Target Information
Target General Infomation | |||||
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Target ID |
T74258
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Former ID |
TTDR01403
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Target Name |
mRNA of PKC-zeta
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Gene Name |
PRKCZ
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Synonyms |
PRKCZ (mRNA); nPKC-zeta (mRNA); PRKCZ
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Target Type |
Discontinued
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Function |
Calcium- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signaling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP). Upon lipopolysaccharide (LPS) treatment in macrophages, or following mitogenic stimuli, functionsdownstream of PI3K to activate MAP2K1/MEK1-MAPK1/ERK2 signaling cascade independently of RAF1 activation. Required for insulin-dependent activation of AKT3, but may function as an adapter rather thana direct activator. Upon insulin treatment may act as a downstream effector of PI3K and contribute to the activation of translocation of the glucose transporter SLC2A4/GLUT4 and subsequent glucose transport in adipocytes. In EGF-induced cells, binds and activates MAP2K5/MEK5-MAPK7/ERK5 independently of its kinase activity and can activate JUN promoter through MEF2C. Through binding with SQSTM1/p62, functions in interleukin-1 signaling and activation of NF-kappa-B with the specific adapters RIPK1 and TRAF6. Participates in TNF-dependent transactivation of NF-kappa-B by phosphorylating and activating IKBKB kinase, which in turn leads to the degradation of NF-kappa-B inhibitors. In migrating astrocytes, forms a cytoplasmic complex with PARD6A and is recruited by CDC42 to function in the establishment of cell polarity along with the microtubule motor and dynein. In association with FEZ1, stimulates neuronal differentiation in PC12 cells. In the inflammatory response, is required for the T-helper 2 (Th2) differentiation process, including interleukin production, efficient activation of JAK1 and the subsequent phosphorylation and nuclear translocation of STAT6. May be involved in development of allergic airway inflammation (asthma), a process dependent on Th2 immune response. In the NF-kappa-B-mediated inflammatory response, can relieve SETD6-dependent repression of NF-kappa-B target genes by phosphorylating the RELA subunit at 'Ser-311'. Necessary and sufficient for LTP maintenance in hippocampal CA1 pyramidal cells. In vein endothelial cells treated with the oxidant peroxynitrite, phosphorylates STK11 leading to nuclear export of STK11, subsequent inhibition of PI3K/Akt signaling, and increased apoptosis.
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BioChemical Class |
Kinase
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Target Validation |
T74258
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UniProt ID | |||||
EC Number |
EC 2.7.11.13
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Sequence |
MPSRTGPKMEGSGGRVRLKAHYGGDIFITSVDAATTFEELCEEVRDMCRLHQQHPLTLKW
VDSEGDPCTVSSQMELEEAFRLARQCRDEGLIIHVFPSTPEQPGLPCPGEDKSIYRRGAR RWRKLYRANGHLFQAKRFNRRAYCGQCSERIWGLARQGYRCINCKLLVHKRCHGLVPLTC RKHMDSVMPSQEPPVDDKNEDADLPSEETDGIAYISSSRKHDSIKDDSEDLKPVIDGMDG IKISQGLGLQDFDLIRVIGRGSYAKVLLVRLKKNDQIYAMKVVKKELVHDDEDIDWVQTE KHVFEQASSNPFLVGLHSCFQTTSRLFLVIEYVNGGDLMFHMQRQRKLPEEHARFYAAEI CIALNFLHERGIIYRDLKLDNVLLDADGHIKLTDYGMCKEGLGPGDTTSTFCGTPNYIAP EILRGEEYGFSVDWWALGVLMFEMMAGRSPFDIITDNPDMNTEDYLFQVILEKPIRIPRF LSVKASHVLKGFLNKDPKERLGCRPQTGFSDIKSHAFFRSIDWDLLEKKQALPPFQPQIT DDYGLDNFDTQFTSEPVQLTPDDEDAIKRIDQSEFEGFEYINPLLLSTEESV |
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Drugs and Mode of Action | |||||
Pathways | |||||
KEGG Pathway | Rap1 signaling pathway | ||||
Chemokine signaling pathway | |||||
Sphingolipid signaling pathway | |||||
Endocytosis | |||||
PI3K-Akt signaling pathway | |||||
Hippo signaling pathway | |||||
Tight junction | |||||
Platelet activation | |||||
Insulin signaling pathway | |||||
Type II diabetes mellitus | |||||
PANTHER Pathway | Alzheimer disease-amyloid secretase pathway | ||||
Angiogenesis | |||||
EGF receptor signaling pathway | |||||
Endothelin signaling pathway | |||||
FGF signaling pathway | |||||
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
Inflammation mediated by chemokine and cytokine signaling pathway | |||||
Muscarinic acetylcholine receptor 1 and 3 signaling pathway | |||||
VEGF signaling pathway | |||||
Wnt signaling pathway | |||||
5HT2 type receptor mediated signaling pathway | |||||
Histamine H1 receptor mediated signaling pathway | |||||
Oxytocin receptor mediated signaling pathway | |||||
Thyrotropin-releasing hormone receptor signaling pathway | |||||
Pathway Interaction Database | RhoA signaling pathway | ||||
Insulin Pathway | |||||
Noncanonical Wnt signaling pathway | |||||
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) | |||||
CDC42 signaling events | |||||
Thromboxane A2 receptor signaling | |||||
IL1-mediated signaling events | |||||
Role of Calcineurin-dependent NFAT signaling in lymphocytes | |||||
CXCR4-mediated signaling events | |||||
IGF1 pathway | |||||
TNF receptor signaling pathway | |||||
IL2 signaling events mediated by PI3K | |||||
Ceramide signaling pathway | |||||
p75(NTR)-mediated signaling | |||||
amb2 Integrin signaling | |||||
ErbB1 downstream signaling | |||||
Neurotrophic factor-mediated Trk receptor signaling | |||||
Nephrin/Neph1 signaling in the kidney podocyte | |||||
Insulin-mediated glucose transport | |||||
Regulation of Ras family activation | |||||
PathWhiz Pathway | Intracellular Signalling Through Adenosine Receptor A2a and Adenosine | ||||
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine | |||||
Reactome | GPVI-mediated activation cascade | ||||
TGF-beta receptor signaling in EMT (epithelial to mesenchymal transition) | |||||
VEGFR2 mediated cell proliferation | |||||
WikiPathways | Calcium Regulation in the Cardiac Cell | ||||
Insulin Signaling | |||||
EGF/EGFR Signaling Pathway | |||||
Wnt Signaling Pathway | |||||
Wnt Signaling Pathway and Pluripotency | |||||
MAPK Signaling Pathway | |||||
G Protein Signaling Pathways | |||||
Myometrial Relaxation and Contraction Pathways | |||||
Signaling by TGF-beta Receptor Complex | |||||
Allograft Rejection | |||||
AGE/RAGE pathway | |||||
TNF alpha Signaling Pathway | |||||
Signaling Pathways in Glioblastoma | |||||
miRs in Muscle Cell Differentiation | |||||
IL-1 signaling pathway | |||||
GPVI-mediated activation cascade | |||||
Type II diabetes mellitus | |||||
References | |||||
Ref 529880 | 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. | ||||
Ref 534154 | J Med Chem. 1996 Jul 5;39(14):2664-71.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. | ||||
Ref 534191 | Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett. 1996 Aug 26;392(2):77-80. |
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