Target name

Q04206: Transcription factor p65


  Protein function

NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related to many biological processes such as inflammation, immunity, differentiation, cell growth, tumorigenesis and apoptosis. NF-kappa-B is a homo- or heterodimeric complex formed by the Rel-like domain-containing proteins RELA/p65, RELB, NFKB1/p105, NFKB1/p50, REL and NFKB2/p52 and the heterodimeric p65-p50 complex appears to be most abundant one. The dimers bind at kappa-B sites in the DNA of their target genes and the individual dimers have distinct preferences for different kappa-B sites that they can bind with distinguishable affinity and specificity. Different dimer combinations act as transcriptional activators or repressors, respectively. NF-kappa-B is controlled by various mechanisms of post-translational modification and subcellular compartmentalization as well as by interactions with other cofactors or corepressors. NF-kappa-B complexes are held in the cytoplasm in an inactive state complexed with members of the NF-kappa-B inhibitor (I-kappa-B) family. In a conventional activation pathway, I-kappa-B is phosphorylated by I-kappa-B kinases (IKKs) in response to different activators, subsequently degraded thus liberating the active NF-kappa-B complex which translocates to the nucleus. NF-kappa-B heterodimeric p65-p50 and p65-c-Rel complexes are transcriptional activators. The NF-kappa-B p65-p65 complex appears to be involved in invasin-mediated activation of IL-8 expression. The inhibitory effect of I-kappa-B upon NF-kappa-B the cytoplasm is exerted primarily through the interaction with p65. p65 shows a weak DNA-binding site which could contribute directly to DNA binding in the NF-kappa-B complex. Associates with chromatin at the NF-kappa-B promoter region via association with DDX1. Essential for cytokine gene expression in T-cells (PubMed:15790681).

  Database links

Uniprot primary ID Q04206
PDB ID 2O61 2LSP 4KV4 4KV1 3GUT 3RC0 3QXY 1NFI
DrugBank ID
BioGrid ID 111902
GuidetoPHARMACOLOGY ID
PharmGKB ID PA296
KEGG ID hsa:5970
DIP ID DIP-24238N
STRING ID 9606.ENSP00000384273
IntAct ID Q04206
DMDM 62906901
BRENDA
Reactome R-HSA-933542 R-HSA-193692 R-HSA-381340 R-HSA-202424 R-HSA-445989 R-HSA-2559582 R-HSA-5603029 R-HSA-448706 R-HSA-5621575 R-HSA-5607761 R-HSA-1810476 R-HSA-209560 R-HSA-5603027 R-HSA-1169091 R-HSA-2871837 R-HSA-5607764 R-HSA-5660668 R-HSA-3134963
SignaLink Q04206
BioCyc
Entrez Gene (Gene ID) 5970
BindingDB Q04206

  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 0.854 0.005 0.806 0.000 0.830 0.000 0.837 0.005 0.910 0.000 0.665 0.005 Download
Estate fingerprints 0.842 0.004 0.808 0.005 0.825 0.005 0.828 0.004 0.900 0.000 0.649 0.007 Download
MACCS fingerprints 0.860 0.000 0.780 0.003 0.820 0.000 0.829 0.003 0.900 0.000 0.640 0.000 Download
Daylight fingerprints 0.680 0.000 0.800 0.004 0.740 0.000 0.724 0.005 0.800 0.000 0.485 0.005 Download
ECFP2 fingerprints 0.930 0.000 0.828 0.004 0.879 0.003 0.884 0.005 0.949 0.003 0.759 0.003 Download
ECFP4 fingerprints 0.923 0.005 0.855 0.003 0.889 0.003 0.891 0.003 0.960 0.000 0.776 0.005 Download
ECFP6 fingerprints 0.903 0.005 0.877 0.003 0.890 0.000 0.890 0.000 0.959 0.003 0.777 0.005 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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