ENST00000407404
• ENSP00000385801
• ENST00000441012
• ENSP00000387946
• ENST00000467728
• ENSP00000420656

Symbol

• LXRA
• LXRA
• LXR-a
• RLD-1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
molecular function	0.98
disease perturbation	0.87
transcription factor binding site profile	0.87
cell type or tissue	0.86

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Oxysterols Receptor Lxr-alpha

Protein / Receptor / Oxysterols Receptor Lxr-alpha

Protein / Nucleic Acid Binding / Oxysterols Receptor Lxr-alpha

Protein / ... / C4 Zinc Finger Nuclear Receptor / Oxysterols Receptor Lxr-alpha

DTO Classes

Protein / Nuclear Receptor / Liver X Receptor-like Receptors / Oxysterols Receptor Lxr-alpha

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 217.03   (req: < 5)

Gene RIFs: 268   (req: <= 3)

Antibodies: 530   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 217.03   (req: >= 5)

Gene RIFs: 268   (req: > 3)

Antibodies: 530   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 48

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 281

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0