Target name

Q06187: Tyrosine-protein kinase BTK


  Protein function

Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation. After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members. PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK. BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways. Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway. The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense. Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells. Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation. BTK plays also a critical role in transcription regulation. Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes. BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B. Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR. GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression. ARID3A and NFAT are other transcriptional target of BTK. BTK is required for the formation of functional ARID3A DNA-binding complexes. There is however no evidence that BTK itself binds directly to DNA. BTK has a dual role in the regulation of apoptosis.

  Database links

Uniprot primary ID Q06187
PDB ID 1QLY 4ZLZ 4ZLY 3GEN 3OCT 3OCS 3PJ2 1BWN 2Z0P 1AWW 4Z3V 4OT6 4OT5 1K2P 3P08 1AWX 3PJ3 4OTF 3PJ1 5BPY 4OTR 4OTQ 4YHF 4RFY 4RFZ 2GE9 1B55 5BQ0 3PIZ 3PIX 3PIY 4RG0 3K54 1BTK 4NWM
DrugBank ID DB09053
BioGrid ID 107160
GuidetoPHARMACOLOGY ID 1948
PharmGKB ID PA25454
KEGG ID hsa:695
DIP ID DIP-34071N
STRING ID 9606.ENSP00000308176
IntAct ID Q06187
DMDM 547759
BRENDA 2.7.10.2
Reactome R-HSA-983695 R-HSA-5663213 R-HSA-2029482 R-HSA-2871809 R-HSA-5602498 R-HSA-2424491 R-HSA-166058 R-HSA-5603041
SignaLink Q06187
BioCyc
Entrez Gene (Gene ID) 695
BindingDB Q06187

  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 0.801 0.017 0.823 0.011 0.812 0.008 0.811 0.011 0.901 0.003 0.627 0.018 Download
Estate fingerprints 0.775 0.008 0.753 0.014 0.764 0.008 0.766 0.007 0.855 0.005 0.526 0.016 Download
MACCS fingerprints 0.870 0.005 0.688 0.013 0.779 0.006 0.797 0.005 0.885 0.005 0.563 0.013 Download
Daylight fingerprints 0.797 0.007 0.779 0.008 0.788 0.006 0.789 0.006 0.837 0.005 0.577 0.009 Download
ECFP2 fingerprints 0.889 0.014 0.879 0.010 0.884 0.011 0.884 0.011 0.952 0.004 0.767 0.021 Download
ECFP4 fingerprints 0.815 0.012 0.943 0.010 0.879 0.007 0.873 0.009 0.957 0.005 0.768 0.014 Download
ECFP6 fingerprints 0.731 0.010 0.981 0.004 0.856 0.005 0.836 0.005 0.953 0.005 0.739 0.009 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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