Target name

P05129: Protein kinase C gamma type


  Protein function

Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress. Binds and phosphorylates GRIA4/GLUR4 glutamate receptor and regulates its function by increasing plasma membrane-associated GRIA4 expression. In primary cerebellar neurons treated with the agonist 3,5-dihyidroxyphenylglycine, functions downstream of the metabotropic glutamate receptor GRM5/MGLUR5 and phosphorylates GRIN1/NMDAR1 receptor which plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. May be involved in the regulation of hippocampal long-term potentiation (LTP), but may be not necessary for the process of synaptic plasticity. May be involved in desensitization of mu-type opioid receptor-mediated G-protein activation in the spinal cord, and may be critical for the development and/or maintenance of morphine-induced reinforcing effects in the limbic forebrain. May modulate the functionality of mu-type-opioid receptors by participating in a signaling pathway which leads to the phosphorylation and degradation of opioid receptors. May also contributes to chronic morphine-induced changes in nociceptive processing. Plays a role in neuropathic pain mechanisms and contributes to the maintenance of the allodynia pain produced by peripheral inflammation. Plays an important role in initial sensitivity and tolerance to ethanol, by mediating the behavioral effects of ethanol as well as the effects of this drug on the GABA(A) receptors. During and after cerebral ischemia modulate neurotransmission and cell survival in synaptic membranes, and is involved in insulin-induced inhibition of necrosis, an important mechanism for minimizing ischemic injury. Required for the elimination of multiple climbing fibers during innervation of Purkinje cells in developing cerebellum. Is activated in lens epithelial cells upon hydrogen peroxide treatment, and phosphorylates connexin-43 (GJA1/CX43), resulting in disassembly of GJA1 gap junction plaques and inhibition of gap junction activity which could provide a protective effect against oxidative stress (By similarity). Phosphorylates p53/TP53 and promotes p53/TP53-dependent apoptosis in response to DNA damage. Involved in the phase resetting of the cerebral cortex circadian clock during temporally restricted feeding. Stabilizes the core clock component ARNTL/BMAL1 by interfering with its ubiquitination, thus suppressing its degradation, resulting in phase resetting of the cerebral cortex clock (By similarity).

  Database links

Uniprot primary ID P05129
PDB ID 2E73 2UZP
DrugBank ID DB00675
BioGrid ID 111568
GuidetoPHARMACOLOGY ID 1484
PharmGKB ID PA33766
KEGG ID hsa:5582
DIP ID DIP-39795N
STRING ID 9606.ENSP00000263431
IntAct ID P05129
DMDM 462455
BRENDA 2.7.11.13
Reactome R-HSA-111933 R-HSA-418597 R-HSA-76005 R-HSA-416993 R-HSA-5099900 R-HSA-114516
SignaLink P05129
BioCyc
Entrez Gene (Gene ID) 5582
BindingDB P05129

  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 0.765 0.008 0.949 0.007 0.857 0.008 0.843 0.007 0.927 0.005 0.729 0.014 Download
Estate fingerprints 0.848 0.011 0.716 0.011 0.782 0.009 0.795 0.005 0.850 0.000 0.568 0.014 Download
MACCS fingerprints 0.878 0.012 0.812 0.013 0.845 0.008 0.851 0.009 0.894 0.005 0.694 0.016 Download
Daylight fingerprints 0.743 0.005 0.951 0.005 0.847 0.005 0.830 0.005 0.909 0.003 0.707 0.008 Download
ECFP2 fingerprints 0.919 0.006 0.931 0.012 0.925 0.005 0.926 0.005 0.970 0.000 0.855 0.008 Download
ECFP4 fingerprints 0.916 0.007 0.978 0.007 0.947 0.005 0.947 0.005 0.980 0.000 0.900 0.011 Download
ECFP6 fingerprints 0.868 0.009 0.982 0.003 0.925 0.005 0.924 0.005 0.975 0.005 0.864 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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