Tclin RXRA Retinoic acid receptor RXR-alpha

Protein Summary

Description

Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes. Retinoid X receptors (RXRs) and retinoic acid receptors (RARs) are nuclear receptors that mediate the biological effects of retinoids by their involvement in retinoic acid-mediated gene activation. These receptors function as transcription factors by binding as homodimers or heterodimers to specific sequences in the promoters of target genes. The protein encoded by this gene is a member of the steroid and thyroid hormone receptor superfamily of transcriptional regulators. Alternative splicing of this gene results in multiple transcript variants. [provided by RefSeq, May 2014]

Uniprot Accession IDs

• P19793
• B3KY83
• Q2NL52
• Q2V504

Gene Name

• RXRA

Ensembl ID

• ENST00000481739
• ENSP00000419692
• ENSG00000186350

Symbol

• NR2B1
• NR2B1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
chemical	0.99
hub protein	0.99
biological process	0.98
kinase	0.94

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Retinoic Acid Receptor Rxr-alpha

Protein / Receptor / Retinoic Acid Receptor Rxr-alpha

Protein / Nucleic Acid Binding / Retinoic Acid Receptor Rxr-alpha

Protein / ... / C4 Zinc Finger Nuclear Receptor / Retinoic Acid Receptor Rxr-alpha

DTO Classes

Protein / Nuclear Receptor / Retinoid X Receptors / Retinoic Acid Receptor Rxr-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: 341.36   (req: < 5)

Gene RIFs: 210   (req: <= 3)

Antibodies: 394   (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: 341.36   (req: >= 5)

Gene RIFs: 210   (req: > 3)

Antibodies: 394   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 44

Tchem

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

Active Ligands: 217

Tclin

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

Active Drugs: 4