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Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by calcium and the second messenger diacylglycerol. PKC family members phosphorylate a wide variety of protein targets and are known to be involved in diverse cellular signaling pathways. PKC family members also serve as major receptors for phorbol esters, a class of tumor promoters. Each member of the PKC family has a specific expression profile and is believed to play a distinct role in cells. The protein encoded by this gene is one of the PKC family members. This kinase has been reported to play roles in many different cellular processes, such as cell adhesion, cell transformation, cell cycle checkpoint, and cell volume control. Knockout studies in mice suggest that this kinase may be a fundamental regulator of cardiac contractility and Ca(2+) handling in myocytes. [provided by RefSeq, Jul 2008]
PRKCA (Protein Kinase C Alpha) is a Protein Coding gene. Diseases associated with PRKCA include Papillary Glioneuronal Tumors and Chordoid Glioma. Among its related pathways are Role of Calcineurin-dependent NFAT signaling in lymphocytes and Wnt Signaling Pathway and Pluripotency. Gene Ontology (GO) annotations related to this gene include transferase activity, transferring phosphorus-containing groups and protein tyrosine kinase activity. An important paralog of this gene is PRKCB.
Protein kinase C (PKC) refers to a family of serine/threonine protein kinases grouped by their activation mechanism. Conventional PKCs (cPKC alpha-, betaI- , betaII- and gamma-) are activated by phosphatidylserine in a calcium dependent manner and can bind diacylglycerol.
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0004672 | protein kinase activity | IDA | 10770950 |
GO:0004674 | protein serine/threonine kinase activity | TAS | -- |
GO:0004697 | protein kinase C activity | ISS | -- |
GO:0005178 | integrin binding | ISS | -- |
GO:0005515 | protein binding | IPI | 12571249 |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0005634 | nucleus | IEA | -- |
GO:0005654 | nucleoplasm | TAS | -- |
GO:0005737 | cytoplasm | IEA,IDA | 15632189 |
GO:0005739 | mitochondrion | HDA,IEA | 20833797 |
GO:0005783 | endoplasmic reticulum | IDA | 18556656 |
SuperPathway | Contained pathways | ||
---|---|---|---|
1 | RET signaling |
.92
.92
|
|
2 | DAG and IP3 signaling |
.93
|
|
3 | IL-2 Pathway |
ErbB Family Pathway
.59
ErbB4 Pathway
.59
Prolactin Signaling
.54
Thrombopoietin Pathway
.51
Growth Hormone Signaling
.49
|
ErbB2-ErbB3 Heterodimers
.49
IL-2 Pathway
.48
LPS Stimulated MAPK Signaling
.47
UVC-Induced MAPK Signaling
.44
PACAP Signaling
.37
|
4 | fMLP Pathway |
CCR3 Pathway in Eosinophils
.44
VEGF and S-1P Signaling
.44
fMLP Pathway
.43
|
CXCR4 Pathway
.39
Alpha-Adrenergic Signaling
.38
Huntington's Disease Pathway
.30
|
5 | CDK-mediated phosphorylation and removal of Cdc6 |
.70
|
.41
|
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0001525 | angiogenesis | IEA | -- |
GO:0001938 | positive regulation of endothelial cell proliferation | IMP | 11909826 |
GO:0002159 | desmosome assembly | IMP | 18474624 |
GO:0006468 | protein phosphorylation | IDA | 10770950 |
GO:0006915 | apoptotic process | IEA | -- |
Name | Status | Disease Links | Group | Role | Mechanism of Action | Clinical Trials |
---|---|---|---|---|---|---|
Ingenol mebutate | Approved | Pharma | Target, ligand | 0 | ||
midostaurin | Approved, Investigational | Pharma | Target, antagonist, inhibitor | Kinase Inhibitors | 43 | |
Vitamin E | Approved, Vet_approved | Nutra | Target | 504,508 | ||
Tamoxifen | Approved | Pharma | Antagonist, Target, inhibitor | TGF-β modulatory and PKC inhibitory effects, ER antagonist, Anti-Estrogens | 446 | |
Calcium | Approved | Nutra | 7773 |
Name | Synonyms | Role | CAS Number | PubChem IDs | PubMed IDs | |
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ADP |
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Full agonist, Agonist, Partial agonist, Antagonist, Gating inhibitor | 58-64-0 |
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Diglycerides Group A |
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Diglycerides Group B |
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Diglycerides Group C |
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Diglycerides Group D |
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Compound | Action | Cas Number |
---|---|---|
Calphostin C | Potent, selective and photo-dependent PKC inhibitor | 121263-19-2 |
CGP 53353 | Selective inhibitor of PKCbetaII | 145915-60-2 |
GF 109203X | Protein kinase C inhibitor | 133052-90-1 |
Oncrasin 1 | Induces abnormal nuclear aggregation of PKCiota; proapoptotic | 75629-57-1 |
Rottlerin | Reported PKCdelta inhibitor | 82-08-6 |
Compound | Action | Cas Number |
---|---|---|
(-)-Epigallocatechin gallate (EGCG) | Antioxidant, antiangiogenic and antitumor agent | 989-51-5 |
[Ser25] Protein Kinase C (19-31) | PKC substrate | 136795-05-6 |
Bryostatin 2 | 87745-28-6 | |
Bryostatin 3 | 143370-84-7 | |
CGP60474 | CDKs and PKC inhibitor, potent | 164658-13-3 |
Chelerythrine | PKC inhibitor | 34316-15-9 |
Chelerythrine Chloride | PKC antagonist | 34316-15-9 |
Daphnetin | Protein kinases inhibitor for EGFR/PKA/PKC | 486-35-1 |
Dequalinium Chloride | 522-51-0 | |
Enzastaurin (LY317615) | PKC beta inhibitor,potent and selective | 170364-57-5 |
GF 109203X | Protein kinase C,MLCK,PKG and PKA inhibitor | 133052-90-1 |
Go 6976 | PKCα/PKCβ1 inhibitor | 136194-77-9 |
Go 6983 | pan-PKC inhibitor | 133053-19-7 |
K-252c | Protein kinase inhibitor | 85753-43-1 |
Midostaurin (PKC412) | PKC inhibitor | 120685-11-2 |
Ro 31-8220 | pan-PKC inhibitor | 125314-64-9 |
Ro 31-8220 Mesylate | Pan-PKC inhibitor | 138489-18-6 |
Sotrastaurin (AEB071) | PKC inhibitor | 425637-18-9 |
Staurosporine | Protein kinase inhibitor,potent and cell permeable | 62996-74-1 |
Verbascoside | PKC/NF-κB inhibitor | 61276-17-3 |
ZIP | PKMζ inhibitor | 863987-12-6 |
Zoledronic Acid | Potent nitrogen-containing bisphosphonates | 118072-93-8 |
ExUns: | 1 | ^ | 2 | ^ | 3 | ^ | 4 | ^ | 5 | ^ | 6 | ^ | 7 | ^ | 8 | ^ | 9 | ^ | 10 | ^ | 11 | ^ | 12 | ^ | 13 | ^ | 14 | ^ | 15 | ^ | 16 | ^ | 17 | ^ | 18 |
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SP1: | - | - | |||||||||||||||||||||||||||||||||
SP2: |