TargetNet


P19793

Retinoic acid receptor RXR-alpha


Function

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. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. 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.


Database Links

Database Links
UniProt P19793
PDB 1BY4, 1DSZ, 1FBY, 1FM6, 1FM9, 1G1U, 1G5Y, 1K74, 1LBD, 1MV9, 1MVC, 1MZN, 1R0N, 1RDT, 1RXR, 1XLS, 1XV9, 1XVP, 1YNW, 2ACL, 2NLL, 2P1T, 2P1U, 2P1V, 2ZXZ, 2ZY0, 3DZU, 3DZY, 3E00, 3E94, 3FAL, 3FC6, 3FUG, 3H0A, 3KWY, 3NSP, 3NSQ, 3OAP, 3OZJ, 3PCU, 3R29, 3R2A, 3R5M, 3UVV, 4J5W, 4J5X, 4K4J, 4K6I, 4M8E, 4M8H
BioGrid 112168
BindingDB P19793
DrugBank DB00459, DB00210, DB00523, DB00926
Guide to PHARMACOLOGY 610
PharmGKB PA34890
KEGG hsa:6256
BioCyc Not available
Entrez Gene (GeneID) 6256

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9867 0.0018
Accuracy 0.9521 0.0037
Sensitivity 0.9529 0.0058
Specificity 0.9514 0.0038
BEDROC 0.988 0.005
MCC Threshold 0.418 N/A
MCC 0.9154 N/A
F-score Threshold 0.418 N/A
F-score 0.9544 N/A

Downloads

R Model Object

Random Forest model object (.RData)

Download RData

Positive Set

SMILES string + affinity value (.tsv)

Download TSV


Copyright © 2014 - 2017 TargetNet. Developed and maintained by Nan Xiao.

Page generated on: 2014-04-29 14:39:27