Target name

P03372: Estrogen receptor


  Protein function

Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1.

  Database links

Uniprot primary ID P03372
PDB ID 4Q50 4MG5 2OUZ 4IW6 2AYR 3HM1 4JDD 4MGA 3L03 4MGC 4MGD 4MGB 2FAI 4TV1 4MG7 2QGW 2QGT 2QR9 3HLV 2YJA 2R6Y 4JC3 4TUZ 2R6W 3DT3 4Q13 2QE4 5AK2 2I0J 4DMA 4IV4 4IV2 2Q70 1GWQ 1GWR 2G5O 2B23 4MG8 4MG9 2G44 2QZO 2Q6J 4ZN9 1SJ0 2BJ4 4MG6 1G50 4AA6 4IVW 2IOG 2IOK
DrugBank ID DB04575 DB00655 DB01108 DB00957 DB04573 DB04574 DB00890
BioGrid ID 108403
GuidetoPHARMACOLOGY ID 620
PharmGKB ID PA156
KEGG ID hsa:2099
DIP ID DIP-5965N
STRING ID 9606.ENSP00000206249
IntAct ID P03372
DMDM 544257
BRENDA
Reactome R-HSA-383280 R-HSA-1251985
SignaLink P03372
BioCyc
Entrez Gene (Gene ID) 2099
BindingDB P03372

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.780 0.000 0.840 0.000 0.810 0.000 0.805 0.005 0.890 0.000 0.622 0.004 Download
Estate fingerprints 0.830 0.000 0.830 0.000 0.830 0.000 0.830 0.000 0.890 0.000 0.664 0.005 Download
MACCS fingerprints 0.791 0.003 0.867 0.000 0.829 0.003 0.820 0.000 0.890 0.000 0.653 0.005 Download
Daylight fingerprints 0.740 0.000 0.760 0.005 0.750 0.000 0.749 0.003 0.791 0.003 0.501 0.003 Download
ECFP2 fingerprints 0.890 0.000 0.930 0.000 0.910 0.000 0.905 0.005 0.960 0.000 0.815 0.005 Download
ECFP4 fingerprints 0.895 0.005 0.965 0.000 0.930 0.000 0.927 0.005 0.960 0.000 0.860 0.000 Download
ECFP6 fingerprints 0.889 0.003 0.971 0.000 0.930 0.000 0.922 0.004 0.960 0.000 0.860 0.000 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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