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

  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 2B1V 1GWR 2G5O 2B23 4MG8 4MG9 2G44 2QZO 2Q6J 1SJ0 2BJ4 4MG6 1G50 4AA6 4IVW 2IOG 2IOK
DrugBank ID DB04575 DB00655 DB01108 DB00957 DB04573 DB04574 DB00890 DB00675 DB01431 DB00286 DB01196 DB00783 DB01357 DB01406 DB00255 DB01065 DB00977 DB00481 DB00947 DB00603 DB00882 DB00294 DB00396 DB04938 DB01183 DB00539 DB01185 DB00823 DB00304 DB00367
BioGrid ID 108403
PharmGKB ID PA156
KEGG ID hsa:2099
Entrez Gene (Gene ID) 2099
STRING 9606ENSP00000206249
MINT MINT-129047
IntAct P03372
DMDM 544257
Rectome R-HSA-383280 R-HSA-1251985
SignaLink P03372
BindingDB P03372

  Model Performance Metrics

Fingerprint type F1_CV AUC_CV Accuracy_CV Sensitivity_CV Specificity_CV F1_test AUC_test Accuracy_test Sensitivity_test Specificity_test Download model
FP2 fingerprints 0.799 0.851 0.806 0.774 0.837 0.813 0.865 0.813 0.806 0.821 Download
MACCS fingerprints 0.819 0.881 0.822 0.812 0.832 0.836 0.899 0.837 0.840 0.834 Download
Daylight fingerprints 0.764 0.810 0.766 0.760 0.772 0.799 0.848 0.794 0.808 0.780 Download
ECFP2 fingerprints 0.890 0.938 0.892 0.879 0.905 0.923 0.965 0.922 0.932 0.911 Download
ECFP4 fingerprints 0.907 0.944 0.910 0.880 0.940 0.928 0.967 0.928 0.922 0.933 Download
ECFP6 fingerprints 0.893 0.941 0.899 0.846 0.952 0.931 0.967 0.931 0.915 0.948 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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