Target name

Q04759: Protein kinase C theta type


  Protein function

Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signaling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2. In TCR-CD3/CD28-co-stimulated T-cells, is required for the activation of NF-kappa-B and JUN, which in turn are essential for IL2 production, and participates to the calcium-dependent NFATC1 and NFATC2 transactivation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11 on several serine residues, inducing CARD11 association with lipid rafts and recruitment of the BCL10-MALT1 complex, which then activates IKK complex, resulting in nuclear translocation and activation of NFKB1. May also play an indirect role in activation of the non-canonical NF-kappa-B (NFKB2) pathway. In the signaling pathway leading to JUN activation, acts by phosphorylating the mediator STK39/SPAK and may not act through MAP kinases signaling. Plays a critical role in TCR/CD28-induced NFATC1 and NFATC2 transactivation by participating in the regulation of reduced inositol 1,4,5-trisphosphate generation and intracellular calcium mobilization. After costimulation of T-cells through CD28 can phosphorylate CBLB and is required for the ubiquitination and subsequent degradation of CBLB, which is a prerequisite for the activation of TCR. During T-cells differentiation, plays an important role in the development of T-helper 2 (Th2) cells following immune and inflammatory responses, and, in the development of inflammatory autoimmune diseases, is necessary for the activation of IL17-producing Th17 cells. May play a minor role in Th1 response. Upon TCR stimulation, mediates T-cell protective survival signal by phosphorylating BAD, thus protecting T-cells from BAD-induced apoptosis, and by up-regulating BCL-X(L)/BCL2L1 levels through NF-kappa-B and JUN pathways. In platelets, regulates signal transduction downstream of the ITGA2B, CD36/GP4, F2R/PAR1 and F2RL3/PAR4 receptors, playing a positive role in 'outside-in' signaling and granule secretion signal transduction. May relay signals from the activated ITGA2B receptor by regulating the uncoupling of WASP and WIPF1, thereby permitting the regulation of actin filament nucleation and branching activity of the Arp2/3 complex. May mediate inhibitory effects of free fatty acids on insulin signaling by phosphorylating IRS1, which in turn blocks IRS1 tyrosine phosphorylation and downstream activation of the PI3K/AKT pathway. Phosphorylates MSN (moesin) in the presence of phosphatidylglycerol or phosphatidylinositol. Phosphorylates PDPK1 at 'Ser-504' and 'Ser-532' and negatively regulates its ability to phosphorylate PKB/AKT1.

  Database links

Uniprot primary ID Q04759
PDB ID 1XJD 4Q9Z 2ENJ 2ENN 4RA5 2JED 2ENZ
DrugBank ID DB00675
BioGrid ID 111574
GuidetoPHARMACOLOGY ID 1488
PharmGKB ID PA33773
KEGG ID hsa:5588
DIP ID
STRING ID 9606.ENSP00000263125
IntAct ID Q04759
DMDM 20141582
BRENDA 2.7.11.13
Reactome R-HSA-202424 R-HSA-111465 R-HSA-418597 R-HSA-2514859 R-HSA-373752 R-HSA-114508 R-HSA-2871837
SignaLink Q04759
BioCyc
Entrez Gene (Gene ID) 5588
BindingDB Q04759

  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 0.873 0.005 0.967 0.004 0.920 0.000 0.916 0.005 0.960 0.000 0.840 0.005 Download
Estate fingerprints 0.755 0.005 0.895 0.004 0.825 0.005 0.812 0.004 0.904 0.005 0.655 0.005 Download
MACCS fingerprints 0.882 0.004 0.858 0.005 0.870 0.000 0.871 0.003 0.930 0.000 0.739 0.007 Download
Daylight fingerprints 0.681 0.003 0.999 0.000 0.840 0.000 0.810 0.000 0.940 0.000 0.711 0.003 Download
ECFP2 fingerprints 0.867 0.007 0.965 0.000 0.916 0.005 0.909 0.003 0.960 0.000 0.833 0.007 Download
ECFP4 fingerprints 0.890 0.000 0.990 0.000 0.940 0.000 0.937 0.005 0.975 0.005 0.881 0.003 Download
ECFP6 fingerprints 0.864 0.005 0.996 0.000 0.930 0.000 0.930 0.000 0.970 0.000 0.872 0.004 Download

  Download datasets

Positive dataset Negative dataset


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School of Pharmaceutical Sciences, Central South University. All rights reserved.

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