Information on EC 2.7.11.13 - protein kinase C

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The expected taxonomic range for this enzyme is: Eukaryota

EC NUMBER
COMMENTARY
2.7.11.13
-
RECOMMENDED NAME
GeneOntology No.
protein kinase C
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
regulation of enzyme activity involves the activation loop, a polypeptide region outside the active site cleft, which is reversibly phosphorylated at a Thr residue
-
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (diacylglycerol-dependent)
A family of serine- and threonine-specific protein kinases that depend on lipids for activity. They can be activated by calcium but have a requirement for the second messenger diacylglycerol. Members of this group of enzymes phosphorylate a wide variety of protein targets and are known to be involved in diverse cell-signalling pathways. Members of the protein kinase C family also serve as major receptors for phorbol esters, a class of tumour promoters.
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
alpha-PKC
P20444
-
aPKCzeta
-
-
C1Bbeta
-
C1 domain of PKC
Calcium-dependent protein kinase C
-
-
-
-
Calcium-dependent protein kinase C
Q16974
-
calcium-independent protein kinase C
Q16975
-
Capkc1p
P43057
-
nPKC eta
P23298
-
PAK-1
Q63433
-
PICK1
P20444
-
PKC
-
-
-
-
PKC
-
-
PKC
-
-
PKC
Mus musculus C57BL/6
-
-
-
PKC alpha
-
-
PKC alpha
-
isozyme
PKC Apl I
Q16974
-
PKC Apl II
Q16975
-
PKC beta II
-
-
PKC beta-II
-
-
PKC beta1
-
-
PKC betaII
-
isozyme
PKC delta
-
-
PKC delta
-
isoform
PKC deltaII
P28867
-
PKC deltaIII
P09215
-
PKC epsilon
-
-
PKC epsilon
-
isozyme
PKC eta
-
-
PKC iota
P41743
-
PKC lambda
Q62074
-
PKC theta
-
-
PKC zeta
O19111
-
PKC-alpha
-
isoform
PKC-alpha
-
-
PKC-alpha/beta
-
isozyme
PKC-beta1
-
-
PKC-betaII
P05771
isozyme
PKC-delta
-
isoform
PKC-delta
Q05655
-
PKC-delta
P09215
-
PKC-epsilon
P16054
-
PKC-L
P24723
-
PKC-like kinase
-
-
PKC-zeta
-
-
PKC-zeta
P05129
-
PKC-zeta
Q05513
isozyme
PKC-zeta
P09217
isozyme
PKCalpha
P17252
isozyme
PKCalpha
P20444
isozyme
PKCalpha
-
isoform
PKCbeta1
P05771
isozyme
PKCbeta1
P68404
isozyme
PKCbeta2
P05771
isozyme
PKCbeta2
P68404
isozyme
PKCbetaI
-
isoform
PKCbetaII
-
-
PKCbetaII
-
isoform
PKCdelta
-
-
PKCdelta
Q05655
isozyme
PKCdelta
P28867
isozyme
PKCdelta
-
isoform
PKCdelta
P09215
-
PKCepsilon
-
-
PKCepsilon
Q02156
isozyme
PKCepsilon
P16054
isozyme
PKCepsilon
-
isoform
PKCeta
P24723
isozyme
PKCgamma
P05129
isozyme
PKCgamma
P63318
isozyme
PKCgamma
-
isoform
PKCiota
Q62074
-
PKCiota/lambda
P41743
isozyme
PKCnu
O94806
-
PKCtheta
-
-
PKCtheta
Q04759
isozyme
PKCthetaC1B
-
C1B subdomain
PKCzeta
Q05513
isozyme
PKD2
Q9BZL6
-
protein kinase C
-
-
-
-
protein kinase C
P13678
-
protein kinase C
-
-
protein kinase C
-
-
protein kinase C
-
-
protein kinase C alpha
P17252
-
protein kinase C betaII
-
-
protein kinase C delta
-
-
protein kinase C delta
P28867
-
protein kinase C delta
P09215
-
protein kinase C, alpha type
P04409
-
protein kinase C, alpha type
P17252
-
protein kinase C, alpha type
P20444
-
protein kinase C, alpha type
P10102
-
protein kinase C, alpha type
P05696
-
protein kinase C, beta type
P05126
-
protein kinase C, beta type
P05771
-
protein kinase C, beta type
P05772
-
protein kinase C, brain isoenzyme
P05130
-
protein kinase C, D2 type
Q9BZL6
-
protein kinase C, delta type
Q05655
-
protein kinase C, delta type
P28867
-
protein kinase C, delta type
P09215
-
protein kinase C, epsilon type
Q02156
-
protein kinase C, epsilon type
P16054
-
protein kinase C, epsilon type
P10830
-
protein kinase C, epsilon type
P09216
-
protein kinase C, eta type
P24723
-
protein kinase C, eta type
P23298
-
protein kinase C, eta type
Q64617
-
protein kinase C, gamma type
P05129
-
protein kinase C, gamma type
P63318
-
protein kinase C, gamma type
P10829
-
protein kinase C, iota type
P41743
-
protein kinase C, iota type
Q62074
-
protein kinase C, mu type
Q15139
-
protein kinase C, nu type
O94806
-
protein kinase C, theta type
Q04759
-
protein kinase C, zeta type
Q05513
-
protein kinase C, zeta type
Q02956
-
protein kinase C, zeta type
O19111
-
protein kinase C, zeta type
P09217
-
protein kinase C-delta
P09215
-
protein kinase C-epsilon
Q02156
-
protein kinase C-eta
Q64617
-
protein kinase C-like
Q00078
-
protein kinase C-like
Q99014
-
protein kinase C-like 1
P34722
-
protein kinase C-like 1
P43057
-
protein kinase C-like 1
Q16512
-
protein kinase C-like 1
Q63433
-
protein kinase C-like 1
P24583
-
protein kinase C-like 1
P36582
-
protein kinase C-like 2
P34885
-
protein kinase C-like 2
Q16513
-
protein kinase C-like 2
P36583
-
protein kinase C-zeta
P09217
isozyme
protein kinase Calpha
-
-
protein kinase Calpha
-
-
protein kinase Cdelta
P28867
-
protein kinase Cdelta
P09215
-
protein kinase D2
Q9BZL6
-
protein kinase epsilon
-
isoform
protein kinase-C
-
-
-
-
protein kinase-C
-
-
epsilonPKC
-
-
-
-
additional information
Q1H8W8
the enzyme belongs to the family of serine/threonine kinases
additional information
-
PKC occurs in multiple isozymes, designated as classical, novel, and atypical isozymes, belonging to the PKC family
additional information
-
PKCs form a family of related serine/threonine kinases that are part of the AGC-type kinase, kinase G/protein kinase C-family kinase, superfamily
CAS REGISTRY NUMBER
COMMENTARY
141436-78-4
calcium-dependent protein kinase C
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
multiple isozymes: classical isozymes alpha, betaI, betaII, and gamma, novel isozymes delta, epsilon, eta, and theta
-
-
Manually annotated by BRENDA team
female and male, several isozymes
-
-
Manually annotated by BRENDA team
enzyme forms alpha, betaI ans betaII, gamma, epsilon, delta, zeta
-
-
Manually annotated by BRENDA team
isozyme PKCbeta; WB strain, ATCC 30957, isozymes beta, delta, epsilon, theta and zeta
SwissProt
Manually annotated by BRENDA team
catfish, female
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
conventional, novel, and atypical isozyme types, overview
-
-
Manually annotated by BRENDA team
isoform PKCbetaII
-
-
Manually annotated by BRENDA team
isozyme pKCalpha
-
-
Manually annotated by BRENDA team
isozymes PKCbetaII and PKCbetaI
-
-
Manually annotated by BRENDA team
multiple isozymes: classical isozymes alpha, betaI, betaII, and gamma, novel isozymes delta, epsilon, eta, and theta, and atypical isozymes zeta and jota
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
C57BL/6 mice
-
-
Manually annotated by BRENDA team
conventional, novel, and atypical isozyme types, overview
-
-
Manually annotated by BRENDA team
isozyme PKCdelta
-
-
Manually annotated by BRENDA team
isozyme PKCepsilon
-
-
Manually annotated by BRENDA team
isozymes PKCepsilon and PKCzeta
-
-
Manually annotated by BRENDA team
multiple isozymes: classical isozymes alpha, betaI, betaII, and gamma, novel isozymes delta, epsilon, eta, and theta, and atypical isozymes zeta and lambda
-
-
Manually annotated by BRENDA team
PKC isoforms can be split into three groups: conventional, novel and atypical, overview
-
-
Manually annotated by BRENDA team
several isozymes
-
-
Manually annotated by BRENDA team
Mus musculus C57BL/6
C57BL/6 mice
-
-
Manually annotated by BRENDA team
Ca2+-dependent isozyme
-
-
Manually annotated by BRENDA team
conventional, novel, and atypical isozyme types, overview
-
-
Manually annotated by BRENDA team
isozyme pKCalpha
-
-
Manually annotated by BRENDA team
isozyme PKCdelta
-
-
Manually annotated by BRENDA team
isozymes alpha, betaI, betaII, and gamma
-
-
Manually annotated by BRENDA team
isozymes alpha, betaI, betaII, gamma, delta, epsilon, lambda, eta, theta, and zeta
-
-
Manually annotated by BRENDA team
Long-Evans rat pups, several isozymes
-
-
Manually annotated by BRENDA team
male sprague-dawley rats
-
-
Manually annotated by BRENDA team
male Wistar rats
-
-
Manually annotated by BRENDA team
several isozymes
-
-
Manually annotated by BRENDA team
several PKC isozymes
-
-
Manually annotated by BRENDA team
Sprague-Dawley rats
-
-
Manually annotated by BRENDA team
Sprague-Dawley rats, isozyme PKCalpha
-
-
Manually annotated by BRENDA team
Sprague-Dawley rats, several isozymes
-
-
Manually annotated by BRENDA team
Wistar rats
-
-
Manually annotated by BRENDA team
Wistar-Kyoto and spontaneously hypertensive rats
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
knockdown of PKCalpha almost completely reduces myristoylated alanine-rich C kinase substrate phosphorylation, indicating that PKCalpha is responsible for the majority of phosphorylated myristoylated alanine-rich C kinase substrate in the cells
malfunction
-
depletion of PKCepsilon in human endothelial cells reduces expression of the cytoprotective genes A1, A20 and Bcl-2. Constitutively active PKCepsilon expressed in human endothelial cells increases mRNA and protein levels of these cytoprotective genes, with up-regulation dependent upon ERK1/2 (extracellular-signal regulated kinase 1/2) activation
malfunction
-
knockdown of PKCdelta accelerates T-cell receptor-induced NF-kappaB activation and IL-2 secretion, suggesting an inhibitory role of PKCdelta in T-cell receptor-mediated NF-kappaB activation. PKCdelta inhibits T-cell receptor-induced NF-kappaB activation by steric hindrance of recruiting TRAF6 to CARMA1 signalosome, overexpression of PKCdelta inhibits CARMA1-mediated NF-kappaB activation
malfunction
-
PKC-beta1 and PKC-gamma are important for the development of retinal, as their absence completely inhibits rod differentiation
metabolism
-
PKC activity controls serine racemase phosphorylation and D-serine levels both in vitro and in vivo
physiological function
-
PKC plays a protective role in cells exposed to cadmium, as its early activation by 4beta-phorbol 12-myristate 13-acetate reduces both delayed extracellular signal-related kinase activation and cadmium toxicity, whereas blocking its activity has the opposite effect
physiological function
-
a significant decline of STAT3 tyrosine phosphorylation is observed by activation of PKC, while inhibition of PKC results in an increase of phosphorylated STAT3 along with a delayed cell cycle exit of progenitors with prolonged PCNA expression
physiological function
-
activation of protein kinase C significantly attenuates starvation- or rapamycin-induced LC3 processing. The formation of autophagosomes in response to starvation or rapamycin is blocked by PKC activators. PKC inhibitors dramatically induce LC3 processing and autophagosome formation
physiological function
-
metabotropic P2Y receptor-mediates ATP stimulated Na+-ATPase activity through the activation of protein kinase C
physiological function
-
phosphorylation of Galpha-interacting, vesicle-associated protein (GIV) by PKCtheta inhibits GIV's guanine exchange factor (GEF) function and generates a unique negative feedback loop for downregulating the GIV-Gi axis of prometastatic signaling downstream of multiple ligand-activated receptors
physiological function
-
phosphorylation of RalB by PKCalpha is critical for RalB-mediated vesicle trafficking and exocytosis
physiological function
-
PKCepsilon plays an important role as an upstream regulator of endothelial cytoprotection through both the specific induction of protective genes, as well as suppression of pro-inflammatory responses
physiological function
-
PKCeta activates NF-kappaB in MCF-7 cells by activating the IkappaB kinase (IKK) and the degradation of IkappaB. PKCeta enhances the nuclear translocation and transactivation of NF-kappaB under non-stressed conditions and in response to the anticancer drug camptothecin
physiological function
-
PKCzeta kinase inhibition reduces CSF-1 supported mitogenesis in 32D.R cells. Its overexpression increases CSF-1 mitogenic responsiveness. PKCzeta's promotion of mitogenic signaling in 32D.R cells is independent of NF-kB. In primary murine bone marrow derived macrophages (BMMs), PKCzeta inhibition has a more modest effect on CSF-1 dependent mitogenesis, and, pan-PKC inhibition has a paradoxically enhancing effect on MEK-Erk phosphorylation. Thus the importance of PKCzeta in the control of CSF-1 mediated MEKErk activity and mitogenesis depends on differentiation stage
physiological function
-
Rab11 phosphorylation might be implicated in recycling transport regulation
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
alphatomega peptide + ATP
ADP + phosphorylated-alphatomega peptide
show the reaction diagram
-
an improved PKCalpha-responsive polyion complex (PIC) to measure PKCalpha activity is reported. The polycation molecule is the poly(amidoamine) (PAMAM) dendrimer modified with both cationic PKCalpha-specific peptide substrates (alphatomega, FKKQGSFAKKK-NH2) and near infrared (NIR) fluorophores (Cy5.5), and the polyanion molecule is the quencher (BHQ-3)-modified chondroitin sulfate
-
-
?
Arg-Phe-Ala-Arg-Lys-Gly-Ser-Leu-Arg-Gln-Lys-Asn-Val + ATP
Arg-Phe-Ala-Arg-Lys-Gly-phosphoSer-Leu-Arg-Gln-Lys-Asn-Val + ADP
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + ADAM17
ADP + phosphorylated ADAM17
show the reaction diagram
-
-
-
-
?
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
phosphorylation by PKC isozymes at Ser473, regulation of the phosphorylation activity by PKCbetaII in mast cells stimulated by stem cell factor or interaleukin-3, and in serum-stimulated fibroblasts, and in antigen-receptor stimulated T- or B-lymphocytes, overview, Akt substrate is protein kinase B, phosphorylation by PKC isozymes at Ser473 involving phorbol esters
-
-
?
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
phosphorylation on Ser473 by isozyme PKCbetaII
-
-
?
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
PKCalpha inhibits Akt activity that is necessary for proper ubiquitin-specific protease 8 expression
-
-
?
ATP + alpha1D Ca channel
ADP + phosphorylated alpha1D Ca channel
show the reaction diagram
-
-
-
-
?
ATP + Bcl-xL
ADP + phosphorylated Bcl-xL
show the reaction diagram
-
recombinant human substrate, recombinant isozyme PKCdelta
-
-
?
ATP + Bcl-xL
ADP + phosphorylated Bcl-xL
show the reaction diagram
-
recombinant human substrate, recombinant isozymes PKCepsilon and PKCzeta
-
-
?
ATP + Btk
ADP + phosphorylated Btk
show the reaction diagram
-
specific phosphorylation leads to inhibition of Btk membrane translocation and activation and the downstream events that promote PKCbeta activation, mechanism, overview, specific phosphorylation of the tyrosine protein kinase at Ser180 within the Tec-homology domain
-
-
?
ATP + calcium-activated potassium channel alpha subunit Slo1
ADP + phosphorylated calcium-activated potassium channel alpha subunit Slo1
show the reaction diagram
-
-
-
-
?
ATP + calcium-independent phospholipase A2
ADP + phosphorylated calcium-independent phospholipase A2
show the reaction diagram
-
PKC regulates membrane-associated, calcium-independent phospholipase A2 in coronary artery endothelial cells in competition to thrombin, overview
-
-
?
ATP + calmodulin
ADP + phosphorylated calmodulin
show the reaction diagram
-
phosphorylation at Thr497 in the calmodulin-binding domain, binding is competitive to substrate endothelial nitric oxide synthase
-
-
?
ATP + diacylglycerol kinase-zeta
ADP + phosphorylated diacylglycerol kinase-zeta
show the reaction diagram
-
the enzyme, especially isozyme PKCalpha, inhibits binding of diacylglycerol kinase-zeta to the retinoblastoma protein, isozyme PKCalpha
-
-
?
ATP + EF factor 1
ADP + phosphorylated EF factor 1
show the reaction diagram
-
i.e. eukaryotic translation elongation factor 1-alpha1, in vitro phosphorylation
-
-
?
ATP + endothelial nitric oxide synthase
ADP + phosphorylated endothelial nitric oxide synthase
show the reaction diagram
-
the enzyme is responsible for the negative regulation of endothelial nitric oxide synthase, a key enzyme in nitric oxide-mediated signal transduction, phosphorylation reduces the affinity of nitric oxide synthase for calmodulin, phosphorylation at Thr497 in the calmodulin-binding domain, binding is competitive to substrate calmodulin
-
-
?
ATP + extracellular signal-regulated kinase 2
ADP + phosphorylated extracellular signal-regulated kinase 2
show the reaction diagram
-
-
-
-
?
ATP + extracellular signal-related kinase
ADP + phosphorylated extracellular signal-related kinase
show the reaction diagram
-
-
-
-
?
ATP + FKKQGSFAKKK
ADP + phosphorylated FKKQGSFAKKK
show the reaction diagram
-
highly specific substrate for isozyme PKCalpha relative to other isozymes, 60% phosphorylation rate with isozyme PKCalpha, less than 20% phosphorylation rate with other PKC isozymes
-
-
?
ATP + Fyn
ADP + phosphorylated Fyn
show the reaction diagram
-
Fyn is a tyrosine protein kinase of the Src family, phosphorylation at a serine residue
-
-
?
ATP + Galpha-interacting, vesicle-associated protein
ADP + phosphorylated-Galpha-interacting, vesicle-associated protein
show the reaction diagram
-
PKCtheta, down-regulates Galpha-interacting, vesicle-associated protein (GIV's) guanine exchange factor, GEF function by phosphorylating Ser-1689 located within GIV's GEF motif. PKCtheta specifically binds and phosphorylates GIV at S1689, and this phosphoevent abolishes GIV's ability to bind and activate trimeric G proteins Galphai
-
-
-
ATP + GluR6 kainate receptor subunit
ADP + phosphorylated GluR6 kainate receptor subunit
show the reaction diagram
-
two specific residues on the GluR6 C terminus, Ser846 and Ser868, are phosphorylated by protein kinase C, PKC phosphorylation of GluR6 retains GluR6 in the endoplasmic reticulum
-
-
?
ATP + glycine transporter 2
ADP + phosphorylated glycine transporter 2
show the reaction diagram
-
-
-
-
?
ATP + hematopoietic-specific G-protein Galpha15
ADP + phosphorylated hematopoietic-specific G-protein Galpha15
show the reaction diagram
-
recombinant substrate expressed in COS-7 cells, phosphorylation at Ser334, mutant G-protein Galpha15 S334A is inactive as substrate for PKC
-
-
?
ATP + hematopoietic-specific G-protein Galpha15 peptide
ADP + phosphorylated hematopoietic-specific G-protein Galpha15 peptide
show the reaction diagram
-
the PKC phosphorylation site peptide sequence RKGSR includes Ser334
-
-
?
ATP + hematopoietic-specific G-protein Galpha16
ADP + phosphorylated hematopoietic-specific G-protein Galpha16
show the reaction diagram
-
substrate from HL-60 cells, phosphorylation at Ser336, mutant G-protein Galpha16 S336A is inactive as substrate for PKC
-
-
?
ATP + hematopoietic-specific G-protein Galpha16 peptide
ADP + phosphorylated hematopoietic-specific G-protein Galpha16 peptide
show the reaction diagram
-
the PKC phosphorylation site peptide sequence KKGARSRR includes Ser336
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
-
in presence of absence of phosphatidylserine-containing liposomes
-
-
?
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
Q9BZL6
PKD2 activated by phorbol esters efficiently phosphorylate the exogenous substrate histone H1
-
-
?
ATP + histone H1-IIIS
ADP + phosphorylated histone H1-IIIS
show the reaction diagram
Q1H8W8
isozyme PKCbeta
-
-
?
ATP + histone H2
ADP + phosphorylated histone H2
show the reaction diagram
-
in vitro phosphorylation
-
-
?
ATP + histone H3
ADP + phosphorylated histone H3
show the reaction diagram
-
in vitro phosphorylation
-
-
?
ATP + histone III-SS
ADP + phosphorylated histone III-SS
show the reaction diagram
-
commercial substrate
-
-
?
ATP + histone IIIS
ADP + phosphorylated histone IIIS
show the reaction diagram
Q64617
poor substrate
-
-
?
ATP + inhibitory killer cell Ig-like receptor
ADP + phosphorylated inhibitory killer cell Ig-like receptor
show the reaction diagram
-
the enzyme regulates expression and function of inhibitory killer cell Ig-like receptors in NK cells, KIR negatively regulate NK cell cytotoxicity by activating Src homology 2 domain-containing protein tyrsine phospatase 1 and 2, overview, phosphorylation of the cytoplasmic tail, mutational analysis of kinase phosphorylation sites, e.g. Ser394, activity with substrate mutants, overview
-
-
?
ATP + insulin receptor
ADP + phosphorylated insulin receptor
show the reaction diagram
-
isozyme PKCalpha
-
-
?
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
show the reaction diagram
-
phosphorylation of insulin receptor substrate proteins on serine residues is an important posttranslational modification that is linked to insulin resistance, overview, a bona fide substrate for conventional isozymes PKCalpha, PKCzeta, and PKCdelta, phosphorylation of IRS1 at Ser24 in the N-terminal pleckstrin homology domain of IRS1, additionally isozyme PKCalpha is indirectly involved in Ser307 and Ser612 phosphorylation
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
-
Ser357 of rat insulin receptor substrate-1 is a PKC-delta phosphorylation site
-
-
?
ATP + insulin receptor substrate-3
ADP + phosphorylated insulin receptor substrate-3
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor substrate-4
ADP + phosphorylated insulin receptor substrate-4
show the reaction diagram
-
-
-
-
?
ATP + IRS
ADP + phosphorylated IRS
show the reaction diagram
-
isozymes PKCalpha and PKCdelta, phosphorylation on Ser307
-
-
?
ATP + lamin A
ADP + phosphorylated lamin A
show the reaction diagram
-
a nuclear membrane protein, isozyme PKCalpha
-
-
?
ATP + lamin C
ADP + phosphorylated lamin C
show the reaction diagram
-
a nuclear membrane protein, isozyme PKCalpha, phosphorylation at Ser572
-
-
?
ATP + LC3
ADP + phosphorylated LC3
show the reaction diagram
-
-
-
-
?
ATP + metabotropic glutamate receptor 5
ADP + phosphorylated metabotropic glutamate receptor 5
show the reaction diagram
-
isozyme-specific phosphorylation of metabotropic glutamate receptor 5 by PKCdelta blocks Ca2+ oscillation and oscillatory translocation of Ca2+-dependent PKCgamma, phosphorylation at Thr840, PKCdelta is active with wild-type substrate and mutant T840A, but not with mutant T840D, no phosphorylation by PKCgamma
-
-
?
ATP + mutant protein p22phox(P156Q)
ADP + phosphorylated mutant protein p22phox(P156Q)
show the reaction diagram
-
-
-
-
?
ATP + mutant protein p22phox(T132A)
ADP + phosphorylated mutant protein p22phox(T132A)
show the reaction diagram
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
P43057
-
-
-
?
ATP + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
-
the substrate is involved in actincytoskeletal rearrangement in response to extra-cellular stimuli, phosphorylation of MARCKS is dramatically upregulated specifically in microglial cells after kainic acid-induced seizures, but not in other types of glial cells, overview
-
-
?
ATP + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
-
a major PKC substrate
-
-
?
ATP + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
Mus musculus C57BL/6
-
the substrate is involved in actincytoskeletal rearrangement in response to extra-cellular stimuli, phosphorylation of MARCKS is dramatically upregulated specifically in microglial cells after kainic acid-induced seizures, but not in other types of glial cells, overview
-
-
?
ATP + Na,K-ATPase
ADP + phosphorylated Na,K-ATPase
show the reaction diagram
-
substrate in membrane vesicles from the rectal gland of the spiny dog fish Squalus acanthias
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + Par-3
ADP + phosphorylated Par-3
show the reaction diagram
-
-
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
-
phosphoinositide-dependent kinases are conserved substrates of PKC
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
-
i.e. PDK, phosphorylation at Ser744 and Ser748 in the activation loop of the catalytic domain of PKD
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
-
i.e. PDK, phosphorylation at Ser744 and Ser748 in the activation loop of the catalytic domain of PKD, reaction is regulated by diacylglycerol
-
-
?
ATP + phospholipase D1
ADP + phosphorylated phospholipase D1
show the reaction diagram
-
phosphorylation by PKC
-
-
?
ATP + phospholipase D2
ADP + phosphorylated phospholipase D2
show the reaction diagram
-
phosphorylation by PKCalpha
-
-
?
ATP + PKC-alpha-derived peptide
ADP + phosphorylated PKC-alpha-derived peptide
show the reaction diagram
Q05513
in the presence of the classical PKC activators phosphatidylserine/diacylglycerol, PKC alpha phosphorylates a PKC-alpha pseudosubstrate-derived peptide, an epidermal-growth-factor-receptor-derived peptide, histone III-S and myelin basic protein to an equal extent, whilst PKC zeta phosphorylates only the PKC-alpha-derived peptide
-
-
?
ATP + poly(ADP-ribose) polymerase-1
ADP + phosphorylated poly(ADP-ribose) polymerase-1
show the reaction diagram
-
-
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
Q15139
autophosphorylation
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
Q62074
autophosphorylation
-
-
?
ATP + protein p22phox
ADP + phosphorylated protein p22phox
show the reaction diagram
-
threonine 147 of protein p22phox is phosphorylated by PKC-alpha and PKC-delta isoforms in vitro
-
-
?
ATP + RalB
ADP + phosphorylated RalB
show the reaction diagram
-
PKCalpha phosphorylates RalB on Ser-192 and Ser-198 in the hypervariable sequence and Ser-198 phosphorylation promotes activation of RalB and causes RalB relocalization from the plasma membrane to late endosomes
-
-
?
ATP + RFARKGSLRQKNV
ADP + phoshorylated RFARKGSLRQKNV
show the reaction diagram
-
a commercially available peptide substrate
-
-
?
ATP + RFARKGSLRQKNV
ADP + phosphorylated RFARKGSLRQKNV
show the reaction diagram
-
-
-
-
?
ATP + RFARKGSLRQKNV
ADP + RFARKGphosphoSLRQKNV
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + ribosomal protein S6-(229-239) peptide analogue
ADP + phosphorylated ribosomal protein S6-(229-239) peptide analogue
show the reaction diagram
-
-
-
-
?
ATP + serine racemase
ADP + phosphorylated serine racemase
show the reaction diagram
-
-
-
-
?
ATP + serotonin N-acetyltransferase
ADP + phosphorylated serotonin N-acetyltransferase
show the reaction diagram
-
PKC regulates the activity and stability of serotonin N-acetyltransferase in vivo, recombinant enzyme expressed in COS-7 cells, recombinant enzyme expressed in COS-7 cells, phosphorylation at Thr29
-
-
?
ATP + sodium channel
ADP + phosphorylated sodium channel
show the reaction diagram
-
PKC mediates inhibition of sodium channels and tetrodotoxin-sensitive transient sodium current by phosphorylation by topiramate, overview
-
-
?
ATP + store-operated channel
ADP + phosphorylated store-operated channel
show the reaction diagram
-
-
-
-
?
ATP + transient receptor potential protein V4
ADP + phosphorylated transient receptor potential protein vanilloid 4
show the reaction diagram
-
-
-
-
?
ATP + transient receptor potential protein vanilloid 1
ADP + phosphorylated transient receptor potential protein vanilloid 1
show the reaction diagram
-
-
-
-
?
ATP + transient receptor potential vanilloid 5
ADP + phosphorylated transient receptor potential vanilloid 5
show the reaction diagram
-
-
-
-
?
ATP + vascular endothelial growth factor receptor 2
ADP + phosphorylated vascular endothelial growth factor receptor 2
show the reaction diagram
-
phosphorylation at Ser1188 and Ser 1191
-
-
?
ATP + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
-
phosphorylation at Ser157
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
-
involved in regulation of endocytosis and association with adaptor molecules, e.g. Shc, Dab1, or CED-6/GULP
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
-
i.e. LPR, phosphorylation of cytoplasmic domain residues T63, T16, S3, S73, S76, and S79
-
-
?
N6-phenyl-ATP + RFARKGSLRQKNV
N6-phenyl-ADP + RFARKGphosphoSLRQKNV
show the reaction diagram
-
synthetic peptide substrate, recombinant isozyme PKCalpha mutant M417A
-
-
?
Rab11 + ATP
ADP + phosphorylated Rab11
show the reaction diagram
-
Rab11 is differentially phosphorylated in vitro by several purified PKC isoenzymes. Ser 177 is identified as the single PKC-phosphorylated residue in Rab11
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
-
i.e. LPR, phosphorylation of cytoplasmic domain serine and threonine residues
-
-
?
additional information
?
-
-
substrate specificity
-
-
-
additional information
?
-
P43057
preferably phosphorylates the Saccharomyces cerevisiae Pkc1p pseudosubstrate peptide and myelin basic protein, but not histones, protamine or dephosphorylated casein
-
-
-
additional information
?
-
P23298
phorbol ester receptor/protein kinase
-
-
-
additional information
?
-
Q05513
constitutive enzyme
-
-
-
additional information
?
-
P68404
protein kinase C beta controls nuclear factor kappaB activation in B cells through selective regulation of the kappaB kinase alpha
-
-
-
additional information
?
-
-
PKC delta is involved in fundamental cellular functions regulated by diacylglycerols and mimicked by phorbol esters
-
-
-
additional information
?
-
-
the enzyme is a phorbol ester receptor
-
-
-
additional information
?
-
-
overproduction of protein kinase C causes disordered growth control in rat fibroblasts, activation of PKC may be of central importance in the process of multistage carcinogenesis
-
-
-
additional information
?
-
Q05513
PKC zeta exhibits a constitutive kinase
-
-
-
additional information
?
-
O19111
PKC zeta action is involved in growth and differentiation of the collecting duct
-
-
-
additional information
?
-
P09215
PKC deltaIII may show a dominant negative effect against PKC deltaI
-
-
-
additional information
?
-
P28867
protein kinase Cdelta controls self-antigen-induced B-cell tolerance
-
-
-
additional information
?
-
-
key regulatory role in a variety of cellular functions, including apoptosis, as well as cell growth and differentiation
-
-
-
additional information
?
-
-
PKC1-depleted cells arrested growth with small buds. PKC1 may regulate a previously unrecognized checkpoint in the cell cycle
-
-
-
additional information
?
-
P20444
plays a central role in the control of proliferation and differentiation of a wide range of cell types by mediating the signal transduction response to hormones and growth factors
-
-
-
additional information
?
-
P16054
protein kinase C-epsilon increases growth and cause malignant transformation when overexpressed in NIH3T3 cells the catalytic domain of PKC-epsilon, in reciprocal PKC-delta and PKC-epsilon chimeras, is responsible for conferring tumorgenicity to NIH3T3 cells, whereas both regulatory and catalytic domains of PKC-epsilon contribute to in vitro transformation
-
-
-
additional information
?
-
Q15139
in normal rat kidney cells, predominant phosphorylation of a 30000 Da protein at serine residues, constitutive low level expression in normal tissues, elevated expression levels in selected tumor cell lines, a role of PKC mu in signal transduction pathways related to growth control
-
-
-
additional information
?
-
Q05655
PKC-delta desensitizes the Pkc1-mediated pathway by regulating an aspect of G protein function
-
-
-
additional information
?
-
-
enzyme may play a role in signal transduction and growth regulatory pathways unique to hematopoietic cells
-
-
-
additional information
?
-
-
activation of metabotropic glutamate receptor 5 induces translocation of PKCgamma and PKCdelta to plasma membrane and elicits cyclical translocations of myristoylated alanine-rich PKC substrate from plasma membrane to cytosol
-
-
-
additional information
?
-
-
alterations in PKC isoenzyme alpha, delta, and epsilon expression and autophosphorylation during the progression of pressure overload-induced left ventricular hypertrophy
-
-
-
additional information
?
-
-
bidirectional regulation of renal cortical Na+,K+-ATPase by PKC
-
-
-
additional information
?
-
-
calcium-dependent protein kinase C activation occurs in acutely isolated neurons during oxygen and glucose deprivation
-
-
-
additional information
?
-
-
Helicobacter pylori activates the enzyme in gastric epithelial cells limiting interleukin-8 production, induced by the pathogen, through suppression of extracellular signal-regulated kinase ERK activation, mechanism overview
-
-
-
additional information
?
-
-
identification of isozymes being involved in calcium-independent phospholipase A2 activation in coronary artery endothelial cells,overview
-
-
-
additional information
?
-
-
intestinal sugar absorption is regulated by phosphorylation and turnover of protein kinase C betaII mediated by phosphatidylinositol 3-kinase and mammalian target of rapamycin-dependent pathways, PKC betaII regulation and degradation control, overview
-
-
-
additional information
?
-
-
isozyme-specific and developmental stage-specific alterations in brain PKC following exposure to a polychlorinated biphenyl mixture
-
-
-
additional information
?
-
-
PKC is involved in cellular processes like cell growth, cytoskeleton remodelling, and gene expression regulation, emerging and diverse roles of PKC isozymes in immune cell signalling, i.e macrophage activation, signal transduction pathway of PKC in B- and T-lymphocytes, overview, isozyme theta is associated to NFkappa-B activation in T-cells
-
-
-
additional information
?
-
-
PKC is involved in regulation of acetylcholine release in cholinergic nervous activity in the central nervous system in hypertension
-
-
-
additional information
?
-
-
PKC is involved in signal transduction in the triiodothyronine-activation of forebrain, i.e. telencephalon and hypothalamus
-
-
-
additional information
?
-
-
PKC isozymes are involved in signal transduction, required for defense against fungal infection
-
-
-
additional information
?
-
-
PKC isozymes are involved in signal transduction, required for host defense
-
-
-
additional information
?
-
-
PKC mediates NF-kappaB activation, pathway overview, PKC isozymes have distinct roles in regulation of B-cell activation and function, e.g. signal transduction, isozyme PKCbeta is essential for B-cell antigen receptor-induced NF-kappaB activation and B-cell survival, isozyme PKCdelta is required for maintainance of self-reactive B-cell tolerance
-
-
-
additional information
?
-
-
PKC regulates Na,K-ATPase isozyme alpha1 specifically via isozyme-specific regions, while it has no effect on isozyme alpha3, overview
-
-
-
additional information
?
-
-
PKCgamma positively regulates P2X7 receptor-mediated calcium signalling in type-2 astrocytes, mechanism, overview
-
-
-
additional information
?
-
-
PKCtheta is important in regulation of immune response in T-cells, overview, PKC is involved in NF-kappaB activation pathways in vivo, overview, PKC isozymes are involved in signal transduction, and thereby in cell adhesion and migration, isozyme PKCtheta is recruited to the plasma membrane by a cytoskeleton-dependent mechanism regulating the Rac-1 guanine nucelotide exchange protein Vav-1
-
-
-
additional information
?
-
-
PKCtheta is important in regulation of immune response in T-cells, overview, PKC is involved in NF-kappaB activation pathways in vivo, overview, PKCdelta acts as negative regulator by feedback inhibition of the CDgamma3 subunit important for immune response in T lymphocytes, overview, PKC isozymes are involved in signal transduction, and thereby in cell adhesion and migration, isozyme PKCtheta is recruited to the plasma membrane by a cytoskeleton-dependent mechanism regulating the Rac-1 guanine nucelotide exchange protein Vav-1
-
-
-
additional information
?
-
-
regulation of amphetamine-stimulated dopamine efflux by PKCbetaII, overview
-
-
-
additional information
?
-
-
some PKC isozymes inhibit BKCa channel activity in pulmonary arterial smooth muscle via inhibition of cAMP-induced activation of the BKCa channel
-
-
-
additional information
?
-
-
the enzyme is essential for transduction of signals in a wide range of cell types, including neurons
-
-
-
additional information
?
-
-
the enzyme is important in signal transduction from extracellular signals to intracellular responses involving the second messengers Ca2+ and diacylglycerol, processing mechanism and regulation overview
-
-
-
additional information
?
-
-
the enzyme is important in signal transduction from extracellular signals to intracellular responses involving the second messengers Ca2+ and diacylglycerol, processing mechanism and regulation overview, PKC is important in diverse biological functions, e.g. in cell proliferation, cell differentiation, immune response, cancer, and memory
-
-
-
additional information
?
-
-
activation of phospholipase D2 by 4beta-phorbol 12-myristate 13-acetate-induced PKCalpha does not require phosphorylation, overview
-
-
-
additional information
?
-
-
activity with wild-type and mutant substrate low density lipoprotein receptor-related protein, overview
-
-
-
additional information
?
-
-
interaction between PKCdelta and Fyn leads to phosphorylation on tyrosine and on serine, respectively, with Fyn kinase being activated by the snake venom alboaggregin-A
-
-
-
additional information
?
-
-
isozymes alpha, delta, and epsilon perform autophosphorylation
-
-
-
additional information
?
-
-
myristoylated alanine-rich PKC substrate is repetitively phosphorylated by oscillating gammaPKC on the plasma membrane
-
-
-
additional information
?
-
-
phosphorylation by PKC is involved in regulation of hematopoietic-specific G-protein Galpha15 and Galpha16, deletion of the PKC phosphorylation site leads to inhibition of receptor-coupled phospholipase C activation
-
-
-
additional information
?
-
-
PKC interacts with CARMA-1, involved in signaling from PKC to NF-kappaB
-
-
-
additional information
?
-
-
regulatory interactions of isozymes with other kinases, overview
-
-
-
additional information
?
-
-
substrate specificity of PKC isozymes, PKC isozymes interacting proteins, overview
-
-
-
additional information
?
-
-
the enzyme depends on basic residues for substrate recognition, autoregulation by a pseudosubstrate mechanism, overview
-
-
-
additional information
?
-
-
activation-induced upregulation of inhibitory killer Ig-like receptors, KIR, is regulated by PKC at the posttranscriptional level via the cytoplasmic tail of KIR by stimulation of the maturation processes in the endoplasmic reticulum-Golgi and by promoting the recycling of surface KIR through sorting endosomes, isozyme PKCdelta plays a role in the exocytosis of KIR in secretory lysosomes, overview
-
-
-
additional information
?
-
-
involvement of isozyme PKCalpha in the early action of angiotensin II type 2 effects on neurite outgrowth in NG108-15 cells, the angiotensin II type 2-receptor inhibits PKC alpha and p21ras activity, inhibition of PKCalpha is not directly involved in the Rap1-MEK-p42/p44mapk cascade, overview
-
-
-
additional information
?
-
-
isozyme PKC-delta inhibits colon cancer cell proliferation by selective changes in cell cycle, arresting cells in the G1 phase, and cell death regulators enhancing apoptosis using two different mechanisms, e.g. by downregulation expression of cyclin E and D1, and Bcl-2, inducing Bax expression, and altering levels of p27Kip1 and p21Waf1, PKC-delta is thus an important tumor suppressor in colonic carcinogenesis, overview
-
-
-
additional information
?
-
Q1H8W8
isozyme PKCbeta is involved in encystment
-
-
-
additional information
?
-
-
isozyme PKCdelta inhibits the production of proteolytic enzymes in murine mammary cells, the PKCdelta effect is mediated by the MEK/ERK pathway, overview
-
-
-
additional information
?
-
-
PKC isoform specificity of cholinergic potentiation of glucose-induced pulsatile 5-HT/insulin release from single mouse pancreatic islets, overview
-
-
-
additional information
?
-
-
PKC signalling has been suggested to play a role in Ca2+ entry, granule secretion, alphaIIbbeta3 activation and outside-in signalling, PKC also is involved in receptor desensitization, extrusion of intracellular Ca2+, secretion and actin-mediated filopodia formation, PKC negatively regulates platelet activation and the diverse processes in which active platelet are involved, detailed overview, PKC increases Ca2+ extrusion from the cytosol and desensitizes some G-protein coupled receptors, isozyme PKCdelta inhibits platelet aggregation by inhibiting VASP phosphorylation at Ser157, reducing filopodial extension, overview, PKCdelta is required for dense granule secretion following stimulation by thrombin, and plays a negative regulatory role in dense granule secretion when platelets are stimulated by convulxin, PKCtheta is also required for outside-in signalling and, as with PKCbeta, platelets deficient in PKCtheta do not fully spread on a fibrinogen-coated surface
-
-
-
additional information
?
-
-
regulation of PKC isozyme expression, overview, specific PKC isozymes act as transducers and modulators of insulin signaling, the activation of PKC isozymes by insulin is modified by several effectors, signaling cascade, overview, isozyme PKCalpha might play a role in insulin resistance, overview
-
-
-
additional information
?
-
-
regulation of PKC isozyme expression, overview, specific PKC isozymes act as transducers and modulators of insulin signaling, the activation of PKC isozymes by insulin is modified by several effectors, signaling cascade, overview, isozyme PKCalpha might play a role in insulin resistance, overview, isozyme PKCepsilon forms signaling complexes with Raf-1 and ERK, isozyme PKCtheta inactivation prevents fat-induced defects in insulin signaling and glucose transport in skeletal muscle
-
-
-
additional information
?
-
-
the enzyme plays a key role in the mechanism of cerebral ischemic/hypoxic preconditioning, the isozymes are differently involved in neuroprotection, overview
-
-
-
additional information
?
-
-
the enzyme plays a role in aldosterone-induced non-genomic inhibition of basolateral potassium IKCa channels in human colonic crypts
-
-
-
additional information
?
-
-
PKCbetaII specifically binds to beta-actin
-
-
-
additional information
?
-
-
pertussis toxin-B suppresses HIV-1 Tat-mediated apoptosis by reducing its activation of phospholipase C-beta through a PKC activation pathway
-
-
-
additional information
?
-
-
PKC plays a pivotal role in desensitization of P2Y1 receptors in RBA-2 astrocytes
-
-
-
additional information
?
-
-
does not phosphorylate insulin receptor substrate-2
-
-
-
additional information
?
-
-
PKC activation alone can target VEGFR2 for limited proteolysis, while PKC inhibition delays VEGFR2 processing but does not block this step
-
-
-
additional information
?
-
-
no phosphorylation of the mutant protein p22phox (T147A) by PKC-alpha or PKC-delta in vitro
-
-
-
additional information
?
-
-
PKCalpha modulates the levels of ubiquitinated epidermal growth factor receptor through Akt and ubiquitin-specific protease 8, PKCalpha is necessary for diacylglycerol kinase delta to modulate ubiquitin-specific protease 8 levels
-
-
-
additional information
?
-
-
PKCepsilon associates with and inhibits activation of the mitochondrial permeability transition pore complex
-
-
-
additional information
?
-
-
quaporin 1 can be trafficked to and from the plasma membrane in response to altered tonicity in a PKC- and microtubule-dependent manner
-
-
-
additional information
?
-
-
thrombin-induced cyclin D1expression requires the activation of conventional PKC isoforms
-
-
-
additional information
?
-
-
tumor necrosis factor alpha-converting enzyme activation is consequent to concomitant actions of intracellular signals mediated by protein kinase C and extracellular signal-regulated kinase as well as reduction of its endogenous inhibitor Timp3
-
-
-
additional information
?
-
-
PKCdelta associates with caspase recruitment domain-containing membrane-associated guanylate kinase 1 (CARMA1), PKCdelta interacts with mucosa-associated lymphoid tissue lymphoma translocation gene 1 (MALT1) and TRAF6
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
phosphorylation by PKC isozymes at Ser473, regulation of the phosphorylation activity by PKCbetaII in mast cells stimulated by stem cell factor or interaleukin-3, and in serum-stimulated fibroblasts, and in antigen-receptor stimulated T- or B-lymphocytes, overview
-
-
?
ATP + Btk
ADP + phosphorylated Btk
show the reaction diagram
-
specific phosphorylation leads to inhibition of Btk membrane translocation and activation and the downstream events that promote PKCbeta activation, mechanism, overview
-
-
?
ATP + calcium-independent phospholipase A2
ADP + phosphorylated calcium-independent phospholipase A2
show the reaction diagram
-
PKC regulates membrane-associated, calcium-independent phospholipase A2 in coronary artery endothelial cells in competition to thrombin, overview
-
-
?
ATP + diacylglycerol kinase-zeta
ADP + phosphorylated diacylglycerol kinase-zeta
show the reaction diagram
-
the enzyme, especially isozyme PKCalpha, inhibits binding of diacylglycerol kinase-zeta to the retinoblastoma protein
-
-
?
ATP + endothelial nitric oxide synthase
ADP + phosphorylated endothelial nitric oxide synthase
show the reaction diagram
-
the enzyme is responsible for the negative regulation of endothelial nitric oxide synthase, a key enzyme in nitric oxide-mediated signal transduction, phosphorylation reduces the affinity of nitric oxide synthase for calmodulin
-
-
?
ATP + histone H1-IIIS
ADP + phosphorylated histone H1-IIIS
show the reaction diagram
Q1H8W8
isozyme PKCbeta
-
-
?
ATP + inhibitory killer cell Ig-like receptor
ADP + phosphorylated inhibitory killer cell Ig-like receptor
show the reaction diagram
-
the enzyme regulates expression and function of inhibitory killer cell Ig-like receptors in NK cells, KIR negatively regulate NK cell cytotoxicity by activating Src homology 2 domain-containing protein tyrsine phospatase 1 and 2, overview
-
-
?
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
show the reaction diagram
-
phosphorylation of insulin receptor substrate proteins on serine residues is an important posttranslational modification that is linked to insulin resistance, overview
-
-
?
ATP + metabotropic glutamate receptor 5
ADP + phosphorylated metabotropic glutamate receptor 5
show the reaction diagram
-
isozyme-specific phosphorylation of metabotropic glutamate receptor 5 by PKCdelta blocks Ca2+ oscillation and oscillatory translocation of Ca2+-dependent PKCgamma
-
-
?
ATP + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
Mus musculus, Mus musculus C57BL/6
-
the substrate is involved in actincytoskeletal rearrangement in response to extra-cellular stimuli, phosphorylation of MARCKS is dramatically upregulated specifically in microglial cells after kainic acid-induced seizures, but not in other types of glial cells, overview
-
-
?
ATP + Na,K-ATPase
ADP + phosphorylated Na,K-ATPase
show the reaction diagram
-
-
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
-
phosphoinositide-dependent kinases are conserved substrates of PKC
-
-
?
ATP + serotonin N-acetyltransferase
ADP + phosphorylated serotonin N-acetyltransferase
show the reaction diagram
-
PKC regulates the activity and stability of serotonin N-acetyltransferase in vivo, recombinant enzyme expressed in COS-7 cells
-
-
?
ATP + sodium channel
ADP + phosphorylated sodium channel
show the reaction diagram
-
PKC mediates inhibition of sodium channels and tetrodotoxin-sensitive transient sodium current by phosphorylation by topiramate, overview
-
-
?
ATP + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
-
phosphorylation at Ser157
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
-
involved in regulation of endocytosis and association with adaptor molecules, e.g. Shc, Dab1, or CED-6/GULP
-
-
?
additional information
?
-
Q05513
constitutive enzyme
-
-
-
additional information
?
-
P68404
protein kinase C beta controls nuclear factor kappaB activation in B cells through selective regulation of the kappaB kinase alpha
-
-
-
additional information
?
-
-
PKC delta is involved in fundamental cellular functions regulated by diacylglycerols and mimicked by phorbol esters
-
-
-
additional information
?
-
-
the enzyme is a phorbol ester receptor
-
-
-
additional information
?
-
-
overproduction of protein kinase C causes disordered growth control in rat fibroblasts, activation of PKC may be of central importance in the process of multistage carcinogenesis
-
-
-
additional information
?
-
Q05513
PKC zeta exhibits a constitutive kinase
-
-
-
additional information
?
-
O19111
PKC zeta action is involved in growth and differentiation of the collecting duct
-
-
-
additional information
?
-
P09215
PKC deltaIII may show a dominant negative effect against PKC deltaI
-
-
-
additional information
?
-
P28867
protein kinase Cdelta controls self-antigen-induced B-cell tolerance
-
-
-
additional information
?
-
-
key regulatory role in a variety of cellular functions, including apoptosis, as well as cell growth and differentiation
-
-
-
additional information
?
-
-
PKC1-depleted cells arrested growth with small buds. PKC1 may regulate a previously unrecognized checkpoint in the cell cycle
-
-
-
additional information
?
-
P20444
plays a central role in the control of proliferation and differentiation of a wide range of cell types by mediating the signal transduction response to hormones and growth factors
-
-
-
additional information
?
-
P16054
protein kinase C-epsilon increases growth and cause malignant transformation when overexpressed in NIH3T3 cells the catalytic domain of PKC-epsilon, in reciprocal PKC-delta and PKC-epsilon chimeras, is responsible for conferring tumorgenicity to NIH3T3 cells, whereas both regulatory and catalytic domains of PKC-epsilon contribute to in vitro transformation
-
-
-
additional information
?
-
Q15139
in normal rat kidney cells, predominant phosphorylation of a 30000 Da protein at serine residues, constitutive low level expression in normal tissues, elevated expression levels in selected tumor cell lines, a role of PKC mu in signal transduction pathways related to growth control
-
-
-
additional information
?
-
Q05655
PKC-delta desensitizes the Pkc1-mediated pathway by regulating an aspect of G protein function
-
-
-
additional information
?
-
-
enzyme may play a role in signal transduction and growth regulatory pathways unique to hematopoietic cells
-
-
-
additional information
?
-
-
activation of metabotropic glutamate receptor 5 induces translocation of PKCgamma and PKCdelta to plasma membrane and elicits cyclical translocations of myristoylated alanine-rich PKC substrate from plasma membrane to cytosol
-
-
-
additional information
?
-
-
alterations in PKC isoenzyme alpha, delta, and epsilon expression and autophosphorylation during the progression of pressure overload-induced left ventricular hypertrophy
-
-
-
additional information
?
-
-
bidirectional regulation of renal cortical Na+,K+-ATPase by PKC
-
-
-
additional information
?
-
-
calcium-dependent protein kinase C activation occurs in acutely isolated neurons during oxygen and glucose deprivation
-
-
-
additional information
?
-
-
Helicobacter pylori activates the enzyme in gastric epithelial cells limiting interleukin-8 production, induced by the pathogen, through suppression of extracellular signal-regulated kinase ERK activation, mechanism overview
-
-
-
additional information
?
-
-
identification of isozymes being involved in calcium-independent phospholipase A2 activation in coronary artery endothelial cells,overview
-
-
-
additional information
?
-
-
intestinal sugar absorption is regulated by phosphorylation and turnover of protein kinase C betaII mediated by phosphatidylinositol 3-kinase and mammalian target of rapamycin-dependent pathways, PKC betaII regulation and degradation control, overview
-
-
-
additional information
?
-
-
isozyme-specific and developmental stage-specific alterations in brain PKC following exposure to a polychlorinated biphenyl mixture
-
-
-
additional information
?
-
-
PKC is involved in cellular processes like cell growth, cytoskeleton remodelling, and gene expression regulation, emerging and diverse roles of PKC isozymes in immune cell signalling, i.e macrophage activation, signal transduction pathway of PKC in B- and T-lymphocytes, overview, isozyme theta is associated to NFkappa-B activation in T-cells
-
-
-
additional information
?
-
-
PKC is involved in regulation of acetylcholine release in cholinergic nervous activity in the central nervous system in hypertension
-
-
-
additional information
?
-
-
PKC is involved in signal transduction in the triiodothyronine-activation of forebrain, i.e. telencephalon and hypothalamus
-
-
-
additional information
?
-
-
PKC isozymes are involved in signal transduction, required for defense against fungal infection
-
-
-
additional information
?
-
-
PKC isozymes are involved in signal transduction, required for host defense
-
-
-
additional information
?
-
-
PKC mediates NF-kappaB activation, pathway overview, PKC isozymes have distinct roles in regulation of B-cell activation and function, e.g. signal transduction, isozyme PKCbeta is essential for B-cell antigen receptor-induced NF-kappaB activation and B-cell survival, isozyme PKCdelta is required for maintainance of self-reactive B-cell tolerance
-
-
-
additional information
?
-
-
PKC regulates Na,K-ATPase isozyme alpha1 specifically via isozyme-specific regions, while it has no effect on isozyme alpha3, overview
-
-
-
additional information
?
-
-
PKCgamma positively regulates P2X7 receptor-mediated calcium signalling in type-2 astrocytes, mechanism, overview
-
-
-
additional information
?
-
-
PKCtheta is important in regulation of immune response in T-cells, overview, PKC is involved in NF-kappaB activation pathways in vivo, overview, PKC isozymes are involved in signal transduction, and thereby in cell adhesion and migration, isozyme PKCtheta is recruited to the plasma membrane by a cytoskeleton-dependent mechanism regulating the Rac-1 guanine nucelotide exchange protein Vav-1
-
-
-
additional information
?
-
-
PKCtheta is important in regulation of immune response in T-cells, overview, PKC is involved in NF-kappaB activation pathways in vivo, overview, PKCdelta acts as negative regulator by feedback inhibition of the CDgamma3 subunit important for immune response in T lymphocytes, overview, PKC isozymes are involved in signal transduction, and thereby in cell adhesion and migration, isozyme PKCtheta is recruited to the plasma membrane by a cytoskeleton-dependent mechanism regulating the Rac-1 guanine nucelotide exchange protein Vav-1
-
-
-
additional information
?
-
-
regulation of amphetamine-stimulated dopamine efflux by PKCbetaII, overview
-
-
-
additional information
?
-
-
some PKC isozymes inhibit BKCa channel activity in pulmonary arterial smooth muscle via inhibition of cAMP-induced activation of the BKCa channel
-
-
-
additional information
?
-
-
the enzyme is essential for transduction of signals in a wide range of cell types, including neurons
-
-
-
additional information
?
-
-
the enzyme is important in signal transduction from extracellular signals to intracellular responses involving the second messengers Ca2+ and diacylglycerol, processing mechanism and regulation overview
-
-
-
additional information
?
-
-
the enzyme is important in signal transduction from extracellular signals to intracellular responses involving the second messengers Ca2+ and diacylglycerol, processing mechanism and regulation overview, PKC is important in diverse biological functions, e.g. in cell proliferation, cell differentiation, immune response, cancer, and memory
-
-
-
additional information
?
-
-
activation-induced upregulation of inhibitory killer Ig-like receptors, KIR, is regulated by PKC at the posttranscriptional level via the cytoplasmic tail of KIR by stimulation of the maturation processes in the endoplasmic reticulum-Golgi and by promoting the recycling of surface KIR through sorting endosomes, isozyme PKCdelta plays a role in the exocytosis of KIR in secretory lysosomes, overview
-
-
-
additional information
?
-
-
involvement of isozyme PKCalpha in the early action of angiotensin II type 2 effects on neurite outgrowth in NG108-15 cells, the angiotensin II type 2-receptor inhibits PKC alpha and p21ras activity, inhibition of PKCalpha is not directly involved in the Rap1-MEK-p42/p44mapk cascade, overview
-
-
-
additional information
?
-
-
isozyme PKC-delta inhibits colon cancer cell proliferation by selective changes in cell cycle, arresting cells in the G1 phase, and cell death regulators enhancing apoptosis using two different mechanisms, e.g. by downregulation expression of cyclin E and D1, and Bcl-2, inducing Bax expression, and altering levels of p27Kip1 and p21Waf1, PKC-delta is thus an important tumor suppressor in colonic carcinogenesis, overview
-
-
-
additional information
?
-
Q1H8W8
isozyme PKCbeta is involved in encystment
-
-
-
additional information
?
-
-
isozyme PKCdelta inhibits the production of proteolytic enzymes in murine mammary cells, the PKCdelta effect is mediated by the MEK/ERK pathway, overview
-
-
-
additional information
?
-
-
PKC isoform specificity of cholinergic potentiation of glucose-induced pulsatile 5-HT/insulin release from single mouse pancreatic islets, overview
-
-
-
additional information
?
-
-
PKC signalling has been suggested to play a role in Ca2+ entry, granule secretion, alphaIIbbeta3 activation and outside-in signalling, PKC also is involved in receptor desensitization, extrusion of intracellular Ca2+, secretion and actin-mediated filopodia formation, PKC negatively regulates platelet activation and the diverse processes in which active platelet are involved, detailed overview, PKC increases Ca2+ extrusion from the cytosol and desensitizes some G-protein coupled receptors, isozyme PKCdelta inhibits platelet aggregation by inhibiting VASP phosphorylation at Ser157, reducing filopodial extension, overview, PKCdelta is required for dense granule secretion following stimulation by thrombin, and plays a negative regulatory role in dense granule secretion when platelets are stimulated by convulxin, PKCtheta is also required for outside-in signalling and, as with PKCbeta, platelets deficient in PKCtheta do not fully spread on a fibrinogen-coated surface
-
-
-
additional information
?
-
-
regulation of PKC isozyme expression, overview, specific PKC isozymes act as transducers and modulators of insulin signaling, the activation of PKC isozymes by insulin is modified by several effectors, signaling cascade, overview, isozyme PKCalpha might play a role in insulin resistance, overview
-
-
-
additional information
?
-
-
regulation of PKC isozyme expression, overview, specific PKC isozymes act as transducers and modulators of insulin signaling, the activation of PKC isozymes by insulin is modified by several effectors, signaling cascade, overview, isozyme PKCalpha might play a role in insulin resistance, overview, isozyme PKCepsilon forms signaling complexes with Raf-1 and ERK, isozyme PKCtheta inactivation prevents fat-induced defects in insulin signaling and glucose transport in skeletal muscle
-
-
-
additional information
?
-
-
the enzyme plays a key role in the mechanism of cerebral ischemic/hypoxic preconditioning, the isozymes are differently involved in neuroprotection, overview
-
-
-
additional information
?
-
-
the enzyme plays a role in aldosterone-induced non-genomic inhibition of basolateral potassium IKCa channels in human colonic crypts
-
-
-
additional information
?
-
-
pertussis toxin-B suppresses HIV-1 Tat-mediated apoptosis by reducing its activation of phospholipase C-beta through a PKC activation pathway
-
-
-
additional information
?
-
-
PKC plays a pivotal role in desensitization of P2Y1 receptors in RBA-2 astrocytes
-
-
-
additional information
?
-
-
PKC activation alone can target VEGFR2 for limited proteolysis, while PKC inhibition delays VEGFR2 processing but does not block this step
-
-
-
additional information
?
-
-
PKCdelta associates with caspase recruitment domain-containing membrane-associated guanylate kinase 1 (CARMA1), PKCdelta interacts with mucosa-associated lymphoid tissue lymphoma translocation gene 1 (MALT1) and TRAF6
-
-
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ATP
-
-
ATP
-
-
ATP
-
preferred by the wild-type PKCalpha
N6-phenyl-ATP
-
preferred by PKCalpha mutant M417A to phosphorylate peptide and protein substrates, no activity with the wild-type PKCalpha
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
-
Ca2+-mediated interactions between the two domains could contribute to enzyme activation as well as to the creation of a positively charged phosphatidylserine-binding site
Ca2+
-
no activation
Ca2+
-
activity is independent of Ca2+
Ca2+
-
enzyme is dependent on Ca2+
Ca2+
-
activates
Ca2+
-
isozymes alpha, betaI, betaII, and gamma require Ca2+ for activity, isozymes delta, epsilon, eta, and theta do not
Ca2+
-
required, second messenger involved in PKC regulation, some isozymes are Ca2+-independent
Ca2+
-
-
Ca2+
-
dependent on, depends on the isozyme, e.g. isozyme betaII and gamma are dependent on Ca2+, while isozyme delta is not
Ca2+
-
PKC isozymes are divided into groups of calcium-independent and of calcium-dependent isozymes
Ca2+
-
binds to C2 domain of PKC, regulatory fucntion for isozymes alpha, betaI, betaII, and gamma, overview
Ca2+
-
binds to C2 domain of PKC, regulatory function for isozymes alpha, betaI, betaII, and gamma, overview
Ca2+
-
calcium-dependent PKC activation in acutely isolated neurons during oxygen and glucose deprivation, involved in PKC activity regulation during ischemia, overview
Ca2+
Q1H8W8
activates, required
Ca2+
-
activates, required
Ca2+
-
activates Ca2+-dependent PKC isozymes
Ca2+
-
stimulates the enzyme, binds to the regulatory domain of PKC, competes with effector curcumin, overview, no effect by cysteine
Ca2+
-
-
Ca2+
-
PKCalpha is a Ca2+-dependent isozyme
Ca2+
-
activates
Ca2+
-
activation mechanism
Ca2+
-
dependent on
Ca2+
-
stimulates activity
Cd2+
-
cell exposure to 0.020 mM cadmium for 24 h results in PKC activation
Mg2+
-
-
Mg2+
-
-
Zn2+
-
the C1 domain of PKC requires two Zn2+ ions for proper folding and stability
Zn2+
-
PKC contains zinc finger structures that are important for its enzymatic activity
Mn2+
-
-
additional information
-
presence of only one cysteine-rich, zinc finger-like domain, absence of an apparent Ca(2+)-binding region
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
1,1'-(1,10-decanediyl)bis[1-amino isoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-amino-1-methylbenzimidazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylbenzothiazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylbenzoxazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-amino-2-methyl quinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-aminoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-N,N,dimethylaminoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[quinolinium] diiodide
-
-
1,1'-decane-1,10-diylbis(4-aminopyridinium) diiodide
-
-
1,1'-decane-1,10-diylbis[4-(dimethylamino)pyridinium]
-
-
1,6-bis[N-(1-methylquinolinium-2-methyl)amino]-hexane diiodide
-
-
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
-
1-(5-isoquinolinesulfonyl)-2-methylpiperazine
-
-
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
-
1-methoxypropan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 49%
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
-
2,7,11-triamino-3,6,13-trihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7,11-triamino-3,6-dihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7-diamino-3,6,13-trihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7-diamino-3,6-dihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
-
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
-
2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carbonitrile
-
0.03 mM, inhibition: 87%
2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylic acid
-
0.03 mM, inhibition: 65%
2-fluorobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
2-methoxyethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
2-methyl-6-(phenylethynyl)-pyridine
-
complete inhibition of PKCgamma oscillation at 0.05 mM
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methyl-N1-[3-(pyridin-3-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 64%
3-(1-(3-(dimethylamino)propyl)-2-methyl-1H-indol-3-yl)-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
a bisindolylmaleimide analogue of BIM-1 inhibitor
3-cyanobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 70%
3-methoxybenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
3-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 67%
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
3-[1-[3-(dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
Go6983, PKC-specific inhibitor, complete inhibition at 500 nM
-
4-amino-1,2-dimethylquinolinium
-
-
4-amino-1-decyl-2-methylquinolinium iodide
-
-
4-cyanobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 10%
4-fluorobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 2%
4-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 50%
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
-
-
alsterpaullone
-
7% inhibition of PKCalpha at 0.01 mM
angiotensin II type 2-receptor
-
inhibits isozyme PKCalpha
-
arachidonoyl fluoromethylketone
-
inhibition of PKCgamma oscillation at 0.1 mM
AVGPRPQT
-
-
benzyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 85%
benzyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 78%
benzyl 2-amino-4-(2-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
benzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
benzyl 2-amino-4-(3-cyanophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 25%
benzyl 2-amino-4-(3-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 53%
benzyl 2-amino-4-(3-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
benzyl 2-amino-4-(3-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 68%
benzyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 86%
benzyl 2-amino-4-(4-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 60%
benzyl 2-amino-4-[3-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 29%
benzyl 2-amino-4-[4-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 21%
betaIIV5.3
-
0.01 mM, peptide translocation inhibitor of isozyme PKC betaII
-
BIM-I
Q1H8W8
inhibits encystment in vivo
bisindolylmaleimide
-
relatively specific for protein kinase C
bisindolylmaleimide
-
strong inhibition of PKCalpha
bisindolylmaleimide derivatives
-
-
bisindolylmaleimide I
-
PKC inhibitors induce LC3 processing and autophagosome formation. Inhibition of protein kinase C increased autophagy
bisindolylmaleimide I
-
-
bromoerol lactone
-
slight inhibition of PKCgamma oscillation at 0.1 mM
calphostin C
-
PKC-specific inhibitor
calphostin C
Q1H8W8
interacts with the regulatory domain of PKC, inhibits encystment in vivo
calphostin C
-
-
calphostin-C
-
inhibition of triiodothyronine-activation in forebrain, overview, can be partially reversed by triiodothyronone, i.e. T3
CG53353
-
inhibitor of isozyme PKCbetaII
CG53353
-
0.01 mM, isozyme PKC betaII antagonist
chelerythrine
-
-
Chelerythrine chloride
Q1H8W8
interacts with the catalytic domain of PKC, inhibits encystment in vivo
cheletrytrine
-
complete inhibition at 0.05 mM
-
compound 48/80
-
complete inhibition of PKCgamma oscillation at 0.1 mM
CRLVLASC
-
targets isozyme PKCgamma, blocks formalin-induced pain response
curcumin
-
inhibits or activates PKC dependent on Ca2+ and the presence of membranes or phosphatidylserine, respectively, in presence of phosphatidylserine curcumin activates PKC, in presence of membranes with phosphatidylserine the enzyme is inhibited, Ca2+ competes with curcumin at the regulatory domainbinding site, overview, effects on different isozymes, overview
cytochalasine D
-
inhibition of PKCgamma oscillation at 0.01 mM
EAVSLKPT
-
targets isozyme PKCepsilon, reverses psi epsilonRACK-mediated protection, and decreases formalin-induced pain response
enzastaurin
-
oral serine/threonine kinase inhibitor
epsilonV1.2
-
0.01 mM, peptide translocation inhibitor of isozyme PKC epsilon
-
ethanol
-
0.03%, inhibition of PKCgamma oscillation at 0.1 mM
ethyl 2-(carbamoylamino)-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 14%
ethyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(2-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 62%
ethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(3-cyanophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 32%
ethyl 2-amino-4-(3-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(3-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 38%
ethyl 2-amino-4-(3-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 82%
ethyl 2-amino-4-(3-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 77%
ethyl 2-amino-4-(4-aminophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(4-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 80%
ethyl 2-amino-4-[3-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 16%; 0.03 mM, inhibition: 30%
ethyl 2-amino-4-[4-(dimethylamino)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 4-(3,4-dimethoxyphenyl)-2-(dimethylamino)thiophene-3-carboxylate
-
0.03 mM, inhibition: 60%
ethyl 4-(3,4-dimethoxyphenyl)-2-(methylamino)thiophene-3-carboxylate
-
0.03 mM, inhibition: 32%
ethyl 4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 3%
FLLDPY
-
-
FNGLLKIKI
-
protects from cardiac ischaemic injury
FTRKRQRAMRRVHQ
-
autoregulatory pseudosubstrate sequence, residues 24-40, lung enzyme
GF 109203X
-
broad-spectrum PKC inhibitor
GF 109203X
-
-
GF109203X
-
specific inhibition of PKC
GF109203X
-
inhibits classical and novel, but not atypical PKC isozymes
GF109203X
-
PKC-specific inhibitor
GF109203X
-
potent inhibitor
GF109203X
-
specific inhibitor
GF109203X
-
bisindolylmaleimide, broad spectrum PKC inhibitor
GF109203X
-
-
GF109203X
-
inhibits all PKC isozymes, except PKCmu
Go6976
-
-
Go6976
-
0.01 mM
Go6976
-
inhibitor of conventional (calcium-dependent) PKC isoforms
Go6979
-
-
-
G 6976
-
slight inhibition of PKCalpha
G 6983
-
-
G-6976
-
inhibits classical, but not novel and atypical PKC isozymes
G-6976
-
selective inhibition of isozymes PKCalpha, PKCbeta, and PKC-my
G-6976
-
IC50 of 2.3-7.9 nM
G6976
-
inhibits classical isozymes
G6976
-
-
G6976
-
an inhibitor of isozymes cPKCalpha, -beta, and -my
G6983
-
an inhibitor of isozyme PKCbeta, but not of PKCmy
H-7
-
specific PKC inhibitor
HDAPIGYD
-
protects from cardiac ischaemic injury, from graft coronary artery disease, and activates potassium current, inhibits sodium current
indirubin-3'-monoxime
-
32% inhibition of PKCalpha at 0.01 mM
K-252a
-
strong inhibition
KGDYEKILVALCGGN
-
targets isozyme PKCbeta
KGDYEKILVALCGGN
-
blocks Xenopus oocyte maturation
KLFIMNL
-
targets isozyme PKCbetaI, inhibits cardiomyocyte hypertrophy
KQKTKTIK T
-
targets isozyme PKCbeta
KQKTKTIK T
-
blocks Xenopus oocyte maturation
LEPEGK
-
-
LY333531
-
specific inhibition of PKCbeta
LY379196
-
highly specific for PKCbeta, inhibits amphetamine-stimulated dopamine efflux in striatum in vivo
-
MRAAEDPM
-
increased injury from cardiac ischaemia
myr-PKC
-
specific protein kinase C inhibitor
-
N,N,N,N',N',N'-hexaethyldecane-1,10-diaminium
-
-
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide
-
-
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide
-
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
-
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-([(3R,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
0.001 mM, 13% inhibition
N-(6,6-dimethyl-5-([(3R,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
0.001 mM, 24% inhibition
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
-
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-cyclohexa-1,3-dien-1-yl-N,N,N',N',N'-pentaphenyldecane-1,10-diaminium
-
-
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
-
N-[3-(pyridin-4-yl)-2,7-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
-
-
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide
-
-
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
-
-
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
-
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
-
-
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
N6-Dimethylaminopurine
-
-
NGRKI
-
-
NKMKSRLRKGALKKNV
-
autoregulatory pseudosubstrate sequence, residues 24-40
PAWHD
-
-
phenyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 48%
phorbol 12,13-dibutyrate
-
activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration, the inhibitory effect can be reversed by preincubation with ethoxyresorufin, 17-octadecynoic acid, wortmannin, LY294002, cytochlasin D, or latrunculin B
propan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
propidiumiodide
-
-
PYIALNVD
-
-
pyridin-4-ylmethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 53%
QEVIRNN
-
targets isozyme PKCbetaII, inhibits cardiomyocyte hypertrophy and activates potassium channels
QLMGGLHRHGAIINRKE
-
autoregulatory pseudosubstrate sequence, residues 391-407
RACK1 peptide I homologue
-
-
-
Ro 31-8220
-
i.e., 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)-maleimide
Ro-31-7549
-
specific inhibitor for isozyme PKCalpha
Ro-31-8220
-
strong inhibition of PKCalpha
Ro-31-8425
-
-
-
Ro-32-0432
-
strong inhibition
Ro-32-0432
-
conventional PKC inhibitor
Ro318220
-
-
rottlerin
-
selective inhibition of isozyme PKCdelta
rottlerin
-
inhibits PKCdelta, but does not block its translocation
rottlerin
-
slight inhibition of PKCalpha
rottlerin
-
specific for PKCdelta
rottlerin
-
inhibits PKCdelta
rottlerin
-
specific inhibitor of isozyme PKCdelta
rottlerin
-
a selective inhibitor of nPKCdelta and PKCtheta
rottlerin
-
PKC delta-specific inhibitor
rottlerin
-
PKC inhibitors induce LC3 processing and autophagosome formation. Inhibition of protein kinase C increased autophagy
safranine O
-
-
SFNSYELGSL
-
targets isozyme PKCdelta, protects from cardiac ischaemic injury, from cerebral injury, from graft coronary artery disease, and increases fibroblast proliferation
SIKIWD
-
targets isozyme PKCbeta
SIYRRGARRWRKLYRAN
-
targets isozyme PKCzeta, which leads to inhibition of fibroblast proliferation
SLNPEWNE
-
targets isozyme PKCbeta
SRIGQ
-
-
staurosporine
-
poorly selective for, unspecific inhibitor of a broad range of protein kinases
staurosporine
P36582
;
staurosporine
-
inhibits all PKC isozymes
staurosporine
-
strong inhibition
staurosporine
-
PKC inhibitory alkaloid isolated from the bacterium Lentzea albida, formerly Streptomyces staurosporeus
thapsigargin
-
complete inhibition of PKCgamma oscillation at 0.005 mM
thymeleatoxin
-
activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration
Tween 80
-
inhibits the enzyme at high concentration
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl][(benzylamino)oxy]methanone
-
0.03 mM, inhibition: 43%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl][(ethylamino)oxy]methanone
-
0.03 mM, inhibition: 50%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl]{[(2-methoxyethyl)amino]oxy}methanone
-
0.03 mM, inhibition: 55%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl]{[(pyridin-4-ylmethyl)amino]oxy}methanone
-
0.03 mM, inhibition: 3%
{3-[5-amino-4-(ethoxycarbonyl)thiophen-3-yl]phenyl}carbamate
-
0.03 mM, inhibition: 89%
MDPNGLSDPYVKL
-
targets isozyme PKCbeta, blocks Ca2+ current
additional information
-
the enzyme is inhibited by its regulatory subunit masking the active site, autoregulation by a pseudosubstrate mechanism, overview
-
additional information
-
synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential
-
additional information
-
synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential, sequences of the different enzyme forms, required sequence properties, overview
-
additional information
-
synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential
-
additional information
-
insensitive to caspase-3
-
additional information
-
insensitive to PKC inhibitors known to interfere either with the regulatory or the catalytic domain
-
additional information
-
no inhibition of PKCalpha by roscovitine, and purvalanol
-
additional information
-
PKC isozymes interacting proteins, overview
-
additional information
-
F-actin, latrunculin B, and phalloidin do not modulate the initial steps of enzyme activation process in living nerve cells
-
additional information
-
no inhibition of PKCdelta by bisindolylmaleimide I
-
additional information
-
rapamycin and wortmannin inhibit PKC betaII turnover
-
additional information
-
no inhibition of PKCgamma oscillation by EGTA, aristolochic acid, and colchicine
-
additional information
-
no inhibition by genistein and H-89
-
additional information
-
peptides derived from the PKC-cognate proteins are useful competitive inhibitors of PKC signalling, inhibitory peptide inhibit enzyme activity and/or enzyme translocation, physiological effects, overview
-
additional information
-
inhibition of PKC by dequalinium analogues of bis-quaternary dequalinium salts, structure-activity studies on head group variations, overview, Mulliken charges on N1 of the model compounds used for correlation, overview
-
additional information
-
isozyme PKCalpha is not inhibited by H-89 and rottlerin
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1,2-diacyl-sn-glycerol
-
-
1,2-dioctanoyl-sn-glycerol
-
-
1,2-diolein
Q1H8W8
activates, required
1,2-dioleoyl-sn-glycerol
-
activates
1-Oleoyl-2-acetyl-sn-glycerol
-
-
1-Oleoyl-2-acetyl-sn-glycerol
-
0.01 mM
1-oleoyl-acetyl-sn-glycerol
-
0.01 mM
1-stearoyl-2-arachidonyl-sn-glycerol
-
-
-
12-O-Tetradecanoylphorbol 13-acetate
-
activates
12-O-Tetradecanoylphorbol 13-acetate
-
activates PKCalpha isozyme about 1.6fold
12-O-Tetradecanoylphorbol 13-acetate
-
activates PKC
12-O-Tetradecanoylphorbol 13-acetate
-
activates isozyme PKCepsilon
12-O-Tetradecanoylphorbol 13-acetate
-
-
12-O-Tetradecanoylphorbol 13-acetate
-
activates PKC isozymes
12-O-Tetradecanoylphorbol 13-acetate
-
modeling of complex formation with PKCgamma, competes with hypericin for binding to the regulatory domain of PKC
12-O-tetradecanoylphorbol-13-acetate
-
-
12-O-tetradecanoylphorbol-13-acetate
-
-
13-O-acetylphorbol 12-myristate
-
-
4beta-phorbol 12-myristate 13-acetate
-
activates PKCalpha-mediated activation of phospholipase D
4beta-phorbol 12-myristate 13-acetate
-
-
acetyl-beta-methylcholine
-
-
adenosine
-
-
Anionic phospholipids
-
isozymes alpha, betaI, betaII, and gamma require anionic phospholipids for activity, isozymes delta, epsilon, eta, and theta do not
-
arachidonic acid
-
alone or a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity; slightly enhances PKC zeta activity
ATP
-
-
cardiolipin
-
activates
CSF-1
-
CSF-1 increases PKCgamma Thr 410 phosphorylation and kinase activity in 32D.R cells
-
curcumin
-
inhibits or activates PKC dependent on Ca2+ and the presence of membranes or phosphatidylserine, respectively, in presence of phosphatidylserine curcumin activates PKC, in presence of membranes with phosphatidylserine the enzyme is inhibited, Ca2+ competes with curcumin at the regulatory domainbinding site, overview, effects on different isozymes, overview
diacylglycerol
-
plus phosphatidylserine, activates
diacylglycerol
-
activates
diacylglycerol
-
activity is dependent on; activity is dependent on
diacylglycerol
-
independent of the presence of Ca2+ or diacylglycerol, when assayed with calf thymus H1 histone as a phosphate acceptor protein
diacylglycerol
-
dependent upon phosphatidylserine or diacylglycerol for maximal activation
diacylglycerol
-
isozymes alpha, betaI, betaII, and gamma require diacylglycerol for activity, isozymes delta, epsilon, eta, and theta do not
diacylglycerol
-
required, second messenger involved in PKC regulation
diacylglycerol
-
binds to the C1 domains of isozymes PKCalpha and PKCgamma, differential roles of C1A and C1B, overview
diacylglycerol
-
binds to C1 domain of PKC, regulatory function for isozymes alpha, betaI, betaII, gamma, delta, epsilon, eta, and theta, overview
diacylglycerol
Q1H8W8
activates
diacylglycerol
-
-
diacylglycerol
-
the membrane recruitment and activation of PKCdelta and PKCepsilon is fully dependent on their direct interaction with diacylglycerol generated by adenosine A2a receptor-induced activation of phospholipase C-gamma, through a mechanism requiring both Src and phosphatidylinositol 3-kinase activities
diacylglycerol
-
activates protein kinase C
diacylglycerol
-
-
diacylglycerol
-
-
Diacylglycerols
-
activate PKC isozymes
dioleoylglycerol
-
-
Epidermal growth factor
-
EGF, activates isozyme PKCalpha in the fetal lung during signaling involved in lung maturation, overview
fatty acids
-
activation mechanism
fatty acids
-
activation mechanism, isozyme PKCdelta is involved in fatty acid-induced hepatic insulin resistance
gamma-linolenic acid
-
a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity
gastrin
-
physiological activator of PKD2 in human AGS-B cells stably transfected with the CCK(B)/gastrin receptor
hydrogen peroxide
-
-
hypericin
-
competes with 12-O-tetradecanoylphorbol 13-acetate for binding to the regulatory domain of PKC, localization of PKC isozymes alpha, delta, and gamma, high affinty binding and interaction witht he C1B domain of PKC, molecular modeling
IGF-1
-
-
-
Insulin
-
activates PKC isozymes alpha, betaII, delta, and zeta in several cell types, activation mechanism
-
Insulin
-
activates PKC isozymes alpha, betaII, delta, and zeta in several cell types, activation mechanism, isozyme PKCdelta is involved in fatty acid-induced hepatic insulin resistance
-
ionomycin
-
-
Kainic acid
-
phosphorylation of MARCKS by PKC isozymes is dramatically upregulated specifically in microglial cells after kainic acid-induced seizures, but not in other types of glial cells, overview, upregulation of isozymes PKCalpha, PKCbetaI, PKCbetaII, and PKCdelta
kenpaullone
-
20% activation of PKCalpha at 0.01 mM
palmitate
-
activates isozyme PKCtheta, but not isozymes PKCalpha and PKCepsilon
phorbo-12-myristate-13-acetate
-
activation of protein kinase C significantly attenuates starvation- or rapamycin-induced LC3 processing. Activation of protein kinase C inhibits autophagy
-
phorbol 12,13-dibutyrate
-
activates PKC, activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration
phorbol 12,13-dibutyrate
-
-
phorbol 12,13-dibutyrate
-
0.001 mM
phorbol 12,13-dibutyrate
-
-
phorbol 12,13-dibutyrate
-
-
phorbol 12-myristate 13-acetate
-
activates PKC 4fold
phorbol 12-myristate 13-acetate
-
mediates isozyme translocation
phorbol 12-myristate 13-acetate
-
-
phorbol 12-myristate 13-acetate
-
binds to the C1 domains of isozymes PKCalpha and PKCgamma, differential roles of C1A and C1B, overview
phorbol 12-myristate 13-acetate
-
i.e. PMA
phorbol 12-myristate 13-acetate
-
i.e. PMA, inhibits IKCa channels
phorbol 12-myristate 13-acetate
-
stimulates IRS1 Ser24 phosphorylation in vivo
phorbol 12-myristate 13-acetate
-
-
phorbol 12-myristate 13-acetate
-
potent activator
phorbol 12-myristate 13-acetate
-
-
phorbol 12-myristate 13-acetate
-
100 nM
phorbol 12-myristate 13-acetate
B7SJR4
100 nM
phorbol 12-myristate 13-acetate
-
100 nM
phorbol 12-myristate 13-acetate
-
-
phorbol 12-myristate 13-acetate
-
10 nM
phorbol 12-myristate 13-acetate
-
activates PKC-mediated phosphorylation of transient receptor potential protein vanilloid 4 at Ser824
phorbol 12-myristate 13-acetate
-
-
phorbol dibutyrate
-
activates
phorbol ester
-
-
Phorbol esters
-
bind to and stimulate the kinase activity of PKC-L
Phorbol esters
Q00078
stimulate
phorbol myristate acetate
-
-
phorbol-ester-12-13-dibutyrate
-
-
phosphatidylserine
-
a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity; plus diacylglycerol, activates
phosphatidylserine
-
dependent upon phosphatidylserine or diacylglycerol for maximal activation
phosphatidylserine
-
PKC Apl I requires much less phosphatidylserine for activation than does purified PKC Apl II; PKC Apl I requires much less phosphatidylserine for activation than does purified PKC Apl II; stimulates
phosphatidylserine
-
PKC Apl I requires much less phosphatidylserine for activation than does purified PKC Apl II
phosphatidylserine
-
-
phosphatidylserine
Q1H8W8
activates, required
phosphatidylserine
-
-
phosphatidylserine
-
activation mechanism
phosphatidylserine-diolein
-
-
Phospholipid
-
strict dependence on the presence of phospholipids
Phospholipid
-
; activity is dependent on; activity is dependent on
Phospholipid
-
significantly dependent on phospholipid when assayed with calf thymus H1 histone as a phosphate acceptor protein
Phospholipid
Q99014
stimulates
Phospholipid
Q64617
dependent on
Phospholipids
-
regulatory function for isozymes alpha, betaI, betaII, gamma, delta, epsilon, eta, and theta
Phospholipids
Q1H8W8
activate
R59949
-
increases isofom PKCdelta and PKCepsilon activities in both membrane and cytosolic fractions
thymeleatoxin
-
activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration
thymeleatoxin
-
-
thymeleatoxin
-
activates Ca2+-dependent PKC isozymes, reversal by chronic thymeleatoxin pretreatment of the effects of carbachol on glucose-induced Ca2+ oscillations and pulsatile 5-HT release, overview
transforming growth factor alpha
-
TGFalpha, activates isozyme PKCalpha in the fetal lung during signaling involved in lung maturation, overview
-
zileuton
-
zileuton acts as a PKC delta activator, causing it to translocate from the cytosol to nucleus, the activation is inhibited by rottlerin
mezerein
-
stimulates classical, but not novel PKC isozymes
additional information
-
autoregulation by a pseudosubstrate mechanism, overview
-
additional information
-
cannot be activated by phorbol ester treatment of NIH 3T3 cells or insect cells, overexpressing the respective PKC isoenzyme
-
additional information
-
PKC isozymes interacting proteins, overview
-
additional information
-
F-actin, latrunculin B, and phalloidin do not modulate the initial steps of enzyme activation process in living nerve cells
-
additional information
-
the isozymes show varying activation requirements
-
additional information
-
phorbol 12-myristate 13-acetate and sugars activate PKC betaII activation and degradation via dephosphorylation and ubiquitinylation pathway
-
additional information
-
activation mechanism of isozymes PKCalpha and PKCgamma
-
additional information
-
PKC activation is influenced by intracellular Ca2+ concentration and activity of the metabotropic glutamate receptor 5
-
additional information
-
Helicobacter pylori activates the enzyme in gastric epithelial cells
-
additional information
-
activation mechanism of isozymes, overview
-
additional information
-
no activation by 4alpha-phorbol-12,13-didecanoate
-
additional information
-
no activation by 4alpha-phorbol 12-myristate 13-acetate
-
additional information
-
no activation by C2 ceramide or chronic insulin treatment
-
additional information
-
PKC isozymes are activated in gamma-ray-irradiated cells and bystander cells; PKC isozymes are activated in gamma-ray-irradiated cells and bystander cells; PKC isozymes are activated in gamma-ray-irradiated cells and bystander cells
-
additional information
-
the activation of PKCalpha isoform leads to increased N1 secretion via the phosphorylation and activation of ADAM17, a process that likely accounts for M1/M3 muscarinic receptors-mediated control of N1 production (the cellular prion protein is physiologically cleaved in the middle of its 106-126 putative toxic core, at the 111/112 peptidyl bond, thus generating an amino-terminal fragment referred to as N1); the activation of PKCdelta isoform leads to increased N1 secretion via the phosphorylation and activation of ADAM17, a process that likely accounts for M1/M3 muscarinic receptors-mediated control of N1 production (the cellular prion protein is physiologically cleaved in the middle of its 106-126 putative toxic core, at the 111/112 peptidyl bond, thus generating an amino-terminal fragment referred to as N1); the activation of PKCepsilon isoform leads to increased N1 secretion via the phosphorylation and activation of ADAM17, a process that likely accounts for M1/M3 muscarinic receptors-mediated control of N1 production (the cellular prion protein is physiologically cleaved in the middle of its 106-126 putative toxic core, at the 111/112 peptidyl bond, thus generating an amino-terminal fragment referred to as N1)
-
additional information
-
not activated by 4alpha-phorbol
-
additional information
-
after binding to alpha2beta1 integrin, human echovirus 1 activates PKCalpha, independent on the E336-mediated conformational changes in alpha2beta1
-
additional information
-
PKC activation can inhibit zinc transporter ZIP8 activity
-
additional information
-
PKC is activated by the addition of 0.03 mg/ml 10:0 1,2-didecanoyl-sn-glycero-3-phosphate, 0.01 mg/ml 1-oleoyl-2-acetoyl-sn-glycerol, and 0.6 mM CaCl2 (no CaCl2 for isoform PKC-delta) for 30 min at 37C
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0093
ATP
-
pH 7.4, 37C, recombinant wild-type isozyme PKCalpha
0.0828
ATP
-
pH 7.4, 37C, recombinant isozyme PKCalpha mutant M417A
0.0166
FKKQGSFAKKK
-
isozyme PKCeta, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0174
FKKQGSFAKKK
-
isozyme PKCalpha, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0205
FKKQGSFAKKK
-
isozyme PKCzeta, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0229
FKKQGSFAKKK
-
isozyme PKCepsilon, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0258
FKKQGSFAKKK
-
isozyme PKCiota/lambda, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.034
FKKQGSFAKKK
-
isozyme PKCtheta, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0347
FKKQGSFAKKK
-
isozyme PKCgamma, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0356
FKKQGSFAKKK
-
isozyme PKCbetaI, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0422
FKKQGSFAKKK
-
isozyme PKCdelta, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
0.0124
N6-phenyl-ATP
-
pH 7.4, 37C, recombinant isozyme PKCalpha mutant M417A
0.0036
S6-(229-239) peptide
-
enzyme activated by cardiolipin
-
0.0599
FKKQGSFAKKK
-
isozyme PKCbetaII, in 20 mM Tris-HCl, pH 7.5, 10 mM MgCl2, and 0.1 mM CaCl2, at 25C
additional information
additional information
-
binding kinetics of phorbol 12-myristate 13-acetate and diacylglycerol
-
additional information
additional information
-
kinetics
-
additional information
additional information
-
binding kinetics of PKC isozymes to hypericin and phorbol esters, overview
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000338
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
-
0.000541
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide
-
pH and temperature not specified in the publication
0.000189
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
pH and temperature not specified in the publication
0.000109
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000046
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.01
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000125
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000092
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000029
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000541
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
pH and temperature not specified in the publication
0.000062
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000131
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide
-
pH and temperature not specified in the publication
additional information
additional information
-
Ki values of the pseudosubstrates in nano- to micromolar range
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000002
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000005
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000008
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000055
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000378
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000829
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.03
1,1'-(1,10-decanediyl)bis[1-amino isoquinolinium] diiodide
-
pH 7.4
0.014
1,1'-(1,10-decanediyl)bis[2-amino-1-methylbenzimidazolium] diiodide
-
pH 7.4
0.017
1,1'-(1,10-decanediyl)bis[2-methylbenzothiazolium] diiodide
-
pH 7.4
0.036
1,1'-(1,10-decanediyl)bis[2-methylbenzoxazolium] diiodide
-
pH 7.4
0.022
1,1'-(1,10-decanediyl)bis[2-methylquinolinium] diiodide
-
pH 7.4
0.007
1,1'-(1,10-decanediyl)bis[4-amino-2-methyl quinolinium] diiodide
-
pH 7.4
0.03
1,1'-(1,10-decanediyl)bis[4-aminoquinolinium] diiodide
-
pH 7.4
0.029
1,1'-(1,10-decanediyl)bis[4-N,N,dimethylaminoquinolinium] diiodide
-
pH 7.4
0.072
1,1'-(1,10-decanediyl)bis[quinolinium] diiodide
-
pH 7.4
0.112
1,1'-decane-1,10-diylbis(4-aminopyridinium) diiodide
-
pH 7.4
0.231
1,1'-decane-1,10-diylbis[4-(dimethylamino)pyridinium]
-
pH 7.4
0.03
1,6-bis[N-(1-methylquinolinium-2-methyl)amino]-hexane diiodide
-
pH 7.4
0.000004
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000007
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000063
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000077
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000433
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000661
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000006
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000008
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000031
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000109
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.000823
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
pH and temperature not specified in the publication
0.001
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
value higher than, pH and temperature not specified in the publication
0.000008
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000013
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000132
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000214
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000771
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000865
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
pH and temperature not specified in the publication
0.000081
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
pH and temperature not specified in the publication
0.000188
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
pH and temperature not specified in the publication
0.000635
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
pH and temperature not specified in the publication
0.000743
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
pH and temperature not specified in the publication
0.001
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
value higher than, pH and temperature not specified in the publication
0.000082
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
pH and temperature not specified in the publication
0.00012
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
pH and temperature not specified in the publication
0.000703
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
pH and temperature not specified in the publication
0.000948
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
pH and temperature not specified in the publication
0.001
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
value higher than, pH and temperature not specified in the publication
0.000052
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000133
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000386
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000738
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.001
2-methyl-N1-[3-(pyridin-3-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000009
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000018
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000044
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000141
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000942
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000967
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.005
3-methoxybenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.000403
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000452
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000818
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.000932
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
pH and temperature not specified in the publication; value higher than, pH and temperature not specified in the publication
3.59
4-amino-1,2-dimethylquinolinium
-
pH 7.4
0.117
4-amino-1-decyl-2-methylquinolinium iodide
-
pH 7.4
0.000735
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
-
pH and temperature not specified in the publication
0.000802
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
-
pH and temperature not specified in the publication
0.001
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
-
pH and temperature not specified in the publication; value higher than, pH and temperature not specified in the publication
0.006
benzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.0075
bisindolylmaleimide I
-
pH not specified in the publication, 30C
0.002
ethyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.004
ethyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.001
ethyl 2-amino-4-(4-aminophenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.002
ethyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.0025
G 6983
-
pH not specified in the publication, 30C
0.0000023 - 0.0000079
G-6976
-
IC50 of 2.3-7.9 nM
0.25
N,N,N,N',N',N'-hexaethyldecane-1,10-diaminium
-
pH 7.4
0.094
N-cyclohexa-1,3-dien-1-yl-N,N,N',N',N'-pentaphenyldecane-1,10-diaminium
-
pH 7.4
0.000079
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000093
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000254
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000997
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000024
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000034
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.00035
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000371
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000027
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000038
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000102
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication; value higher than, pH and temperature not specified in the publication
0.000005
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.00002
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000077
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000859
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.0009
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.00001
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.000013
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.000053
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.000097
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.000676
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.000779
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
pH and temperature not specified in the publication
0.001
N-[3-(pyridin-4-yl)-2,7-naphthyridin-1-yl]ethane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000743
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000877
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication; value higher than, pH and temperature not specified in the publication
0.000401
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000929
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication; value higher than, pH and temperature not specified in the publication
0.000044
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000054
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000157
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.000355
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000862
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000961
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.001
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.00006
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000147
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000294
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000378
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000496
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000015
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000047
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000093
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000221
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.000018
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000062
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.000124
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.00014
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
pH and temperature not specified in the publication
0.001
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
value higher than, pH and temperature not specified in the publication
0.006
propan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
pH and temperature not specified in the publication
0.016
propidiumiodide
-
pH 7.4
0.000008
Ro-31-8425
-
pH 7.3, 25C
-
0.048
safranine O
-
pH 7.4
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7
-
assay at
7.2
-
assay at
7.3
-
assay at
7.4
-
assay at
7.4
-
assay at
7.4
-
assay at
7.4
-
assay at
7.5
Q1H8W8
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
20
-
assay at
21
-
assay at room temperature
22
-
assay at room temperature
22
-
assay at room temperature
24
-
assay at
25
-
assay at
25
-
assay at
30
Q1H8W8
assay at
30
-
assay at
30
-
assay at
30
-
assay at
36
-
assay at
37
-
assay at
37
-
assay at
37
-
assay at, in vivo
37
-
assay at
37
-
assay at
37
-
assay at
pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6.7
B7SJR4
deduced from amino acid sequence
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
primary, cortical
Manually annotated by BRENDA team
-
PKC isozyme expression patterns
Manually annotated by BRENDA team
-
isozyme PKCdelta
Manually annotated by BRENDA team
-
arterial pulmonary
Manually annotated by BRENDA team
-
in adult brain, the relative activities of alpha-, beta I-, beta II-, and gamma-subspecies are roughly 16%, 8%, 55%, and 21%
Manually annotated by BRENDA team
-
isozyme-specific and developmental stage-specific alterations in brain PKC following exposure to a polychlorinated biphenyl mixture
Manually annotated by BRENDA team
-
shows higher levels of PKCalpha than normal breast tissue
Manually annotated by BRENDA team
-
high expression of isozyme PKCalpha in most cell lines, overview
Manually annotated by BRENDA team
-
isozyme gamma
Manually annotated by BRENDA team
-
expression of several isozymes
Manually annotated by BRENDA team
-
PR-17 cells and wild-type HL-60 cells
Manually annotated by BRENDA team
-
fibrosarcoma cell line
Manually annotated by BRENDA team
-
epidermoid carcinoma line A431
Manually annotated by BRENDA team
-
insulin-secreting cell line RINm5F
Manually annotated by BRENDA team
-
Swiss 3T3 fibroblasts
Manually annotated by BRENDA team
-
undifferentiated mouse embryonal carcinoma cell line P19, NIH 3T3 cells
Manually annotated by BRENDA team
Q02956
several hemopoietic tumor lines
Manually annotated by BRENDA team
-
NIH/hIR/rIRS1cells
Manually annotated by BRENDA team
Mus musculus C57BL/6
-
-
-
Manually annotated by BRENDA team
-
isozyme PKCgamma
Manually annotated by BRENDA team
-
ontogenetic isozyme profiling
Manually annotated by BRENDA team
-
isozymes alpha, betaI, betaII, gamma, delta, epsilon, lambda, eta, theta, and zeta
Manually annotated by BRENDA team
-
purified PKC from brain
Manually annotated by BRENDA team
-
recombinant isozymes
Manually annotated by BRENDA team
-
from normal sigmoid colon
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
isozymes gamma, and epsilon
Manually annotated by BRENDA team
-
from coronary artery
Manually annotated by BRENDA team
-
primary from fetal lung
Manually annotated by BRENDA team
-
follicular lymphoma cell line
Manually annotated by BRENDA team
-
follicular lymphoma cell line
Manually annotated by BRENDA team
Mus musculus C57BL/6
-
-
-
Manually annotated by BRENDA team
-
primary cerebellar, cultured
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
myeloma cell line
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
precursor T-lymphoblastic leukemia cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
hematopoietic stemcell and hemopoietic progenitor cells
Manually annotated by BRENDA team
-
enzyme is predominantly expressed in
Manually annotated by BRENDA team
-
shows higher levels of PKCalpha than normal liver tissue
Manually annotated by BRENDA team
-
from fetal liver
Manually annotated by BRENDA team
-
constitutively active isozyme PKCdelta
Manually annotated by BRENDA team
-
ontogenetic isozyme profiling
Manually annotated by BRENDA team
-
cellular distribution and phosphorylation of MARCKS by PKC isozymes in the hippocampus following kainic acid-induced seizures, immunohistochemic detection, overview
Manually annotated by BRENDA team
Mus musculus C57BL/6
-
cellular distribution and phosphorylation of MARCKS by PKC isozymes in the hippocampus following kainic acid-induced seizures, immunohistochemic detection, overview
-
Manually annotated by BRENDA team
-
myenteric neurons, isozymes gamma, lambda, and epsilon
Manually annotated by BRENDA team
-
isozyme PKCalpha
Manually annotated by BRENDA team
O19111
cortex, low expression in vascular elements and high expression in tubule epithelium, highly expressed in proximal tubule, thick limb, and collecting duct
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
P34885
abundant at the earliest larval stage, but their relative concentrations decrease coordinately in late larvae
Manually annotated by BRENDA team
-
fetal, isozymes PKCalpha, PKCepsilon, PKCmy, and PKCzeta, isozyme PKCalpha is localized in the cuboidal epithelium and in mesenchyme
Manually annotated by BRENDA team
-
ABPL-3 myeloid tumor
Manually annotated by BRENDA team
-
derived from bone marrow
Manually annotated by BRENDA team
Mus musculus C57BL/6
-
-
-
Manually annotated by BRENDA team
-
myeloid progenitor cell line 32D.R
Manually annotated by BRENDA team
-
myenteric neuron, isozyme beta in submucosal ganglia of neurons, isozymes gamma, eta, and theta are present in intrinsic primary afferent neurons, but not in other myenteric neurons, low expression of isozyme alpha, isozyme epsilon
Manually annotated by BRENDA team
-
acutely dissociated CA1 neurons in non-excitotoxic ischemia
Manually annotated by BRENDA team
-
a hybridomal cell line of a rat neuroblastoma and a mouse glioma, expression of isozymes PKCalpha, PKCepsilon, PKCjota, and PKCzeta, no expression of isozymes PKCbeta, PKCdelta, PKCgamma, PKCmy, and PKCtheta
Manually annotated by BRENDA team
-
highly expressed
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
virus-induced macrophage cell line
Manually annotated by BRENDA team
-
cultured type-2 astrocyte cell line
Manually annotated by BRENDA team
-
the PKCalpha is expressed prominently in the retinal growth cones, while abundant in the filopodial and lamellipodial processes, the PKCbeta1 isozymes is expressed prominently in the retinal growth cones, whilst the beta2 isozyme is barely detected, the beta1 isozyme is restricted largely in the core region of the growth cones, the PKCdelta isozyme is barely detected in the retinal growth cones, the PKCepsilon isozyme is expressed prominently in the retinal growth cones and is abundant in the filopodial and lamellipodial processes, the PKCgamma isozyme is barely detected in the retinal growth cones
Manually annotated by BRENDA team
-
bipolar cells of the retina
Manually annotated by BRENDA team
-
isozyme PKCtheta is decreased in obese patients' skeletal muscle
Manually annotated by BRENDA team
-
myenteric neurons
Manually annotated by BRENDA team
-
no isozyme beta, high expression of isozyme delta
Manually annotated by BRENDA team
-
pulmonary arterial
Manually annotated by BRENDA team
-
isozyme PKCalpha
Manually annotated by BRENDA team
-
peripheral blood CD8+ T cell
Manually annotated by BRENDA team
-
highly expressed
Manually annotated by BRENDA team
-
increased expresison of isozyme PKCtheta in insulin-resistant rats
Manually annotated by BRENDA team
-
fibroblast cell line
Manually annotated by BRENDA team
additional information
-
expression analysis of isozymes alpha, betaII, gamma, and delta in reactive lymphoid tissues, B-cell lymphoma and lymphoma cell lines, overview
Manually annotated by BRENDA team
additional information
-
PKC isozymes are expressed in a wide range of tissues, some isozymes are tissue-specific
Manually annotated by BRENDA team
additional information
-
tissue- and cell-type-specific expression of isozymes, overview, involved in regulation of organ, e.g. intestinal, function
Manually annotated by BRENDA team
additional information
-
developmental expression patterns of isozymes PKCalpha, PKCepsilon, PKCmy, and PKCzeta
Manually annotated by BRENDA team
additional information
-
tissue distribution of PKC isozymes, overview
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
isozyme PKCdelta
Manually annotated by BRENDA team
-
isozymes beta, gamma, delta, epsilon
Manually annotated by BRENDA team
-
non-activated PKCbetaII and PKCbetaI
Manually annotated by BRENDA team
-
translocation form cytoplasm to plasma membrane after addition of phorbol 12-myristate 13-acetate or 1,2-dioctanoyl-sn-glycerol
Manually annotated by BRENDA team
-
stimulation by phorbol ester causes weak translocation of deltaIII-GFP from the cytosol to the plasma membrane
Manually annotated by BRENDA team
-
isozyme epsilon, gamma, and alpha
Manually annotated by BRENDA team
-
translocation of PKCgamma from cytosol to membrane
Manually annotated by BRENDA team
Q1H8W8
PKC is commonly associated with a rapid redistribution of the kinase from the cytosol to membranes
Manually annotated by BRENDA team
B7SJR4
inactive enzyme
Manually annotated by BRENDA team
-
activated PKCbetaII and PKCbetaI are translocated from cytosol, juxtanuclear location, isozyme-specific translocation of PKCbetaII and not PKCbetaI to a juxtanuclear subset of recycling endosomes, involvement of phospholipase D
Manually annotated by BRENDA team
-
isozyme PKCepsilon in a perinuclear site is associated with the Golgi apparatus, phosphorylation of isozyme PKCepsilon at Ser279 is required for translocation to the nucleus during which the enzyme looses the phsophate group at Ser279, overview
Manually annotated by BRENDA team
Q1H8W8
intracellular localization pattern during cyst formation
Manually annotated by BRENDA team
-
localization of PKC isozymes alpha, delta, and gamma, is influenced by hypericin, high affinity binding and interaction with the C1B domain of PKC, molecular modeling
Manually annotated by BRENDA team
P34885
associated with
Manually annotated by BRENDA team
-
bound to via second messengers and phorbol esters, the ligand-binding domains are required for membrane targeting
Manually annotated by BRENDA team
-
cellular membrane translocation mechanism of isozyme PKCalpha and PKCgamma
Manually annotated by BRENDA team
-
isozyme epsilon, gamma, and alpha
Manually annotated by BRENDA team
-
jejunal brush border membrane
Manually annotated by BRENDA team
-
translocation
Manually annotated by BRENDA team
Q1H8W8
PKC is commonly associated with a rapid redistribution of the kinase from the cytosol to membranes
Manually annotated by BRENDA team
-
isozymes PKC-beta and PKC-gamma are recruited to microtubules by LFA-1 signalling, i.e. lymphocyte-function-associated antigen-1 signalling
Manually annotated by BRENDA team
-
isozyme PKCepsilon in a perinuclear site is associated with the Golgi apparatus, phosphorylation of isozyme PKCepsilon at Ser279 is required for translocation to the nucleus during which the enzyme looses the phsophate group at Ser279, overview
-
Manually annotated by BRENDA team
-
stimulation by phorbol ester causes weak translocation of deltaIII-GFP from the cytosol to the plasma membrane
Manually annotated by BRENDA team
-
activated PKCbetaII and PKCbetaI are translocated from cytosol
Manually annotated by BRENDA team
-
PKC is recruited by other kinases
Manually annotated by BRENDA team
-
translocation of PKCgamma from cytosol to membrane, PKCgamma oscillates on the membrane induced by glutamate and activated metabotropic glutamate receptor 5, overview
Manually annotated by BRENDA team
-
using a PKC-GFP fusion protein it is shown that NPKC localizes to growing tips and sub-apical plasma membrane in actively growing hyphae
Manually annotated by BRENDA team
additional information
-
isozyme PKCtheta is recruited to the plasma membrane by a cytoskeleton-dependent mechanism regulating the Rac-1 guanine nucelotide exchange protein Vav-1
-
Manually annotated by BRENDA team
additional information
-
no isozyme delta in the nucleus
-
Manually annotated by BRENDA team
additional information
-
phorbol 12-myristate 13-acetate-mediated translocation of isozymes alpha, betaI, betaII, and gamma
-
Manually annotated by BRENDA team
additional information
-
PKC is translocated from cytoplasm to membrane upon stimulation, latrunculin B does not influence enzyme localization
-
Manually annotated by BRENDA team
additional information
-
PKCdelta is translocated from cytosol to plasma membrane in platelets activated by the snake venom alboaggregin-A
-
Manually annotated by BRENDA team
additional information
-
subcellular distribution of isozymes in brain regions during development
-
Manually annotated by BRENDA team
additional information
-
subcellular distribution of isozymes PKCbetaII and PKCbetaI
-
Manually annotated by BRENDA team
additional information
-
analysis of subcellular distribution of isozymes in rat cerebellum, overview
-
Manually annotated by BRENDA team
additional information
-
cell passage induces rapid translocation of isozyme PKCepsilon to the periphery where it appears to colocalize with F-actin, which renders the cells proliferative again while PKCepsilon return to the perinuclear site
-
Manually annotated by BRENDA team
additional information
-
quantitative determination of membrane translocation of isozymes under hypoxic conditions in neuroblastoma SH-SY5Y cells, overview
-
Manually annotated by BRENDA team
additional information
-
subcellular distribution of isozymes PKCalpha, PKCepsilon, PKCmy, and PKCzeta
-
Manually annotated by BRENDA team
additional information
Q1H8W8
subcellular localization study, during encystment PKCbeta redistributs to plasma membrane from cytosol
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7000
-
SDS-PAGE, PKCthetaC1B subdomain
724241
76000
B7SJR4
deduced from amino acid sequence
692618
78000
-
SDS-PAGE
724707
100000
-
SDS-PAGE, full-length PKCtheta
724241
additional information
-
the molecular weight of the Xenopus PKC isozyme proteins varies from 75 to 90 kDa
691557
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 78000, SDS-PAGE
?
-
x * 120000, SDS-PAGE
?
-
x * 105000, SDS-PAGE
?
-
x * 64000, SDS-PAGE
?
-
x * 65000
?
-
x * 116000
?
-
x * 103925, calculation from nucleotide sequence
?
Q99014
x * 126000
?
-
x * 78000-80000, PKC betaII, SDS-PAGE
?
-
x * 82000, isozyme PKCalpha, SDS-PAGE
additional information
-
PKC domain composition
additional information
-
PKC domain structure, overview
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phosphoprotein
-
phosphorylation regulates the enzyme activity, the enzyme is phosphorylated by PDK-1 at the activation loop
phosphoprotein
-
phosphorylation of Thr642 is an early event in the processing of newly synthesized protein kinase C beta 1 and is essential for its activation
phosphoprotein
-
activation loop phosphorylation of PKCdelta in response to serum stimulation of cells is PI 3-kinase-dependent and is enhanced by PDK1 coexpression
phosphoprotein
-
COOH-terminal autophosphorylation sites are critical for enzyme function and possibly subcellular localization in COS cells
phosphoprotein
-
processing by protein kinase C cannot occur until the enzyme is first phosphorylated by a protein kinase C kinase
phosphoprotein
-
protein kinase C is processed by three phosphorylations. Firstly, trans-phosphorylation on the activation loop T500 renders it catalytically competent to autophosphorylate. Secondly, a subsequent autophosphorylation on the carboxyl terminus T641 maintains catalytic competence. Thirdly, a second autophosphorylation on the carboxyl terminus S660 regulates the enzyme's subcellular localization
phosphoprotein
-
phosphorylation of PKCny leads to its activation in response to B-cell receptor engagement in subcellular compartment redistribution
phosphoprotein
-
phosphorylation of isozyme PKCepsilon at Ser279 is required for translocation to the nucleus during which the enzyme looses the phsophate group at Ser279, overview
phosphoprotein
-
isozymes alpha, delta, and epsilon require trans- and autophosphorylation for activity
phosphoprotein
-
phorbol 12,13-dibutyrate in the presence of dioleoylphosphatidylserine stimulates the autophosphorylation of PKD2 in a synergistic fashion. Phorbol esters also stimulate autophosphorylation of PKD2 in intact cells, C-terminal Ser876 is an in vivo phosphorylation site within PKD2 that is correlated with the activation status of the kinase
additional information
-
two types of complementary DNA clones for rat brain protein kinase C, these clones encode 671 and 673 amino acid sequences, which differ from each other only in the carboxyl-terminal regions of approximately 50 amino acid residues. This difference seems to result from alternative splicing
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
purified recombinant isozyme PKCbetaII catalytic domain, residues 321-673, hanging drop vapour diffusion method, 8 mg/ml protein in 0.1 M acetamidoiminodiacetic acid, pH 6.5, and 1.7-2.3 M sodium acetate, 19C, X-ray diffraction structure determination and analysis at 3.2 A resolution, molecular replacement, modeling
-
crystal structure of PKCioata is determined at 2.4 A. The structure of the PKCiota/Par-3 peptide complex reveals that the kinase domain adopts an active conformation even though Thr402 in the activation loop is not phosphorylated. The Par-3 peptide binds to the groove between the N- and C-lobes of the kinase via combined hydrophobic and charge-charge interactions
-
crystal structure of PKCthetaC1B is determined to 1.63 A resolution. It is shown that, Trp253 at the rim of the activator-binding pocket is orientated towards the membrane
-
crystal structure of the cys2 activator-binding domain of protein kinase C delta in complex with phorbol ester
-
crystal structure of full-length protein kinase C bII is determined at 4.0 A. The C1B domain clamps the NFD helix in a low activity conformation, which is reversed upon membrane binding. A low-resolution solution structure of the closed conformation of PKCbII is derived from small-angle X-ray scattering
-
crystal structure of PKC-delta C2 domain. Structural elements unique to this C2 domain include a helix and a protruding beta hairpin which may contribute basic sequences to a membrane-interaction site
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
native PKCbeta is very sensitive to protease degradation
Q1H8W8
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
native isozyme partially by anion exchange chromatography and gel filtration
Q1H8W8
partial; partial purification of the PKC-zeta isoenzyme
-
recombinant full-length enzyme by nickel affinity chromatography, proteolytic clevage of the recombinant full-length enzyme to obtain the catalytic domain, followed by anion exchange chromatography and gel filtration
-
using affinity purification through glutathione-Sepharose 4B columns, subsequent cleavage of the GST tag, ammonium sulfate precipitation and gel filtration chromatography
-
using Ni-NTA chromatography
-
anion-exchange chromatography and gel filtration
-
isozyme PKC betaII from jejunal loops
-
isozymes partially from primary cerebellar granule cells, Tris buffer leads to degradation of the proteins
-
partial; partial
-
protein A Sepharose column chromatography
-
recombinant full-length isozymes PKCalpha and PKCgamma from Sf9 cells by ion exchange chromatography, recombinant His-tagged isolated isozymes PKCalpha and PKCgamma domains C1 from Escherichia coli strain BL21(DE3) inclusion bodies by nickel affinity chromatography
-
partial
Q99014
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Sf9 cells using a baculovirus expression system
B7SJR4
structure and nucleotide sequence of a Drosophila melanogaster protein kinase C gene
P05130
gene pkcb, isozyme PKCbeta, DNA and amino acid sequence determination and analysis, expression of the catalytic domain from PKCbeta
Q1H8W8
co-expression of PKC isozymes and insulin in HEK-293 or CHO cells, interaction analysis, overview
-
expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells
-
expressed in HeLa cells
-
expression in COS cells
-
expression in COS1 cells; expression in COS1 cells
-
expression in COS7 cells
-
expression in recombinant baculovirus-infected insect cells; expression in recombinant baculovirus-infected insect cells, overexpression in NIH 3T3 cells or insect cells
-
expression in the baculovirus insect-cell expression system
-
expression of FLAG-tagged wild-type and mutant isozyme PLCalpha in MCF-10A human breast epithelial cells
-
expression of full-length His-tagged isoform PKCbetaII in Spodoptera frugiperda Sf21 cells
-
expression of GFP-tagged PKC
-
expression of GFP-tagged wild-type PKC isozymes in HEK-293 cells, and of GFP-tagged PKCgamma wild-type and mutants lacking the C1 or C2 domain in HEK-293 cells
-
expression of wild-type and mutant isoyzem PKCalpha in COS-7 cells, co-expression of PKCalpha with diacylglycerol kinase-zeta and retinoblastoma protein in COS-7 cells
-
isolation of cDNA
-
isozymes PKCbetaII and PKCbetaI are products of alternative splicing of gene PKCbeta, expression of GFP- or HA-tagged isozymes PKCbetaII, wild-type and mutant, and PKCbetaI in HEK-293 or HeLa cells
-
protein kinase C-epsilon E1 and E2, expression in Sf9 cells, the recombinant protein displays protein kinase C activity and phorbol ester binding activity
-
the 5' segment of the gene for protein kinase C beta is cloned from a human leukocyte genomic library in EMBL3 bacteriophage
-
cDNA sequence encoding mouse PKC-gamma isolated from a C57BL/6 brain cDNA library
-
co-expression of PKC isozymes and insulin in HEK-293 or CHO cells, interaction analysis, overview
-
COS cells transfected with the PKC lambda expression plasmid
-
expressed in Escherichia coli as a GST-fusion protein
-
expressed in insect cells via a baculovirus expression vector, a 75000 Da protein is synthesized which, unlike other PKC isoforms, does not bind phorbol ester, even at very high concentrations
Q02956
expressed in Sf9 cells as a His-tagged fusion protein using the baculovirus system
-
expression in COS cells; expression in COS cells
-
expression of GFP-tagged PKC
-
expression of isozymes PKCepsilon and PKCzeta in Saccharomyces cerevisiae, subcloning in Escherichia coli
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expression of mutant enzymes in COS cells
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expression of wild-type and mutant isozyme PKCepsilon in NIH3T3 fibroblasts as GFP-tagged proteins
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isolation of cDNA clones encoding protein kinase C
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isolation of cloned mouse protein kinase C beta-II cDNA
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overexpression PKCdelta in NMuMG cells, a normal immortalized mammary cell line derived from NAMRU mice
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PKCdeltaII expressed in COS-1 cells
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wild-type and mutant enzymes overexpressed in COS cells
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expressed as a PKC-GFP fusion protein in Neurospora conidiospores
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cDNA cloning of an alternative splicing variant of protein kinase C delta, expression of truncated form of PKC deltaIII fused to green fluorescent protein in CHO-K1 cells
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co-expression of PKC isozymes and insulin in HEK-293 or CHO cells, interaction analysis, overview
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expressed in COS 7 cells
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expressed in COS-7 cells
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expressed in Escherichia coli
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expressed in HEK-293 cells
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expressed in Sf9 cells as a GST-fusion protein
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expression in COS cells
Q64617
expression of full-length isozymes PKCalpha and PKCgamma in Spodoptera frugiperda Sf9 cells using the baculovirus infection system, expression of His-tagged isolated isozymes PKCalpha and PKCgamma domains C1 in Escherichia coli strain BL21(DE3)
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expression of isozyme PKCbetaI in HEK-293 cells, and co-expression with dopamine transporter significantly enhancing the amphetamine-stimulated dopamine efflux
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expression of isozyme PKCdelta in Saccharomyces cerevisiae, subcloning in Escherichia coli
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
prolonged PKC activation by phorbol esters is downregulates PKC for at least 24 h
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knockdown of diacylglycerol kinase delta enhances PKCalpha activity
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mitochondrial reactive oxygen species production activates PKCepsilon
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
K368D
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site-directed mutagenesis of isozyme PKCalpha ATP-binding site, a dominant-negative mutant
K371R
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site-directed mutagenesis, inactive isozyme PKCbetaII mutant
K368A
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a dominant-negative mutant of PKCalpha
Q258G
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mutated activator-binding site: mutation reduces affinity for both phorbol ester and diacylglycerol. Mutation causes significantly reduced membrane translocation by phorbol ester treatment
S279A
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site-directed mutagenesis of the isozyme PKCepsilon phosphorylation site results in altered subcellular localization not in the perinulcear/Golgi site
S279E
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site-directed mutagenesis of the isozyme PKCepsilon phosphorylation site results in altered subcellular localization not in the perinulcear/Golgi site
S279T
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site-directed mutagenesis of the isozyme PKCepsilon phosphorylation site results in altered subcellular localization not in the perinulcear/Golgi site
T243A
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mutated activator-binding site: mutation reduces affinity for both phorbol ester and diacylglycerol. Mutation causes significantly reduced membrane translocation by phorbol ester treatment
T500E
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expression as a catalytically active protein kinase C in COS cells
T500V
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expression as a catalytically inactive protein kinase C in COS cells
W253G
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mutated activator-binding site: mutation reduces affinity for both phorbol ester and diacylglycerol. Mutation causes significantly reduced membrane translocation by phorbol ester treatment
Y239A
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mutated activator-binding site: mutation reduces affinity for both phorbol ester and diacylglycerol. Mutation causes significantly reduced membrane translocation by phorbol ester treatment
D116A
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site-directed mutagenesis, isozyme PKCgamma domain C1B mutant shows unaltered activity
D55A
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site-directed mutagenesis, isozyme PKCalpha and PKCgamma mutants show unaltered activity and ligand binding, isozyme PKCalpha shows enhanced activation by phospholipids
DELTA621-622
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deletion of two residues in the AGC linker that passes through the cleft of the C1B domain (DELTA621622) results in a 2fold decrease in the concentration of phorbol 12-myristate 13-acetate required to mediate half-maximal translocation
F629D
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within the NFD helix, mutant F629D and mutant F633D lead to 2- to 5fold decrease in EC50 for phorbol 12-myristate 13-acetate induced translocation
F633D
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within the NFD helix, mutant F629D and mutant F633D lead to 2- to 5fold decrease in EC50 for phorbol 12-myristate 13-acetate induced translocation
K368A
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a dominant-negative mutant of PKCalpha
L125D
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mutation of Leu125 in the C1B domain, which is part of the C1B clamp interface, increases EC50 for phorbol 12-myristate 13-acetate induced translocation more than 10fold
L358D
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mutation of residues in the hydrophobic interface between the kinase N lobe and the C1B domain (L358D, L367D, Y422D, Y430D) results in 5- to 14fold decrease in the EC50 for phorbol 12-myristate 13-acetate induced translocation
W58A
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site-directed mutagenesis, isozyme PKCgamma domain C1A mutant shows impaired binding of phorbol 12-myristate 13-acetate and diacylglycerol
Y123A
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site-directed mutagenesis, isozyme PKCgamma domain C1B mutant shows impaired binding of phorbol 12-myristate 13-acetate and diacylglycerol
Y123W
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the mutation in the C1 domain of PKC leads to measurable changes upon membrane binding
Y422D
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mutation of residues in the hydrophobic interface between the kinase N lobe and the C1B domain (L358D, L367D, Y422D, Y430D) results in 5- to 14fold decrease in the EC50 for phorbol 12-myristate 13-acetate induced translocation
Y430D
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mutation of residues in the hydrophobic interface between the kinase N lobe and the C1B domain (L358D, L367D, Y422D, Y430D) results in 5- to 14fold decrease in the EC50 for phorbol 12-myristate 13-acetate induced translocation
M417A
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site-directed mutagenesis, utilizes the alternate cofactor N6-phenyl-ATP
additional information
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downregulation of PKCdelta by short interfering RNA, deletion of domain C2 of PKCgamma leads to complete loss of activity, while deletion of C1 domain shows no effect on PKCgamma activity
additional information
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siRNA knockdown of isozyme PKC-delta in Caco-2 cells leads to increased cell proliferation and apoptosis
additional information
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using a kinase dead mutant it is shown that the kinase activity of PKCdelta is not required for its inhibitory role in TCR-induced NF-kappaB activation
L255G
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mutated activator-binding site: mutation reduces affinity for both phorbol ester and diacylglycerol. Mutation causes significantly reduced membrane translocation by phorbol ester treatment
additional information
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construction of isozyme PKCtheta T-cell knockout mice, which show slightly impaired immune system and are defective in NF-kappaB activation, overview, isozyme PKCdelta knockout mice show a deregulated immune system, overview
additional information
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construction of isozyme-knockout mice, immunological phenotypes of isozyme alpha, beta, delta, epsilon, theta, and zeta knockout mice, overview
additional information
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construction of PKC isozyme, e.g. PKCzeta-deficient or PKCdelta-deficient, knockout mice, construction of PKCbeta-deficient B-cells
additional information
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construction of PKC isozyme-deletion mutant mice leading to important metabolic deficiencies in the mutant mice
additional information
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depletion of PKCdelta using RNAi leads to a marked increase in both urokinase-type plasminogen activator and matrix metalloproteinase-9 secretion, while PKCdelta overexpression significantly decreases urokinase-type plasminogen activator and matrix metalloproteinase-9 production, two proteases associated with migratory and invasive capacities
additional information
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specific modulation of apoptosis and Bcl-xL phosphorylation in recombinant yeast by isozymes PKCepsilon and PKCzeta
L367D
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mutation of residues in the hydrophobic interface between the kinase N lobe and the C1B domain (L358D, L367D, Y422D, Y430D) results in 5- to 14fold decrease in the EC50 for phorbol 12-myristate 13-acetate induced translocation
additional information
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specific modulation of apoptosis and Bcl-xL phosphorylation in recombinant yeast by isozymes PKCepsilon and PKCzeta
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
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a phase II trial of enzastaurin is conducted to determine the 6-month progression-free survival rate in advanced non-small-cell lung cancer using Enzaustaurin: 13% of the patients have a progression-free survival for more than 6 months
molecular biology
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a technique is developed to detect PKCalpha activity in a cancerous cell lysate through the simple measurement of fluorescence intensity. The principle of this methodology is based on a fluorescence increase associated with polyion complex dissociation due to phosphorylation by PKCalpha