Information on EC 2.7.11.1 - non-specific serine/threonine protein kinase and Organism(s) Homo sapiens and UniProt Accession P78368

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Homo sapiens
UNIPROT: P78368


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.1
-
RECOMMENDED NAME
GeneOntology No.
non-specific serine/threonine protein kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (non-specific)
This is a heterogeneous group of serine/threonine protein kinases that do not have an activating compound and are either non-specific or their specificity has not been analysed to date.
CAS REGISTRY NUMBER
COMMENTARY hide
191808-15-8
phosphoinositide dependent protein kinase 1
340830-03-7
-
37278-10-7
-
377752-08-4
ribosomal protein S6 kinase 2
389133-24-8
ribosomal S6 kinase 3
52660-18-1
casein kinase, protein kinase CK2
9026-43-1
this CAS Reg. No. encompasses a great variety of protein kinases including the serine/threonine specific kinases
90698-26-3
ribosomal protein S6 kinase 1
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
important role of Pim1 kinase in regulating hematopoietic stem cell (HSC) cell proliferation and survival, and relative role of individual Pim kinase in hematopoietic stem cell functions and regulation, overview
malfunction
chemical inhibition, siRNA, and expression of dominant-negative p110alpha are all associated with increased AMPK T172 phosphorylation, whereas expression of constitutively-active p110alpha reduces T172 phosphorylation. Pharmacological inhibition of p110a reduces AMPK S485/491 phosphorylation, while constitutively-active p110alpha increases AMPK S485/491 phosphorylation. In response to oligomycin or serum starvation, AMPK T172 phosphorylation is elevated in p110alpha-deficient myoblasts compared to control myoblasts. p110alpha deficiency modifies AMPK responses to cellular stress
physiological function
AMP-activated protein kinase (AMPK) is a serine/threonine kinase that functions as a sensor of intracellular energy. Activation of AMPK is associated with increased phosphorylation of the alpha-subunit at threonine 172 and decreased phosphorylation at serine 485 in AMPKalpha1 and serine 491 in AMPKalpha2 (S485/491). p110alpha-mediated phosphorylation of AMPKa at S485/491 is Akt-dependent
malfunction
Blockade of p110alpha by RNA interference or multiple independent PI3K inhibitors not only blocks Ser585 phosphorylation in cytokine-dependent cells and primary human AML blasts, but also results in a block in survival signaling and cell death
physiological function
phosphoinositide 3-kinase (PI3K) is a dual specificity kinase that is known to be involved in cell survival and malignant transformation, and it is able to phosphorylate both lipid and protein substrates. PI3K protein kinase activity can directly phosphorylate growth factor receptors on human hematopoietic (blood) cells to promote a survival-only response. The protein kinase activity but not the lipid kinase activity of PI3K promotes cytokine-mediated cell survival. It phosphorylates serine residues in the cytoplasmic portion of cytokine receptors to promote hemopoietic cell survival. The PI3K lipid kinase activity is not essential for regulating cell survival
malfunction
isoproterenol-induced EGFR transactivation is abolished in PI3Kgamma null mutants or through enzyme inhibition by wortmannin or LY-294002
metabolism
the enzyme is involved in isoproterenol-induced EGFR transactivation. PI3K is required for beta2AR-stimulated EGFR transactivation
physiological function
the generation of phosphatidylinositol (3,4,5)-tris-phosphate (PIP3) by the lipid kinase function stabilizes beta2AR-EGFR complexes while the protein kinase activity of PI3K regulates Src activation by direct phosphorylation. Phosphorylation of Src by phosphoinositide 3-kinase regulates beta-adrenergic receptor-mediated EGFR transactivation. EGFR transactivation is a mechanism by which the EGF receptor is stimulated, internalized, and downstream signaling initiated following agonist stimulation by a GPCR, such as the beta-adrenergic receptor. The protein kinase activity of PI3K phosphorylates serine residue 70 on Src to enhance its activity and induce EGFR transactivation following beta-adrenergic receptor stimulation. This additional function for PI3K, whereby Src is a substrate for the protein kinase activity of enzyme PI3K, is of importance since Src plays a key role in pathological and physiological signaling
evolution
the enzyme is a member of the family of phosphatidylinositol-3 kinase-related kinases (PIKKs). All of these can interact with different membrane mimetics and may have different preferences only for membrane properties such as surface charge, curvature, and lipid packing. The FATC domain is shared by all members of the family and plays an important role for the regulation of each PIKK. Sequence conservation of the FATC domain
physiological function
the enzyme is important for DNA damage response and signaling in the presence of DNA damages
evolution
the enzyme is a member of the family of phosphatidylinositol-3 kinase-related kinases (PIKKs). All of these can interact with different membrane mimetics and may have different preferences only for membrane properties such as surface charge, curvature, and lipid packing. The FATC domain is shared by all members of the family and plays an important role for the regulation of each PIKK. Sequence conservation of the FATC domain
physiological function
the enzyme is important for DNA damage response and signaling in the presence of DNA damages
evolution
the enzyme is a member of the family of phosphatidylinositol-3 kinase-related kinases (PIKKs). All of these can interact with different membrane mimetics and may have different preferences only for membrane properties such as surface charge, curvature, and lipid packing. The FATC domain is shared by all members of the family and plays an important role for the regulation of each PIKK. Sequence conservation of the FATC domain
physiological function
the enzyme is important for DNA damage response and signaling in the presence of DNA damages
evolution
human serine/threonine kinase ULK3 is annotated as belonging to unc-51-like family of serine/threonine kinases, but shares similarity with STK36 and dFu proteins
malfunction
kinase-deficient mutants of ULK3 are inactive in regulation of GLI protein activity
physiological function
the serine/threonine kinase ULK3 acts as a positive regulator of Hedgehog pathway and Gli proteins, ULK3 catalytical activity is crucial for its function in SHH pathway, overview. The Hedgehog signaling pathway plays crucial roles in embryonic development and is implicated in tissue homeostasis maintenance and neurogenesis in adults. ULK3 enhances endogenous and overexpressed GLI1 and GLI2 transcriptional activity in cultured cells, and ULK3 kinase activity is required for nuclear translocation of GLI1 from cytosol
evolution
the enzyme is a member of the family of phosphatidylinositol-3 kinase-related kinases (PIKKs). All of these can interact with different membrane mimetics and may have different preferences only for membrane properties such as surface charge, curvature, and lipid packing. The FATC domain is shared by all members of the family and plays an important role for the regulation of each PIKK. Sequence conservation of the FATC domain
physiological function
the enzyme is important for DNA damage response and signaling in the presence of DNA damages
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + 4E-BP1 protein
ADP + phosphorylated 4E-BP1 protein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + ABCA1 NBD1-R1 protein
ADP + phosphorylated ABCA1 NBD1-R1 protein
show the reaction diagram
-
substrate protein is a recombinant construct of wild-type and mutant nucleotide binding domain 1 and cytoplasmic domain R1 of ATP-binding cassette transporter protein A1 expressed in Escherichia coli, phosphorylation at T1242, T1243, and S1255
-
-
?
ATP + ABCA1 NBD2-R2 protein
ADP + phosphorylated ABCA1 NBD2-R2 protein
show the reaction diagram
-
substrate protein is a recombinant construct of wild-type and mutant nucleotide binding domain 2 and cytoplasmic domain R2 of ATP-binding cassette transporter protein A1 expressed in Escherichia coli
-
-
?
ATP + Ac-RPRAASF
ADP + Ac-Ac-RPRAApSF
show the reaction diagram
-
an efficient fluorescence assay for serine/threonine kinases using a peptide array is developed. Assay is based on chemical reactions specific to phosphoserine and phosphothreonine residues, that is, base-mediated beta-elimination of the phosphate group and subsequent Michael addition of a thiol-containing fluorescent reagent. This procedure enables the covalent introduction of a fluorescent moiety into the phosphorylated peptide. Novel fluorescent reagents are designed for this purpose and synthesized
-
-
?
ATP + acetyl-CoA carboxylase
ADP + phosphorylated acetyl-CoA carboxylase
show the reaction diagram
-
phosphorylation and inactivation
-
-
?
ATP + adenomatous polyposis coli protein
ADP + phosphorylated adenomatous polyposis coli protein
show the reaction diagram
-
i.e. APC, APC is phosphorylated in vitro by CKIdelta and CKIepsilon
-
-
?
ATP + AIB1 protein
ADP + phosphorylated AIB1 protein
show the reaction diagram
-
phosphorylation at S601 by isozyme CK1delta
-
-
?
ATP + AKAP450
ADP + phospho-AKAP450
show the reaction diagram
ATP + alpha-casein
ADP + phosphorylated alpha-casein
show the reaction diagram
-
casein kinase 1alpha
-
-
?
ATP + AMP-activated protein kinase alpha1
ADP + phospho-AMP-activated protein kinase
show the reaction diagram
phosphorylation of Ser485 at subunit alpha1 and of Ser491 at subunit alpha2
-
-
?
ATP + ataxin-3 protein
ADP + phosphorylated ataxin-3 protein
show the reaction diagram
-
phosphorylation at serines 340 and 352
-
-
?
ATP + axin
ADP + phosphorylated axin
show the reaction diagram
-
glycogen synthase kinase 3
-
-
?
ATP + BAF155
ADP + phosphorylated BAF155
show the reaction diagram
ATP + BAF170
ADP + phosphorylated BAF170
show the reaction diagram
-
BAF170 is a hSWI/SNF protein that contains one Akt consensus site
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
ATP + beta-hydroxy beta-methylglutaryl-coenzyme A reductase
ADP + phosphorylated beta-hydroxy beta-methylglutaryl-coenzyme A reductase
show the reaction diagram
-
phosphorylation and inactivation
-
-
?
ATP + calmodulin
ADP + phosphorylated calmodulin
show the reaction diagram
-
phosphorylation by isozyme CK1alpha
-
-
?
ATP + CARMA1 protein
ADP + phosphorylated CARMA1
show the reaction diagram
-
i.e. CARD11 protein, phosphorylation at S608 by isozyme CK1alpha
-
-
?
ATP + CDC25A
ADP + phospho-CDC25A
show the reaction diagram
ATP + Cdc25A
ADP + phosphorylated Cdc25A
show the reaction diagram
ATP + Cdc25C
ADP + ?
show the reaction diagram
-
Chk2 phosphorylated Cdc25C on Ser216
-
-
?
ATP + Cdc42Hs
ADP + ?
show the reaction diagram
PAK4 interacts only with the activated form of Cdc42Hs through its GTPase-binding domain
-
-
?
ATP + Cdk2 interacting protein
ADP + phosphorylated Cdk2 interacting protein
show the reaction diagram
-
-
-
-
?
ATP + cell division cycle 7
ADP + phosphorylated cell division cycle 7
show the reaction diagram
-
-
-
-
?
ATP + claspin
ADP + phosphorylated claspin
show the reaction diagram
-
-
-
-
?
ATP + CREB
ADP + phosphorylated CREB
show the reaction diagram
ATP + Daxx
ADP + phosphorylated Daxx
show the reaction diagram
ATP + Dnmt1 protein
ADP + phosphorylated Dnmt1 protein
show the reaction diagram
-
phosphorylation at S147 by isozymes CK1delta and CK1epsilon
-
-
?
ATP + FADD protein
ADP + phosphorylated FADD protein
show the reaction diagram
-
phosphorylation at S194 by isozyme CK1alpha
-
-
?
ATP + geminin
ADP + phosphorylated geminin
show the reaction diagram
ATP + Gli protein
ADP + phosphorylated Gli protein
show the reaction diagram
ATP + Gli1 protein
ADP + phosphorylated Gli1 protein
show the reaction diagram
low activity
-
-
?
ATP + Gli2 protein
ADP + phosphorylated Gli2 protein
show the reaction diagram
high activity
-
-
?
ATP + Gli3 protein
ADP + phosphorylated Gli3 protein
show the reaction diagram
low activity
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
show the reaction diagram
ATP + glycogen synthase kinase 3
ADP + phosphorylated glycogen synthase kinase 3
show the reaction diagram
ATP + glycogen synthase kinase-3 (GSK-3) fusion protein
ADP + phosphorylated- glycogen synthase kinase-3 fusion protein
show the reaction diagram
-
-
-
-
?
ATP + granulocyte macrophage colony stimulating factor receptor
ADP + phospho-granulocyte macrophage colony stimulating factor receptor
show the reaction diagram
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
ATP + histone H2A
ADP + phosphorylated histone H2A
show the reaction diagram
recombinant human substrate, substrate of SSTK
-
-
?
ATP + histone H2AX
ADP + phosphorylated histone H2AX
show the reaction diagram
recombinant human substrate, substrate of SSTK
-
-
?
ATP + histone H2B
ADP + phosphorylated histone H2B
show the reaction diagram
recombinant human substrate, substrate of SSTK
-
-
?
ATP + histone H4
ADP + phosphorylated histone H4
show the reaction diagram
recombinant substrate from Xenopus laevis, substrate of SSTK
-
-
?
ATP + hypoxia-inducible factor-1
ADP + phosphorylated hypoxia-inducible factor-1
show the reaction diagram
ATP + IFNAR1 protein
ADP + phosphorylated IFNAR1 protein
show the reaction diagram
-
phosphorylation at S535 by isozyme CK1alpha
-
-
?
ATP + IKKalpha protein
ADP + phosphorylated IKKalpha protein
show the reaction diagram
-
-
-
-
?
ATP + interleukin 3
ADP + phospho-interleukin-3
show the reaction diagram
ATP + KKRNRRLSVA
ADP + KKRNRRL-phosphoserine-VA
show the reaction diagram
-
peptide substrate of NDR1
-
-
?
ATP + KKRNRRLSVA
ADP + phosphorylated-KKRNRRLSVA
show the reaction diagram
-
-
-
?
ATP + KLP10A protein
ADP + phosphorylated KLP10A protein
show the reaction diagram
-
phosphorylation at S573 by isozyme CK1alpha
-
-
?
ATP + Lys-Lys-Phe-Asn-Arg-Thr-Leu-Ser-Val-Ala
ADP + ?
show the reaction diagram
ATP + M3-muscarnic receptor
ADP + phosphorylated M3-muscarnic receptor
show the reaction diagram
-
-
-
-
?
ATP + MARCKS protein
ADP + MARCKS phosphoprotein
show the reaction diagram
-
isozyme PKNalpha
-
-
?
ATP + MB protein
ADP + MB phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + MCM2
ADP + ?
show the reaction diagram
-
wild-type huCdc7 protein expressed in COS7 cells phosphorylates MCM2 and MCM3 proteins in vitro
-
-
?
ATP + MCM3
ADP + ?
show the reaction diagram
-
wild-type huCdc7 protein expressed in COS7 cells phosphorylates MCM2 and MCM3 proteins in vitro
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
ATP + non-structural protein 2
ADP + phospho-non-structural protein 2
show the reaction diagram
-
non-structural protein 2 from bluetongue virus (BTV)
-
-
?
ATP + non-structural protein 2
ADP + phosphorylated non-structural protein 2
show the reaction diagram
-
-
-
-
?
ATP + NS5A protein
ADP + phosphorylated NS5A protein
show the reaction diagram
-
recombinant NS5A expressed in Sf9 cells, substrate is a hepatitis C virus protein playing a critical role in virus replication and conferring interferon resistance to the virus, the viral protein is phosphorylated by several STE or AGC type protein kinases CK2, AKT1, SGK1, 90S6K, STE, phosphorylation patterns, overview
-
-
?
ATP + OTUB1
ADP + phospho-OTUB1
show the reaction diagram
-
OTUB1 is a tumor domain protease, phosphorylation at Ser16, in GSDSEGVN
-
-
?
ATP + OTUB1 protein
ADP + phosphorylated OTUB1 protein
show the reaction diagram
-
phosphorylation at serine 16
-
-
?
ATP + OTUD5 protein
ADP + phosphorylated OTUD5 protein
show the reaction diagram
-
phosphorylation at serine 177
-
-
?
ATP + peptide LRRKtide
ADP + phosphorylated peptide LRRKtide
show the reaction diagram
-
high activity towards the peptidic substrate LRRKtide
-
-
?
ATP + PHLPP1 protein
ADP + phosphorylated PHLPP1 protein
show the reaction diagram
-
phosphorylation at T851 by isozyme CK1alpha
-
-
?
ATP + phospho-glycogen synthase peptide
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + phosphoglycogen synthase peptide 2
ADP + phosphorylated phosphoglycogen synthase peptide 2
show the reaction diagram
-
-
-
-
?
ATP + phospholipase D
ADP + phosphorylated phospholipase D
show the reaction diagram
ATP + PKB protein kinase
ADP + phosphorylated PKB protein kinase
show the reaction diagram
ATP + PKD2 protein
ADP + phosphorylated PKD2 protein
show the reaction diagram
-
phosphorylation at S244 by isozymes CK1alpha, CK1delta, and CK1epsilon
-
-
?
ATP + procaspase-2
ADP + phosphorylated procaspase-2
show the reaction diagram
ATP + protein
ADP + a phosphoprotein
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
phosphorylates and inactivates the actin binding/depolymerizing factor cofilin and induces actin cytoskeletal changes
-
-
?
ATP + protein INI
ADP + phosphorylated INI
show the reaction diagram
-
INI is a hSWI/SNF protein
-
-
?
ATP + protein kinase C
ADP + phosphorylated protein kinase C
show the reaction diagram
-
isozyme PKNalpha
-
-
?
ATP + protein LRP6
ADP + phosphorylated protein LRP6
show the reaction diagram
-
CKIgamma
-
-
?
ATP + protein TCF3
ADP + phosphorylated protein TCF3
show the reaction diagram
-
CKIepsilon
-
-
?
ATP + rapamycin
ADP + phospho-rapamycin
show the reaction diagram
-
-
-
?
ATP + Rec8 protein
ADP + phosphorylated Rec8 protein
show the reaction diagram
-
phosphorylation at S412 by isozyme CK1delta and CK1epsilon, and at S400, S402, S404, S410, T414, and S416
-
-
?
ATP + RRRDDDSDDD
ADP + RRRDDDphosphoSDDD
show the reaction diagram
-
a CK2-specific synthetic peptide substrate
-
-
?
ATP + RRRLSSLRA
ADP + RRRLSpSLRA
show the reaction diagram
-
enzyme activities are determined by measuring initial velocities for His6-S6K1aII(DELTA AID)-T389E catalyzed phosphorylation of a commercially available S6K/RSK model peptide substrate 1 (S6K1-Tide, RRRLSSLRA)
-
-
?
ATP + RSRSRSRSRSRSPPPVSK
ADP + phosphorylated RSRSRSRSRSRSPPPVSK
show the reaction diagram
-
SC35-derived peptide 180-197, recombinant GSK-3beta
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
ATP + SF2/ASF
ADP + phosphorylated SF2/ASF
show the reaction diagram
ATP + SIV/17E-Fr Nef protein
ADP + phosphorylated SIV/17E-Fr Nef protein
show the reaction diagram
ATP + SLR1 protein
ADP + phosphorylated SLR1 protein
show the reaction diagram
-
phosphorylation at S196 and SS510
-
-
?
ATP + Snail protein
ADP + phosphorylated Snail protein
show the reaction diagram
-
phosphorylation at S104 and S07 by isozyme CK1epsilon
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
enzyme plays a role as a co-repressor for homeodomain transcription factors
-
-
?
ATP + Src protein
ADP + phosphorylated Src protein
show the reaction diagram
ATP + SSH1L protein
ADP + SSH1L phosphoprotein
show the reaction diagram
-
PKD1 phosphorylates the SSH enzyme SSH1L at serine 978
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + TRPM4
ADP + phospho-TRPM4
show the reaction diagram
-
i.e. transient receptor potential melastatin-like 4, phosphorylation at Ser839
-
-
?
ATP + TRPM4 protein
ADP + phosphorylated TRPM4 protein
show the reaction diagram
-
phosphorylation at serine 839
-
-
?
ATP + Varicella-Zoster viral gB protein
ADP + phosphorylated Varicella-Zoster viral gB protein
show the reaction diagram
-
phosphorylation at S34 in the sequence QSEDIT
-
-
?
ATP + vimentin
ADP + phosphorylated vimentin
show the reaction diagram
-
isozyme PKNalpha
-
-
?
ATP + YAP protein
ADP + phosphorylated YAP protein
show the reaction diagram
-
phosphorylation at S384 and S387 by isozymes CK1delta and CK1epsilon
-
-
?
ATP + [FRAT-2 protein]
ADP + phosphorylated [FRAT-2 protein]
show the reaction diagram
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, phosphorylation by GSK3beta
-
-
?
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
show the reaction diagram
-
recombinant substrate expressed in HEK-293 and CHO cells, casein kinase 1alpha
-
-
?
ATP + [tau-protein]
ADP + O-phospho -[tau-protein]
show the reaction diagram
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
casein + ATP
phosphorylated casein + ADP
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + 4E-BP1 protein
ADP + phosphorylated 4E-BP1 protein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + adenomatous polyposis coli protein
ADP + phosphorylated adenomatous polyposis coli protein
show the reaction diagram
-
i.e. APC, APC is phosphorylated in vitro by CKIdelta and CKIepsilon
-
-
?
ATP + AKAP450
ADP + phospho-AKAP450
show the reaction diagram
-
-
-
-
?
ATP + alpha-casein
ADP + phosphorylated alpha-casein
show the reaction diagram
-
casein kinase 1alpha
-
-
?
ATP + AMP-activated protein kinase alpha1
ADP + phospho-AMP-activated protein kinase
show the reaction diagram
P42336
phosphorylation of Ser485 at subunit alpha1 and of Ser491 at subunit alpha2
-
-
?
ATP + ataxin-3 protein
ADP + phosphorylated ataxin-3 protein
show the reaction diagram
-
phosphorylation at serines 340 and 352
-
-
?
ATP + axin
ADP + phosphorylated axin
show the reaction diagram
-
glycogen synthase kinase 3
-
-
?
ATP + BAF155
ADP + phosphorylated BAF155
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
ATP + CDC25A
ADP + phospho-CDC25A
show the reaction diagram
-
STK38 phosphorylates CDC25A at Ser76
-
-
?
ATP + Cdc25A
ADP + phosphorylated Cdc25A
show the reaction diagram
-
phosphorylation site Ser76
-
-
?
ATP + Cdk2 interacting protein
ADP + phosphorylated Cdk2 interacting protein
show the reaction diagram
-
-
-
-
?
ATP + cell division cycle 7
ADP + phosphorylated cell division cycle 7
show the reaction diagram
-
-
-
-
?
ATP + claspin
ADP + phosphorylated claspin
show the reaction diagram
-
-
-
-
?
ATP + CREB
ADP + phosphorylated CREB
show the reaction diagram
Q6SA08
phosphorylation by TSSK5 at Ser133 stimulates the cAMP responsive element/cAMP responsive element binding protein CRE/CREB responsive pathway in recombinant HEK293 cells
-
-
?
ATP + Daxx
ADP + phosphorylated Daxx
show the reaction diagram
-
Daxx is a protein acting in TGF-beta-induced JNK activation and in apoptosis
-
-
?
ATP + geminin
ADP + phosphorylated geminin
show the reaction diagram
-
a cell cycle regulatory protein
-
-
?
ATP + Gli protein
ADP + phosphorylated Gli protein
show the reaction diagram
-
the Gli proteins are important in regulation of Hedgehog signaling, overview
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
show the reaction diagram
-
glycogen synthase kinase 3 is involved in the insulin signaling pathway regulating glycogen synthesis via glycogen synthase antagonizing insulin
-
-
?
ATP + glycogen synthase kinase 3
ADP + phosphorylated glycogen synthase kinase 3
show the reaction diagram
-
PKB protein kinase
-
-
?
ATP + granulocyte macrophage colony stimulating factor receptor
ADP + phospho-granulocyte macrophage colony stimulating factor receptor
show the reaction diagram
P42336
-
-
-
?
ATP + hypoxia-inducible factor-1
ADP + phosphorylated hypoxia-inducible factor-1
show the reaction diagram
-
i.e. HIF-1, casein kinase 2 inhibits the activation of HIF-1 activity by phosphorylation and thereby stabilization of the protein, CK2 is involved in and influenced by hypoxia, overview
-
-
?
ATP + IKKalpha protein
ADP + phosphorylated IKKalpha protein
show the reaction diagram
-
-
-
-
?
ATP + interleukin 3
ADP + phospho-interleukin-3
show the reaction diagram
P42336
-
-
-
?
ATP + M3-muscarnic receptor
ADP + phosphorylated M3-muscarnic receptor
show the reaction diagram
-
-
-
-
?
ATP + non-structural protein 2
ADP + phosphorylated non-structural protein 2
show the reaction diagram
-
-
-
-
?
ATP + OTUB1
ADP + phospho-OTUB1
show the reaction diagram
-
OTUB1 is a tumor domain protease, phosphorylation at Ser16, in GSDSEGVN
-
-
?
ATP + OTUB1 protein
ADP + phosphorylated OTUB1 protein
show the reaction diagram
-
phosphorylation at serine 16
-
-
?
ATP + OTUD5 protein
ADP + phosphorylated OTUD5 protein
show the reaction diagram
-
phosphorylation at serine 177
-
-
?
ATP + peptide LRRKtide
ADP + phosphorylated peptide LRRKtide
show the reaction diagram
-
high activity towards the peptidic substrate LRRKtide
-
-
?
ATP + phospholipase D
ADP + phosphorylated phospholipase D
show the reaction diagram
-
CKII is involved in 4beta-phorbol 12-myristate 13-acetate-induced phospholipase D activation, of PLD1 or PLD2 activity as well as basal PLD activity
-
-
?
ATP + PKB protein kinase
ADP + phosphorylated PKB protein kinase
show the reaction diagram
-
PDK1 kinase, phosphorylates Thr308 and Ser473, which is required for activation of PKB
-
-
?
ATP + procaspase-2
ADP + phosphorylated procaspase-2
show the reaction diagram
-
phosphorylation of procaspase-2 by CK2 prevents the activation of caspase activity by inhibiting the dimerization of procaspase-2, CK2 activity is involved in the direct regulation of the caspase-8 pathway, where it can control caspase-8 activity through the phosphorylation of ARC or by preventing the ability of caspase-8 to cleave its target Bid
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
P53667
phosphorylates and inactivates the actin binding/depolymerizing factor cofilin and induces actin cytoskeletal changes
-
-
?
ATP + protein LRP6
ADP + phosphorylated protein LRP6
show the reaction diagram
-
CKIgamma
-
-
?
ATP + protein TCF3
ADP + phosphorylated protein TCF3
show the reaction diagram
-
CKIepsilon
-
-
?
ATP + rapamycin
ADP + phospho-rapamycin
show the reaction diagram
P78527, Q13315, Q13535, Q96Q15
-
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
-
-
?
ATP + SIV/17E-Fr Nef protein
ADP + phosphorylated SIV/17E-Fr Nef protein
show the reaction diagram
-
phosphorylation at Ser12, the protein kinase CK2 associates with the Nef proteins from the Human immunodeficiency virus and the macrophage-tropic neurovirulent Simian immunodeficiency virus clone, SIV/17E-Fr, the Nef protein play important roles in viral disease progression
-
-
?
ATP + SR protein
ADP + ?
show the reaction diagram
Q9H2X6
enzyme plays a role as a co-repressor for homeodomain transcription factors
-
-
?
ATP + Src protein
ADP + phosphorylated Src protein
show the reaction diagram
P48736
-
-
-
?
ATP + SSH1L protein
ADP + SSH1L phosphoprotein
show the reaction diagram
-
PKD1 phosphorylates the SSH enzyme SSH1L at serine 978
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
-
tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview
-
-
?
ATP + TRPM4
ADP + phospho-TRPM4
show the reaction diagram
-
i.e. transient receptor potential melastatin-like 4, phosphorylation at Ser839
-
-
?
ATP + TRPM4 protein
ADP + phosphorylated TRPM4 protein
show the reaction diagram
-
phosphorylation at serine 839
-
-
?
ATP + [tau-protein]
ADP + O-phospho -[tau-protein]
show the reaction diagram
-
tau is primarily found in neurons, regulation of tau phosphorylation by GSK3beta via interaction with FRAT-1 and FRAT-2, i.e. frequently rearranged in advanced T-cell lymphoma proteins
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zn2+
-
bound to the zinc finger core at residues 105-147 and coordinated by Cys109, Cys114, Cys137 ans Cys140, of the beta subunit dimer
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid
-
i.e. IQA
(5Z)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylidene)-2-thioxoimidazolidin-4-one
-
-
(S)-2-(2-aminopyrimidiny-4-yl)-7-(2-fluoroethyl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridinione
-
-
(Z)-5-(4-propoxybenzylidene) thiazolidine-2,4-dione
-
a Pim-2 inhibitor
1-(beta-D-2'-deoxyribofuranosyl)-4,5,6,7-tetrabromo-1H-benzimidazole
-
TDB, a cell-permeable selective inhibitor of CK2, inhibts the phosphorylation of OTUB1 at Ser16. In addition to CK2, TDB inhibits 3 other kinases, namely PIM1, CLK2 and DYRK1A, but none of these kinases phosphorylates OTUB1 in vitro
-
2-(2-aminopyrimidin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
-
-
2-Aminopurine
-
-
2-chloro-N-(4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)phenyl)benzamide
-
2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole
2-phenyl-5-(pyridin-4-yl)-1H-pyrrole-3-carboxamide
-
-
3,8-dibromo-7-hydroxy-4-methyl-2H-chromen-2-one
-
i.e. DBC
3-{3-[4-(1-Methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate
-
-
4,5,6,7-tetrabromo-1H-benzotriazole
-
i.e. TBB
4,5,6,7-tetrabromobenzimidazole
-
i.e. TBBz or TBI
4,5,6,7-tetrabromobenzotriazole
4-(2-(4-(2-(4-acetylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)-N-(2-chlorophenyl)benzamide
-
4-hydroxy-trans-2-nonenal
-
i.e. 4-HNE, binds to the enzyme at Lys197 and inhibits its activity by 69% by inhibiting its posttranslational phosphorylation. 4-HNE binding has no effect on the association of LKB1 with its adaptor proteins, sterile-20-related adaptor and mouse protein 25
5-fluoro-N2,N4-bis(4-methoxyphenyl)pyrimidine-2,4-diamine
-
5-fluoro-N2,N4-di(m-tolyl)pyrimidine-2,4-diamine
-
6-(3-chlorophenyl)-4-(1H-indazol-5-yl)pyrimidin-2(1H)-one
-
-
7,9-dimethyl-8-(prop-2-en-1-yl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amine
-
-
8-hydroxy-4-methyl-9-nitro-2H-benzo[g]chromen-2-one
-
i.e. NBC
alsterpaullone
-
inhibition of AMPK, GSK3beta, S6K1, PKBalpha, PDK1, MAPKAP-K2
AMP-PNP
-
ATP analogue adenosine 5'-(beta,gamma-imino)triphosphate
apigenin
auoinhibitory domain of S6K1
-
-
-
Baicalin
-
one of the major compounds in the Chinese medical herb Scutellaria baicalensis, reduces enzyme expression and activity in badder cancer cells T24
benzene 1,2,3,4-tetrakisphosphate
-
-
benzene 1,2,3,5-tetrakisphosphate
-
-
benzene 1,2,3-trisphosphate
-
-
benzene 1,2,4,5-tetrakisphosphate
-
-
benzene 1,2,4-trisphosphate
-
-
benzene 1,3,5-trisphosphate
-
-
biphenyl 2,3',4,5',6-pentakisphosphate
-
-
BMS-863233
-
-
CKI-7
-
-
Ctl peptide
-
-
CX-4945
-
a CK2 inhibitor
-
D-myo-Inositol 1,3,4,5-tetrakisphosphate
-
-
diC8-phosphatidylinositol 3,4,5-trisphosphate
-
-
ellagic acid
-
-
emodin
enzastaurin
FAALS
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
heparin
-
strongly inhibits casein kinase II
idelalisib
5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4(3H)-one, a PI3Kdelta inhibitor used to treat hematological malignancies. The inhibitior idelalisib is selective, noncovalent, reversible, and ATP-competitive, The compound binds reversibly and noncovalently to the p110delta subunit of the kinase, analysis of binding interactions that confer the potency and selectivity of idelalisib, overview. Idelalisib is a propeller-shaped inhibitor
indirubin-3'-monoxime
-
inhibition of AMPK, GSK3beta, S6K1, PKBalpha, PDK1, MAPKAP-K2
JAK3 inhibitor VI
-
-
K252a
-
-
kenpaullone
-
slight inhibition of AMPK, GSK3beta, PKBalpha, PDK1
LAALS
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
lithium
-
after inhibition of GSK-3 in cortical neurons, the splicing factor SC35 is nuclearly redistributed and enriched in nuclear speckles and colocalizes with the kinase
Ly-294002
-
MLN8054
Aurora A-selective inhibitor
N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide
-
N-(2-chlorophenyl)-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide
-
N-cyclopropyl-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide
-
N-ethyl-3-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]-3a,6a-dihydro-1H-thieno[3,2-c]pyrazole-5-carboxamide
-
-
N-[2-(4-fluorophenyl)ethyl]-5-[2-[(methylsulfonyl)amino]pyrimidin-4-yl]thiophene-2-carboxamide
-
-
PF670462
-
a CK1delta/epsilon kinase inhibitor
-
PHA-767491
-
nanomolar, ATP-competitive, Cdc7 inhibitor
PIK-75
a p110alpha-selective PI3K inhibitor
purvalanol
-
inhibition of AMPK, slight inhibition of GSK3beta and S6K1, PKBalpha
Ro 31-8220
-
-
roscovitine
-
slight inhibition of PKBalpha and MAPKAP-K2
SB203580
slight inhibition of the protein kinase
staurosporine
-
-
Su-11248
-
-
TAACS
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALD
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALE
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TBCA
-
-
Wortmannin
-
YM024
a p110alpha-selective PI3K inhibitor
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
5'-AMP
arachidonic acid
-
activates in vitro, binds at the autoinhibitory site at the C-terminal C2-domain
cardiolipin
-
activates isozyme PKNalpha
cytokine
physiological concentrations of cytokine in the picomolar range were sufficient for activating the protein kinase activity of PI3K leading to Ser585 phosphorylation and hemopoietic cell survival but did not activate PI3K lipid kinase signaling or promote proliferation
-
fatty acids
-
activate PKN1
FRAT-2
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, activates phosphorylation of primed sites of tau protein about 8fold, no effect on unprimed site phosphorylation
-
gastrin
-
bind to the cysteine-rich domain C1b, activates, triggers nuclear accumulation of PPKD2 in AGS-B cancer cells
Insulin
-
kenpaullone
-
slight activation of S6K1
linoleic acid
-
-
lysophosphatidic acid
-
activates isozyme PKNalpha
lysophosphatidylinositol
-
activates isozyme PKNalpha
PDK1 interacting fragment PIF
-
required for activity of PDK1
-
pervanadate
-
activation of Akt is associated with tyrosine phosphorylation of Akt
-
Phorbol esters
-
bind to the cysteine-rich domain C1b
phosphatidylinositol 3,4,5-trisphosphate
phosphatidylinositol 4,5-bisphosphate
-
activates isozyme PKNalpha
pyrvinium
-
an FDA-approved anthelmintic drug, a very potent allosteric activator of CKalpha that inhibits the Wnt/beta-catenin pathway by increasing phosphorylation and degradation of beta-catenin, along with other key substrates. it is specific for CK1alpha versus other forms of CK1
Rho
-
activates PKN1
-
RhoA
-
small GTPase, binds to the ACC domain and activates isozymes PKNalpha and PRK2/PKNgamma/PAK-2
Serum
-
,activation of Akt is associated with tyrosine phosphorylation of Akt
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0048 - 0.134
ATP
0.0093
Lys-Lys-Phe-Asn-Arg-Thr-Leu-Ser-Val-Ala
-
-
0.0036 - 0.0037
RRRLSSLRA
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.057 - 0.19
ATP
0.057 - 0.19
RRRLSSLRA
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00017
(5-oxo-5,6-dihydroindolo[1,2-a]quinazolin-7-yl)acetic acid
-
-
0.00004
2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole
-
-
0.0004
4,5,6,7-tetrabromo-1H-benzotriazole
-
-
0.0007
4,5,6,7-tetrabromobenzimidazole
-
-
0.00074
apigenin
-
-
0.00008
benzene 1,2,3,4-tetrakisphosphate
-
values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate
0.00022
benzene 1,2,3,5-tetrakisphosphate
-
values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate
0.00059
benzene 1,2,3-trisphosphate
-
values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate
0.00011
benzene 1,2,4,5-tetrakisphosphate
-
values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate
0.00061
benzene 1,2,4-trisphosphate
-
values for inhibition at the PH-domain of PKBalpha are obtained using competition with biotinylated diC8-phosphatidylinositol 3,4-bisphosphate
0.00218
benzene 1,3,5-trisphosphate