Information on EC 2.7.10.2 - non-specific protein-tyrosine kinase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY
2.7.10.2
-
RECOMMENDED NAME
GeneOntology No.
non-specific protein-tyrosine kinase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
reaction mechanism
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
catalytic mechanism
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
regulation of enzyme activity involves the activation loop, a polypeptide region outside the active site cleft, which is reversibly phosphorylated
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
structure-function relation ship, active site structure, catalytic mechanism involving the catalytic base Asp386 and enzyme regulation, overview
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
structure-function relationship, active site structure, catalytic mechanism and enzyme regulation, overview
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
substrate binding site involving residues R279, R281, and R283, more distant residues S280, F382, S273, and D276 are also important for activity
-
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
residue W1038 is essential for catalytic activity
Q62120
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (non-specific)
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families [1].
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
70 kDa zeta-associated protein
-
-
-
-
ACTR-IIB
-
-
-
-
ACTRIIA
-
-
-
-
Agammaglobulinaemia tyrosine kinase
-
-
-
-
Amylovoran biosynthesis membrane-associated protein amsA
-
-
-
-
ATK
-
-
-
-
B cell progenitor kinase
-
-
-
-
B lymphocyte kinase
-
-
-
-
B-cell/myeloid kinase
-
-
-
-
BCR-ABL tyrosine kinase
-
-
-
-
BMK
-
-
-
-
BMP type II receptor
-
-
-
-
BMP-2/BMP-4 receptor
-
-
-
-
Bone marrow kinase BMX
-
-
-
-
BPK
-
-
-
-
Breast tumor kinase
-
-
-
-
Bruton's tyrosine kinase
-
-
-
-
c-ABL
-
-
-
-
c-FER
-
-
-
-
C-FES
-
-
-
-
C-SRC
-
-
-
-
C-SRC kinase
-
-
-
-
C-YES
-
-
-
-
CADTK
-
-
-
-
CAK beta
-
-
-
-
Calcium-dependent tyrosine kinase
-
-
-
-
Cell adhesion kinase beta
-
-
-
-
D-ash
-
-
-
-
DFer
-
-
-
-
Dsrc28C
-
-
-
-
ectoprotein kinase
-
-
-
-
Epithelial and endothelial tyrosine kinase
-
-
-
-
EPS I polysaccharide export protein epsB
-
-
-
-
focal adhesion kinase 1
-
-
-
-
gene lck protein kinase
-
-
-
-
gene lck tyrosine kinase
-
-
-
-
Hematopoietic consensus tyrosine-lacking kinase
-
-
-
-
Hemopoietic cell kinase
-
-
-
-
IL-2-inducible T-cell kinase
-
-
-
-
Itk
-
-
-
-
JAK protein tyrosine kinase
-
-
-
-
Kinase EMB
-
-
-
-
Kinase EMT
-
-
-
-
Kinase TLK
-
-
-
-
kinase, protein (phosphorylating tyrosine)
-
-
-
-
kinase, protein p56lck (phosphorylating)
-
-
-
-
L-JAK
-
-
-
-
Lck Tyrosine kinase
-
-
-
-
Leukocyte janus kinase
-
-
-
-
LSK
-
-
-
-
nonreceptor protein tyrosine kinase
-
-
-
-
NTK38
-
-
-
-
Nuclear tyrosine protein kinase RAK
-
-
-
-
ORF6
-
-
-
-
p150
-
-
-
-
p55-BLK
-
-
-
-
P55-FGR
-
-
-
-
p56-HCK
-
-
-
-
p56-HCK/p59-HCK
-
-
-
-
P56-LCK
-
-
-
-
p56lck kinase
-
-
-
-
p56lck protein kinase
-
-
-
-
p56lck protein tyrosine kinase
-
-
-
-
p56lck tyrosine kinase
-
-
-
-
P57-STK
-
-
-
-
P59-FYN
-
-
-
-
p59-HCK/p60-HCK
-
-
-
-
P60-SRC
-
-
-
-
p60-YRK
-
-
-
-
P61-YES
-
-
-
-
p94-FER
-
-
-
-
phosphotyrosyl-protein kinase
-
-
-
-
PP125FAK
-
-
-
-
Protein kinase (tyrosine-phosphorylating)
-
-
-
-
protein kinase A
-
-
-
-
Protein kinase BATK
-
-
-
-
Protein kinase HYL
-
-
-
-
Protein kinase Lck
-
-
-
-
Protein kinase NTK
-
-
-
-
Protein kinase p56-LCK
-
-
-
-
Protein kinase p56lck
-
-
-
-
Protein p56c-lck kinase
-
-
-
-
Protein p56lck tyrosine kinase
-
-
-
-
Protein tyrosine kinase
-
-
-
-
protein tyrosine kinase 2beta
-
-
-
-
Protein tyrosine kinase lck
-
-
-
-
Protein tyrosine kinase p56lck
-
-
-
-
Protein tyrosine kinase pp56lck
-
-
-
-
Protein-tyrosine kinase C-TKL
-
-
-
-
Protein-tyrosine kinase CYL
-
-
-
-
PTK
-
-
-
-
PTK-RL-18
-
-
-
-
PTK70
-
-
-
-
Quek1
-
-
-
-
Related adhesion focal tyrosine kinase
-
-
-
-
Resting lymphocyte kinase
-
-
-
-
Rlk/Txk
-
-
-
-
S-domain receptor-like protein kinase
-
-
-
-
SLK
-
-
-
-
Spleen tyrosine kinase
-
-
-
-
src-kinase
-
-
-
-
SRC-related intestinal kinase
-
-
-
-
Syk-related tyrosine kinase
-
-
-
-
SYN
-
-
-
-
T cell-specific protein-tyrosine kinase
-
-
-
-
T-cell-specific kinase
-
-
-
-
Tyrosine kinase
-
-
-
-
Tyrosine kinase ARG
-
-
-
-
Tyrosine kinase lck
-
-
-
-
Tyrosine kinase p56lck
-
-
-
-
Tyrosine phosphokinase
-
-
-
-
Tyrosine protein kinase
-
-
-
-
Tyrosine protein kinase p56lck
-
-
-
-
Tyrosine-protein kinase brk
-
-
-
-
Tyrosine-protein kinase CTK
-
-
-
-
Tyrosine-protein kinase Lyk
-
-
-
-
Tyrosine-protein kinase TYRO 10
-
-
-
-
Tyrosine-specific protein kinase
-
-
-
-
Tyrosylprotein kinase
-
-
-
-
v-fps Protein-tyrosine kinase
-
-
-
-
WEE1hu
-
-
-
-
YES related kinase
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
114051-78-4
p56lck protein kinase
80449-02-1
protein-tyrosine kinase
9026-43-1
this CAS Reg. No. encompasses a great variety of protein kinases including the serine/threonine specific kinases
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Abelson leukaemia virus
-
-
-
Manually annotated by BRENDA team
Avian erythroblastosis virus S13
strain S13
SwissProt
Manually annotated by BRENDA team
strain PR2257
SwissProt
Manually annotated by BRENDA team
strain PRCII
SwissProt
Manually annotated by BRENDA team
strain S1
SwissProt
Manually annotated by BRENDA team
strain S2
SwissProt
Manually annotated by BRENDA team
strain UR2
SwissProt
Manually annotated by BRENDA team
strain Y73
SwissProt
Manually annotated by BRENDA team
strain PR2257
SwissProt
Manually annotated by BRENDA team
strain PRCII
SwissProt
Manually annotated by BRENDA team
strain S1
SwissProt
Manually annotated by BRENDA team
strain S2
SwissProt
Manually annotated by BRENDA team
Avian sarcoma virus UR2
strain UR2
SwissProt
Manually annotated by BRENDA team
Avian sarcoma virus Y73
strain Y73
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
zebrafish
SwissProt
Manually annotated by BRENDA team
genes wzc and etk
-
-
Manually annotated by BRENDA team
strain Gardner-Arnstein
SwissProt
Manually annotated by BRENDA team
strain Gardner-Rasheed
SwissProt
Manually annotated by BRENDA team
strain Hardy-Zuckerman 2
SwissProt
Manually annotated by BRENDA team
strain McDonough
SwissProt
Manually annotated by BRENDA team
strain Snyder-Theilen
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus Gardner-Arnstein
strain Gardner-Arnstein
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus Gardner-Rasheed
strain Gardner-Rasheed
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus Hardy-Zuckerman 2
strain Hardy-Zuckerman 2
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus McDonough
strain McDonough
SwissProt
Manually annotated by BRENDA team
Feline sarcoma virus Snyder-Theilen
strain Snyder-Theilen
SwissProt
Manually annotated by BRENDA team
ssp. catus
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
12-year old female
-
-
Manually annotated by BRENDA team
ABL1; patients with chronic myeloid leukemia
SwissProt
Manually annotated by BRENDA team
ACK1
UniProt
Manually annotated by BRENDA team
c-Abl, two splice variants, one c-Abl 1b that is N-terminally myristoylated, and another that is 19 residues shorter at the N-terminus and not known to be myristoylated
-
-
Manually annotated by BRENDA team
FER
SwissProt
Manually annotated by BRENDA team
gene c-fps/fes, the feline sarcoma oncogene
SwissProt
Manually annotated by BRENDA team
JAK1 and JAK2
-
-
Manually annotated by BRENDA team
Jak2
SwissProt
Manually annotated by BRENDA team
Mexican patients with X-linked agammaglobulinemia
-
-
Manually annotated by BRENDA team
reference sequence for mutated Btk genes
SwissProt
Manually annotated by BRENDA team
SRC
SwissProt
Manually annotated by BRENDA team
YES1
SwissProt
Manually annotated by BRENDA team
strain HT-1, overproduced in Escherichia coli under the control of phage lambda promoter
SwissProt
Manually annotated by BRENDA team
Moloney murine sarcoma virus HT-1
strain HT-1, overproduced in Escherichia coli under the control of phage lambda promoter
SwissProt
Manually annotated by BRENDA team
Moloney murine sarcoma virus M1
strain M1
SwissProt
Manually annotated by BRENDA team
Moloney murine sarcoma virus MuSVts110
MuSVts110
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
Btk
SwissProt
Manually annotated by BRENDA team
C57BL/6 mice
-
-
Manually annotated by BRENDA team
female and male Swiss albino mice
-
-
Manually annotated by BRENDA team
hybrid C57BL6J/129Sv
-
-
Manually annotated by BRENDA team
Jak2
SwissProt
Manually annotated by BRENDA team
Mus musculus C57BL/6
C57BL/6 mice
-
-
Manually annotated by BRENDA team
Mus musculus C57BL6J/129Sv
hybrid C57BL6J/129Sv
-
-
Manually annotated by BRENDA team
New Zealand white rabbits
-
-
Manually annotated by BRENDA team
strain PAO1 and strain ATCC 27853
-
-
Manually annotated by BRENDA team
male sprague-dawley rats
-
-
Manually annotated by BRENDA team
male Wistar rats
SwissProt
Manually annotated by BRENDA team
Sprague-Dawley rats
-
-
Manually annotated by BRENDA team
Wistar rat
-
-
Manually annotated by BRENDA team
Wistar rat
SwissProt
Manually annotated by BRENDA team
strain H-19
SwissProt
Manually annotated by BRENDA team
strain Prague C
SwissProt
Manually annotated by BRENDA team
Rous sarcoma virus H-19
strain H-19
SwissProt
Manually annotated by BRENDA team
Rous sarcoma virus Prague C
strain Prague C
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
deficiency of Jak3 or Tyk2 results in defined clinical disorders, a striking phenotype associated with inactivating Jak3 mutations is severe combined immunodeficiency syndrome, whereas mutation of Tyk2 results in autosomal recessive hyperimmunoglobulin E syndrome, complete deletion of Jak1 or Jak2 in the mouse are not compatible with life and do not have counterparts in human disease. Activating mutations of each of the Jaks are found in association with malignant transformation, the most common being gain-of-function mutations of Jak2 in polycythemia vera and other myeloproliferative disorders.
malfunction
-
deficiency of Jak3 or Tyk2 results in defined clinical disorders, a striking phenotype associated with inactivating Jak3 mutations is severe combined immunodeficiency syndrome, whereas mutation of Tyk2 results in autosomal recessive hyperimmunoglobulin E syndrome, complete deletion of Jak1 or Jak2 in the mouse are not compatible with life and do not have counterparts in human disease. Activating mutations of each of the Jaks are found in association with malignant transformation, the most common being gain-of-function mutations of Jak2 in polycythemia vera and other myeloproliferative disorders. Jak1 knockout mice have major deficits in lymphopoiesis and a failure to respond to signals from class II cytokine receptors, gammac cytokine receptors, and cytokine receptors that contain the gp130 subunit. Jak2 deficiency is lethal.
malfunction
-
mutations of JAK3 may be a cause of severe combined immunodeficiency
malfunction
-
mutations of JAK3 may be a cause of severe combined immunodeficiency, JAK3 knockout mice have a profound reduction in thymic progenitor cells and reduced ability to reconstitute T cell development, in the periphery, CD8+ T and NK cells are severely reduced. JAK3- (and gamma chain) deficient mice also have severely defective B cell development, deficiency of JAK1 and JAK2 is lethal
malfunction
-
only 75% of ABL1 knockout mice survive the first week,33 the remaining animals show severe defects in spermatogenesis, thymic and splenic atrophy, susceptibility to infections and reductions of T- and B-cell lymphocytes and their early precursors in lymphoid organs
physiological function
-
ABL1 binds to the actin cytoskeleton and is involved in cytoskeletal organization, non-erythroid myelopoiesis and regulation of small GTPases, in response to genotoxic stress such as DNA damage or the increase of reactive oxygen species, ABL1 is translocated into the nucleus where its activity contributes to induction of apoptosis and inhibition of cell growth
physiological function
O60674
constitutive JAK activation leads to persistent activation of STAT transcription factors, and several cancers exhibit constitutive STAT activation, in the absence of JAK or STAT activating mutations
physiological function
-
crucial for cytokine receptor signaling in blood formation and immune responses
physiological function
-
JAK-STAT signaling is required for germline stem cell and cyst progenitor cells maintenance in testis
physiological function
-
JAK1 and JAK2 activate c-Myc promoter in interleukin 5 signaling
physiological function
-
JAK3 associates with the common gamma chain cytokine receptor, Tyk2 is involved in signaling by type I interferons, interleukin-12 and interleukin-23
physiological function
-
conditional knockout of isoform c-Abl in the nervous system prevents the phosphorylation of substrate parkin, the accumulation of parkin substrates aminoacyl-tRNA synthetase-interacting multifunctional protein type 2, AIMP2, and fuse-binding protein 1, FBP, and subsequent neurotoxicity in response to 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine intoxication
physiological function
P07947
in HT29 colon carcinoma cells, silencing of tyrosine kinase c-Yes, but not of kinase c-Src, selectively leads to an increase of cell clustering associated with a localisation of beta-catenin at cell membranes and a reduction of expression of beta-catenin target genes. c-Yes silencing induces an increase in apoptosis, inhibition of growth in soft-agar and in mouse xenografts, inhibition of cell migration and loss of the capacity to generate liver metastases in mice. Reintroduction of c-Yes, but not c -Src, restores transforming properties of c-Yes depleted cells. c-Yes kinase activity is required for its role in beta-catenin localisation and growth in soft agar, whereas kinase activity is dispensable for its role in cell migration. c-Yes regulates specific oncogenic signalling pathways important for colon cancer progression that are not shared with c-Src
physiological function
Q07912
interaction of the Src homology 3 domain SH3 with the epidermal growth factor receptor-binding domain in isoform ACK1 leads to auto-inhibition of the kinase activity. Release of this auto-inhibition is a key step for activation of ACK1. Mutation of the SH3 domain causes activation of ACK1, independent of cell adhesion. A region at the N-terminus of ACK1, Leu10-Leu14, is essential for cell adhesion-mediated activation. In the activation of ACK1 by epidermal growth factor receptor signalling, growth-factor-receptor-bound protein Grb2 mediates the interaction of ACK1 with epidermal growth factor receptor through binding to the epidermal growth factor receptor-binding domain and activates ACK1 by releasing the auto-inhibition
physiological function
-
isoform c-Abl kinase is required for neutrophil recruitment in vivo and migration in vitro, and the inhibition of c-Abl kinase activity has a significant impact on neutrophil migratory behavior. c-Abl kinase activation depends on 2 integrin engagement, and the activated c-Abl kinase further regulates actin polymerization and membrane protrusion dynamics at the extended leading edges during neutrophil migration. The Rho guanine exchange factor Vav1 is a major downstream effector of c-Abl kinase. The C-terminal SH3-SH2-SH3 domain and proline-rich region of Vav1 are required for its interaction with c-Abl kinase, and c-Abl kinase probably regulates the activity of Vav1 by direct phosphorylation at Tyr-267 in the Dbl homology domain
physiological function
-
lymphocyte-specific protein tyrosine kinase LCK is involved in the fractionated radiation-induced expansion of the glioma-initiating cell population and acquisition of resistance to anticancer treatments. Fractionated radiation causes a selective increase in the activity of LCK. The activities of other Src family kinases Src, Fyn, and Lyn are not significantly increased. Knockdown of LCK expression with siRNA effectively block fractionated radiation-induced expansion of the CD133+ cell population. siRNA targeting of LCK also suppresses fractionated radiation-induced expression of the glioma stem cell marker proteins CD133, Nestin, and Musashi. Expression of the proteins Notch2 and Sox2 in glioma cells treated with fractionated radiation is also downregulated by LCK inhibition. siRNA-mediated knockdown of LCK effectively restores the sensitivity of glioma cells to cisplatin and etoposide
physiological function
P35991
murine Btk-/- natural killer cells have decreased innate immune responses to the toll-like receptor TLR3 ligand, with reduced expressions of IFN-gamma, perforin, and granzyme-B and decreased cytotoxic activity. Isoform Btk promotes TLR3-triggered natural killer cell activation mainly by activating the NF-kappaB pathway. Poly(I:C)-induced natural killer cell-mediated acute hepatitis is attenuated in Btk-/- mice or the mice with in vivo administration of Btk inhibitor. Correspondingly, liver damage is aggravated in Btk-/- mice after the adoptive transfer of Btk-/- natural killer cells
physiological function
P16591
non-receptor tyrosine kinase Fer is able to phosphorylate RhoGDIalpha, regulator of the small GTPase Rac, and form a direct protein complex with it. This interaction is mediated by the C-terminal end of RhoGDIalpha. Tyrosine phosphorylation of RhoGDIalpha by Fer prevents subsequent binding of Rac to RhoGDIalpha, but once a RhoGDIalpha-Rac complex is formed, the Fer kinase is not able to cause Rac release through tyrosine phosphorylation of preformed RhoGDIalpha-Rac complexes
physiological function
-
Notch-1-Furin interaction is regulated by the non-receptor tyrosine kinase, c-Src. c-Src and Notch-1 are physically associated, and this association is responsible for Notch-1 processing and activation. Growth factor TGF-alpha, an epidermal growth factor receptor ligand, and PDGF-BB, a platelet derived growth factor receptor ligand, induce the Notch-1-Furin interaction mediated by c-Src. The association between Notch-1 and Furin is a well-regulated process, extracellular growth factor signals regulate this interaction, which is mediated by c-Src, and there is cross-talk between the plasma growth factor receptor-c-Src and Notch pathways
physiological function
-
selective Src-kinase inhibitors 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine and 4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine, at 5 microM, attenuate acetylcholine-induced ionic currents and intracellular Ca2+ ion concentration transients in major pelvic ganglion neurons. Blocking the tyrosine kinase activity of Src kinase by pp60 c-src inhibitory peptide also reduces the acetylcholine-induced currents. Sodium orthovanadate, at 200 microM, a tyrosine phosphatase inhibitor, significantly augments the acetylcholine-induced currents
physiological function
-
specific pharmacological inhibition and genetic silencing indicate the involvement of isoform Lck in the regulation of neuritic outgrowth. Specific Lck inhibition also selectively impairs the long-term hippocampal synaptic plasticity without affecting spontaneous excitatory synaptic transmission or short-term synaptic potentiation and significantly alters hippocampus-dependent spatial learning and memory in vivo
physiological function
-
Src family kinases are important for a balanced production of inflammatory cytokines by human monocyte-derived dendritic cells upon stimulation of toll-like receptors TLR3 and TLR8 with their respective agonists. Disruption of this equilibrium through pharmacological inhibition of Src kinases alters the dendritic cell maturation pattern. While expression of interleukin IL-12 and other inflammatory cytokines depends on Src kinases, the induction of IL-23 and co-stimulatory molecules does not. Dendritic cells treated with Src inhibitors are not compromised in their ability to induce CD4 T cell proliferation and to promote the T helper cell Th17 subset survival but are less efficient in inducing T helper cell Th1 differentiation
physiological function
-
Src family tyrosine kinase activation is a required step in non-capacitative cation entry activation. Application of specific inhibitor 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine completely abolishes thrombin-induced non-capacitative cation entry into platelets, a Ca2+ entry pathway that is independent of Ca2+ store depletion
physiological function
Q9WUD9
Src kinase plays an important role in angiotensin II-elicited protein kinase C zeta activation and the subsequent downstream signaling including ERK1/2 activation and vascular smooth muscle cell proliferation. Angiotensin II induces rapid activation of protein kinase C zeta, which is associated with its phosphorylation and nuclear translocation. angiotensin II not only induces activation by Src, but also promotes the physical association between Src and protein kinase C zeta, which is abolished by Src inhibition with inhibitor 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine. Src inhibition also abrogates angiotensin II-stimulated protein kinase C zeta activation, ERK1/2 phosphorylation and vascular smooth muscle cell proliferation
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
AEEEIYGEFEAKKKK + ATP
? + 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
-
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
phosphorylates tyrosine, serine and threonine
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O70146
serine-threonine kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme plays an important role in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
ILK is a receptor-proximal protein kinase regulating integrin-mediated signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme is upregulated in HT-144 melanoma cells following TGF-beta1 stimulation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q13418
ILK is involved in agonist stimulated, Pi(3)K-dependent, PKB/AKT activation. ILK is thus a receptor-proximal effector for the Pi(3)K-dependent, extracellular matrix and growth factor mediated, activation of PKB/AKT, and inhibition of GSK-3
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
the enzyme controls shoot and floral meristem size
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme contributes to signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q15569
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q63572
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
P53666
it is likely that LIMK is involved in developmental or oncogenic processes through interactions with these LIM-containing proteins
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q924U5
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q96S53
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O70146
role for this kinase in spermatogenesis
-
-
-
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O43187
proximal mediators of IL-1 signaling
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q9Y572
apoptosis-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O43353
NF-kappaB-activating and cell death-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
the enzyme is a downstream effector of activated Ras. Interaction with Ras leads to Raf-1 activation and results in transduction of cell growth and differentiation signals
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme functions as an intermediary in TNFalpha-induced apoptosis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme is required in early larval development
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
P10398
enzyme plays a critical role in cell growth and development
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
PhK phosphorylates e.g. the protein substrate GPb, v-Fps phosphorylates e.g. the peptide substrate EAEIYEAEI, Csk phosphorylates e.g. the substrate poly-Glu4-Tyr
-
-
?
ATP + a [peptide]-L-tyrosine
ADP + a [peptide]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
O60674
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
activation of Syk is responsible for K-Cl cotransport in SS cells by relieving Src-mediated inhibition of the transporter
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
enzymes of the Tec tyrosine kinase family phosphorylate themselves or other family members
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
substrate docking-site and binding structure of Src involving R279, R281, and R283
-
-
?
ATP + A-kinase anchor protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells, Abl is also required for Src-induced transformation of mouse fibroblasts, overview
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is a substrate of Src
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is a substrate of Src, phosphorylation on Tyr245 and Tyr412
-
-
?
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
show the reaction diagram
-
tyrosine kinase Akt is phosphorylated by PYK2 for activation of the Akt signaling pathway, overview
-
-
?
ATP + arsenate resistance protein ARS2
?
show the reaction diagram
-
-
-
-
?
ATP + ataxin 2 related protein
?
show the reaction diagram
-
-
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + Bcl-2-associated transcription factor 1
?
show the reaction diagram
-
-
-
-
?
ATP + beta 1-integrin cytoplasmic domain peptide
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + biotin-GGEAIYAAPFKK-amide
ADP + phosphorylated biotin-GGEAIYAAPFKK-amide
show the reaction diagram
-
a peptide with the preferred c-Abl substrate sequence carrying an Nterminal biotin
-
-
?
ATP + c-Src
?
show the reaction diagram
-
-
-
-
?
ATP + calponin 3
?
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + casein
ADP + phosphocasein
show the reaction diagram
-
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + Cbp
? + ADP
show the reaction diagram
-
murine Csk binding protein, Cbp, amino acids 74-474, substrate used in kinase activity assay
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
show the reaction diagram
-
-
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
show the reaction diagram
P47817
phosphorylated exclusively on Y15
-
?
ATP + cdc2
ADP + phosphorylated cdc2
show the reaction diagram
-
the Cdc2-inhibitory kinase is required for preventing premature activation of the mitotic program. Maternally provided Dwee1 is sufficient for regulating Cdc2 during embryogenesis
-
-
?
ATP + cdc2(6-20) peptide
?
show the reaction diagram
-
i.e. KVEKIGEGTYGVVYK, substrate of Src family kinases
-
-
?
ATP + chromosome 20 open reading frame 77
?
show the reaction diagram
-
-
-
-
?
ATP + cleavage and polyadenylation specific factor 5
?
show the reaction diagram
-
-
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
show the reaction diagram
Q924U5
phosphorylation specifically at Ser-3
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
show the reaction diagram
Q96S53
phosphorylation specifically at Ser-3
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cortactin
?
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
P30291
phosphorylated on Y15, Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + EEEEY
ADP + EEEE(phospho)Y
show the reaction diagram
-
-
-
-
?
ATP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
ADP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G phosphate
show the reaction diagram
-
Y7 Sox-based substrate, kinetic assay
-
-
?
ATP + EEEPQYEEIPI +
ADP + EEEPQpYEEIPI
show the reaction diagram
-
-
-
-
?
ATP + enolase
ADP + ?
show the reaction diagram
-
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability, activated Abl phosphorylates the EGFR primarily on Tyr1173, no activity with the Tyr1173 mutant substrate
-
-
?
ATP + EQEDEPEGDYFEWLE
ADP + EQEDEPEGDpYFEWLE
show the reaction diagram
-
-
-
-
?
ATP + eukaryotic translation initiation factor 3, subunit 4
?
show the reaction diagram
-
-
-
-
?
ATP + ewing sarcoma breakpoint region 1
?
show the reaction diagram
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + F peptide
ADP + phospho-L-tyrosinyl-F peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIFGEI-NH2
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + FUS interacting protein (serine/arginine rich) 1
?
show the reaction diagram
-
-
-
-
?
ATP + FUS/TLS oncogene
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein 2
?
show the reaction diagram
-
-
-
-
?
ATP + GAPEVIYATPGAKKK
ADP + GAPEVI-phosphotyrosinyl-ATPGAKKK
show the reaction diagram
-
consensus substrate
-
-
?
ATP + GGEAIYAAPFKK
ADP + GGEAIYAAPFKK phosphate
show the reaction diagram
-
kinase assay using biotinylated model substrate peptide
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein A3
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein AB
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein D-like
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein K
?
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
P53671
serine/threonine-specific kinase activity
-
-
?
ATP + homeobox prox 1
?
show the reaction diagram
-
-
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role, Lck interacts via its SH2 domain with tyrosine-phosphorylated IkappaBalpha
-
-
?
ATP + KVEKIGEGTYGVVYK
ADP + ?
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + KVEKIGEGTYGVVYK
? + ADP
show the reaction diagram
-
substrate peptide used in kinase activity assay, derived from p34cdc2
-
-
?
ATP + lysozyme-L-tyrosine
ADP + lysozyme-L-tyrosine phosphate
show the reaction diagram
-
substrate of Src, low activity with Csk or Chk
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
Q15569
serine/threonine kinase activity
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
P53671
serine/threonine-specific kinase activity
-
-
?
ATP + myelin basic protein
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + myosin light chain
ADP + ?
show the reaction diagram
-
serine/threonine kinase activity, and no tyrosine kinase activity
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + NEFA-interacting nuclear protein
?
show the reaction diagram
-
-
-
-
?
ATP + NICE-4
?
show the reaction diagram
-
-
-
-
?
ATP + P1 peptide
ADP + phospho-L-tyrosinyl-P1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIpYGEI-NH2
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
show the reaction diagram
-
p32 is a sperm protein
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
-
phosphorylated exclusively on Y15
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
-
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1, a serine-threonine kinase, phosphorylation at Y153, Y201, and Y285 activates PAK1, no activation of PAK1 mutants Y153F,Y201F,Y285F, mutational analysis of phosphorylation sites,overview
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + peptide
ADP + phospho-L-tyrosinyl-peptide
show the reaction diagram
-
PTKs phosphorylate substrates in a sequence-specific manner, relatively short peptide sequences determine selectivity, substrate specificity analysis using 144 different peptides, overview
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview, i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation at Y682 and Y774 by fyn, the kinase domain of activated fyn binds to the ArfGAP domain of PIKE-A, reduced activity with Y682F and with Y774F mutant PIKE-A, no activity with Y682F/Y774F mutant PIKE-A
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu,Tyr)
? + ADP
show the reaction diagram
-
substrate used in the tyrosine kinase asssay
-
-
?
ATP + poly(Glu-Tyr)
? + ADP
show the reaction diagram
-
substrate used in the activity assay
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu-Tyr)-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
show the reaction diagram
-
artificial substrate
-
-
?
ATP + poly-(Tyr-Glu)
ADP + phospho-poly-(Tyr-Glu)
show the reaction diagram
-
tyrosine kinase substrate, phosphoryated by Swe1p, Mps1p, Ime2p, and Hrr25p, but not by Ste7p, Rad53p, or Mck1p
-
-
?
ATP + proteasome activator subunit 3
?
show the reaction diagram
-
-
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
P41239
phosphorylates the regulatory C-terminal tyrosine residue present on cytoplasmic tyrosine kinases of the Src family
-
-
?
ATP + protein
?
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
protein kinase activity with specificity for tyrosine residues
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P32577
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain, specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + RasGAP SH3-domain binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + recombinant GST/beta3 integrin cytoplasmic tail peptide
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 10
?
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 4B
?
show the reaction diagram
-
-
-
-
?
ATP + S1 peptide
ADP + phospho-L-tyrosinyl-S1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIYGEI-NH2
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
show the reaction diagram
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
show the reaction diagram
-
-
-
-
?
ATP + similar to zinc finger CCCH-type domain-containing protein 6
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor proline/glutamine-rich
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor, arginine/serine-rich9
?
show the reaction diagram
-
-
-
-
?
ATP + Src
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
wild-type Src and catalytically inactive mutant Src K295M, terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site, Glu510 of Src interacts with Arg283 of Csk in Csk-Src recognition, activity with Src fragments, overview
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
P42679
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + STAT3
ADP + phospho-L-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth, physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, phosphorylation mainly at Tyr406, no activity with TCGAP Y406F mutant, recombinant substrate from mouse and human, overview
-
-
?
ATP + thyroid hormone receptor associated protein 3
?
show the reaction diagram
-
-
-
-
?
ATP + TRK-fused gene
?
show the reaction diagram
-
-
-
-
?
ATP + Tyr267 of Vav1
ADP + phosphorylated Tyr267 of Vav1
show the reaction diagram
-
-
isoform c-Abl kinase probably regulates the activity of Rho guanine exchange factor Vav1 by direct phosphorylation at Tyr267 in the Dbl homology domain. The C-terminal SH3-SH2-SH3 domain and proline-rich region of Vav1 are required for its interaction with c-Abl kinase
-
?
ATP + zinc finger, CCHC domain containing protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + [Abi1]-L-tyrosine
ADP + [Abi1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl phosphorylates Y213 of Abi1
-
-
?
ATP + [actin-stabilizing adapter protein HS1]-L-tyrosine
ADP + [actin-stabilizing adapter protein HS1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl binds to phospho-HS1 via its SH2 domains and is required for full tyrosine phosphorylation of HS1 during T-cell activation
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316, in vivo assay utilizing Hep-G2 cells or H4IIE cells expressing AhR and Src kinase
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
-
proto-oncogenic PTK protein substrate, activity and phosphorylation patterns of Syk, Fyn, and Abl with recombinant wild-type and mutant Y700F, Y731F, and Y774F c-Cbl proteins, phosphorylation site preferences are determined by interaction of the enzymes' SH2 domain with the substrate via p85, a phosphatidylinositol 3-kinase, overview
-
-
?
ATP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine
ADP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CAEEEIYGEFEA derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGKYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTFGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTpYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYFVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVEYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVFK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGKGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
show the reaction diagram
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
show the reaction diagram
Mus musculus C57BL6J/129Sv
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion, estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen receptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
show the reaction diagram
A1A5H8
activation of FAK during epiboly and gastrulation by dynamic phosphorylation at Tyr861
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2, activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2, activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain
-
-
?
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
show the reaction diagram
-
substrate HCN4, tyrosine 531 is phosphorylated
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. kinase-defective chicken Src mutant K295M
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. kinase-defective Src, substrate of Chk and Csk, inactivation mechanism of Src, overview
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein kinase C zeta]-L-tyrosine
ADP + [protein kinase C zeta]-L-tyrosine phosphate
show the reaction diagram
Q9WUD9
-
Src kinase plays an important role in angiotensin II-elicited protein kinase C zeta activation and the subsequent downstream signaling including ERK1/2 activation and vascular smooth muscle cell proliferation
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q35346
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
P58764
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q07014
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q06187
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q9WUD9
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q38KH2
-
-
-
?
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [tubulin]-L-tyrosine
ADP + [tubulin]-L-tyrosine phosphate
show the reaction diagram
-
highly active with c-Fes, which also catalyzes tubulin polymerization in vitro
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism, substrate of Lck, Fyn, and c-Abl
-
-
?
denatured enolase + ATP
phosphorylated denatured enolase + ADP
show the reaction diagram
-
-
-
-
?
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition, phosphorylation at Tyr31 and Tyr118 by Fak
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
-
phosphorylation by Jak2 at tyrosine residues
-
-
?
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery, phosphorylation by PYK2
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
P00522
-
-
-
-
additional information
?
-
P42679
-
-
-
-
additional information
?
-
-
JAK2 plays a central role in non-protein tyrosine kinase receptor signaling pathways
-
-
-
additional information
?
-
-
catalytic domain Src including the C-terminal tail autophosphorylates and efficiently phosphorylates substrate peptides and proteins. Autophosphorylation occurs by an intermolecular mechanism
-
-
-
additional information
?
-
-
p60src, the transforming protein of Rous sarcoma virus, is a protein kinase that has a strict specificity for Tyr. The phosphorylation of cellular proteins by p60src results in transformation
-
-
-
additional information
?
-
-
interaction of the Fyn SH3 domain with the p85 subunit of PI3-kinase
-
-
-
additional information
?
-
Q9U5Y2
in vitro autophosphorylation activity at tyrosine residues
-
-
-
additional information
?
-
P10741
transforms NIH 3T3 cells
-
-
-
additional information
?
-
P27040
all isoforms of the activin receptor type II bind inhibin A with low affinity
-
-
-
additional information
?
-
P07331
p40mos binds ATP analog p-fluorosulfonylbenzoyladenosine and exhibits ATPase activity
-
-
-
additional information
?
-
-
the bone morphogenetic protein receptor binds bone morphogenetic protein 2 and bone morphogenetic protein 4
-
-
-
additional information
?
-
Q9QZl0
activates NF-kappaB
-
-
-
additional information
?
-
-
activates NF-kappaB
-
-
-
additional information
?
-
-
PTK6 may function as an intracellular signal transducer in specific tissues
-
-
-
additional information
?
-
Q62137
role for JAK3 in hematopoiesis and T- and B-cell development
-
-
-
additional information
?
-
-
transcriptionally induced in normal T cells by interleukin 2 stimulation, roles in T cell proliferation and differentiation
-
-
-
additional information
?
-
-
involvement of the Jak-3 Janus kinase in signalling by interleukins 2 and 4 in lymphoid and myeloid cells
-
-
-
additional information
?
-
-
JAK3 kinase is associated with terminal differentiation of hematopoietic cells
-
-
-
additional information
?
-
-
sensitizes mammary epithelial cells to epidermal growth factor
-
-
-
additional information
?
-
Q24592
required maternally for the establishment of the normal array of embryonic segments
-
-
-
additional information
?
-
Q9U5Y2
plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
-
-
-
additional information
?
-
-
is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
-
-
-
additional information
?
-
P34152
the enzyme transduces signals initiated by integrin engagement and G protein-coupled receptors. Several splice isoforms of FAK are preferentially expressed in rat brain, some of which have an increased autophosphorylation activity
-
-
-
additional information
?
-
-
activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
-
-
-
additional information
?
-
Q91738
participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
-
-
-
additional information
?
-
P00541
oncogene v-fps induces fibrosarcomas in birds
-
-
-
additional information
?
-
-
associated with breast cancer and osteoporosis
-
-
-
additional information
?
-
-
mutations in the gene encoding the Drosophila tyrosine kinase Abelson substantially enhanced the severity of the CNS phenotype of armadillo mutations, consistent with these proteins functioning co-operatively at adherens junctions in both the CNS and the epidermis
-
-
-
additional information
?
-
-
enzyme plays a critical role in a variety of signal transduction pathways
-
-
-
additional information
?
-
-
lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes, enzyme is implicated in neoplastic transformation
-
-
-
additional information
?
-
-
enzyme is involved in pathway for signaling through glycosyl-phosphatidylinositol (GPI)-anchored membrane proteins
-
-
-
additional information
?
-
-
involved in signal transduction by association with a number of membrane receptors
-
-
-
additional information
?
-
-
elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
-
-
-
additional information
?
-
-
p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
-
-
-
additional information
?
-
P06240
p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
-
-
-
additional information
?
-
P10936
yes gene product is likely to play an important role in oogenesis or early development
-
-
-
additional information
?
-
-
enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
-
-
-
additional information
?
-
-
Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
-
-
-
additional information
?
-
-
participates in signal transduction events regulating the growth, differentiation and function of phagocytes
-
-
-
additional information
?
-
P16591
it may be involved in key regulatory processes
-
-
-
additional information
?
-
-
may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
-
-
-
additional information
?
-
-
may interact with the intracellular domain of cell surface receptors
-
-
-
additional information
?
-
-
participates in the signalling pathways of a broad range of cytokines
-
-
-
additional information
?
-
-
enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
-
-
-
additional information
?
-
P27446, P27447
possible function during secondary steps of tumor progression
-
-
-
additional information
?
-
-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
-
-
-
additional information
?
-
P32577
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain. Specifically phosphorylates a negative regulatory site of p60c-src
-
-
-
additional information
?
-
-
deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia
-
-
-
additional information
?
-
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
-
-
-
additional information
?
-
-
CSK is involved in regulation of src family kinases
-
-
-
additional information
?
-
P43403
ZAP-70 that associates with T cell antigen receptor zeta chain and undergoes tyrosine phosphorylation following TCR stimulation
-
-
-
additional information
?
-
-
tandem ZAP-70 SH2 domains bind phosphorylated, but not nonphosphorylated, T cell antigen receptor zeta cyt. The NH2-terminal ZAP-70 SH2 domain also binds to T cell antigen receptor zeta cyt but with 100-fold lower affinity. No binding is observed with the COOH-terminal ZAP-70 SH2 domain. Similar studies demonstrate that the ZAP-70 tandem SH2 domain can bind a T cell antigen receptor zeta 3 TAM peptide in which both tyrosine residues are phosphorylated: Little or no binding is observed with peptides phosphorylated at only one tyrosine residue, or a nonphosphorylated peptide. Binding of the tandem SH2 domains to the other two TCR zeta TAM peptides and to a CD3 epsilon TAM peptide is also observed. All four doubly tyrosine phosphorylated TAM peptides cross-compete with each other for binding to the tandem SH2 domains of ZAP-70. The affinity of these peptides for the tandem SH2 construct demonstrates a hierarchy of TAM zeta 1, TAM zeta 2, TAM epsilon, TAM zeta 3
-
-
-
additional information
?
-
-
perinatal lethality and blocked B-cell development in mice lacking the tyrosine kinase Syk. Syk-deficient radiation chimaeras fail to accumulate mature B cells, Syk-deficient mice show impaired development of thymocytes using the V gamma 3 variable region gene, Syk is not required for signalling through the IL-2 and G-CSF receptors
-
-
-
additional information
?
-
-
mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency
-
-
-
additional information
?
-
-
Rlk has potential functions in intrathymic T cell development and mature T cell signaling
-
-
-
additional information
?
-
P52333
JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: persistence of genetically and biochemically defective autologous B cells, associated with reconstitution of cellular and humoral immunity, suggests that integrity of the gammac-JAK3 signalling pathway is not strictly required for immunoglobulin production
-
-
-
additional information
?
-
-
JAK3 deficiency in humans results in autosomal recessive T-B+ severe combined immunodeficiency disease
-
-
-
additional information
?
-
-
HYL plays a significant role in the signal transduction of hematopoietic cells
-
-
-
additional information
?
-
-
enzyme plays a pivotal role in cell signal transduction
-
-
-
additional information
?
-
-
Ntk may play an inhibitory role in the control of T-cell proliferation
-
-
-
additional information
?
-
-
may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
-
-
-
additional information
?
-
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
-
-
-
additional information
?
-
P51813
effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells
-
-
-
additional information
?
-
-
autosomal recessive form of severe combined immunodeficiency disease in which ZAP-70 is absent as a result of mutations in the ZAP-70 gene. This absence is associated with defects in TCR signal transduction. Integral role in T cell activation and differentiation
-
-
-
additional information
?
-
-
may play a role in the growth and differentiation of hematopoietic cells
-
-
-
additional information
?
-
P42685
may have a role in human cancer
-
-
-
additional information
?
-
P41243
Batk may function as a brain-specific regulator of kinases involved in the development and maintenance of the nervous system
-
-
-
additional information
?
-
-
JAK3 splice isoforms are functional in JAK3 signaling and may enrich the complexity of the intracellular response functional in IL-2 or cytokine signaling
-
-
-
additional information
?
-
P43404
activating motif occurs in four discrete steps: binding of p59fyn, phosphorylation of the motif, binding of ZAP-70, and activation of ZAP-70 kinase activity
-
-
-
additional information
?
-
-
Ctk is involved in the regulation of neural function and differentiation of male germ cells through interactions with members of the Src family kinases
-
-
-
additional information
?
-
-
mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
-
-
-
additional information
?
-
Q04736
could be responsible for the tyrosine phosphorylation observed in a murine thymic medullary epithelial cell line E-5 following complex formation with thymocytes
-
-
-
additional information
?
-
Q07014
appear to play a role in B-cell-IgM and FcERI receptor signaling
-
-
-
additional information
?
-
-
functions during reinitiation of meiotic division
-
-
-
additional information
?
-
-
TGF-beta RII expression is down-regulated in cells treated with exogenous TGF-beta1
-
-
-
additional information
?
-
-
type II receptor isoforma exist which play preferential binding to TGF-beta2 and have their own defined role in debvelopment
-
-
-
additional information
?
-
P12965
the kinase induces progression through the cell cycle for both meiotic and mitotic cells
-
-
-
additional information
?
-
-
the receptor shares two-hit inactivation mechanism with tumor suppressor genes and mutation of it may occur in the early stage of tumorgenesis
-
-
-
additional information
?
-
-
mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2
-
-
-
additional information
?
-
P27037
activin and its receptor play an important role in development
-
-
-
additional information
?
-
P37023
the activin receptor-like kinase 1 gene is the second locus for the autosomal dominant vascular disease hereditary hemorrhagic telangiectasia
-
-
-
additional information
?
-
-
signal transduction by TGF bet involves the formation of a heteromeric complex of two different serine/threonine kinase receptors
-
-
-
additional information
?
-
P27041
involved in signal transduction
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-
additional information
?
-
-
insensitivity to anti-mullerian hormone is due to a mutation in the human anti-mullerian hormone receptor
-
-
-
additional information
?
-
P36897
transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
-
-
-
additional information
?
-
P50488
the receptor controls dauer larva development
-
-
-
additional information
?
-
P27039
importance of the function of activin receptor in the regulatory mechanism for body axis formation
-
-
-
additional information
?
-
Q09488
enzyme is involved in TGFbeta signaling
-
-
-
additional information
?
-
Q95126
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
-
additional information
?
-
P36894
enzyme is involved in bone morphogenetic protein signaling
-
-
-
additional information
?
-
Q62893
mullerian inhibiting substance causes regression of the fetal Mullerian duct on binding a heteromeric complex of types I and II cell-surface receptors in the fetal urogenital ridge. The anti-mullerian hormone type II receptor provides specificity for mullerian inhibiting substance
-
-
-
additional information
?
-
P20792
cell-surface receptor required for transduction of environmental signals into an appropriate developmental response, controls dauer larva development
-
-
-
additional information
?
-
Q9QZl0
mRIP3 uses a novel mechanism to induce death
-
-
-
additional information
?
-
O43353
RIP2 interacts with members of the TNFR-1 signaling complex, including inhibitor of apoptosis protein cIAP1 and with members of the TNFR-associated factor family, specifically TRAF1, TRAF5, and TRAF6, but not with TRAF2, TRAF3, or TRAF4
-
-
-
additional information
?
-
-
CARDIAK may be involved in NF-kappa B/JNK signaling and in the generation of the proinflammatory cytokine IL-1 beta through activation of caspase-1
-
-
-
additional information
?
-
-
in a cell cycle the wee1 kinase is phosphorylated at M-phase, phosphorylation occurs in the N-terminal domain resulting in inactivation of the kinase activity. The N-terminal domain, or the entire molecule is extensively phosphorylated by cdc2-cyclin B kinase
-
-
-
additional information
?
-
-
blocks cell division when overexpressed in Hela cells
-
-
-
additional information
?
-
P30291
activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
-
-
-
additional information
?
-
P47817
down-regulation of Wee1-like kinase activity by phosphorylation at mitosis is a multistep process that occurs after other biochemical reactions have signaled the successful completion of S phase
-
-
-
additional information
?
-
-
active c-Fes tyrosine kinase binds tubulin and microtubules through separate domains and promotes microtubule assembly, c-Fes colocalization with microtubules in vivo requires the SH2 enzyme domain, implication in the differentiation of vascular, endothelial, myeloid, hematopoietic, and neuronal cells, overview
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-
-
additional information
?
-
-
ALK-MYH9 performs tyrosine autophosphorylation in vivo, but not in vitro, possible mechanism
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-
-
additional information
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
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-
-
additional information
?
-
-
CX3CL1, i.e. fractalkine, only member of the delta subclass of chemokines, triggers PTK Syk activity in monocytes/macrophages localized in F-actin-enriched cell protrusions, which are formed due to CX3CL1 treatment and subsequent increase in F-actin, Syk deficiency results in strong impairment of RAW cell migration to CX3CL1, overview
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-
-
additional information
?
-
-
enzyme is involved in cell growth, differentiation, and apoptosis
-
-
-
additional information
?
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-
Fes tyrosine kinase promotes survival and terminal granulocyte differentiation of factor-dependent myeloid progenitors (32D) and activates lineage-specific transcription factors, e.g. CCAAT/enhancer-binding protein-alpha and STAT3, down-regulation of macrophage marker F4/80
-
-
-
additional information
?
-
-
Fps/Fes and Fer protein-tyrosine kinases play redundant roles in regulating hematopoiesis
-
-
-
additional information
?
-
-
Fps/Fes tyrosine kinase is involved in regulation of erythropoiesis and of myeloid differentiation and survival
-
-
-
additional information
?
-
-
IP3 production in the hypersensitive response of lemon seedlings against Alternaria alternata involves active protein tyrosine kinases but not a G-protein, overview
-
-
-
additional information
?
-
-
JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases
-
-
-
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, overview
-
-
-
additional information
?
-
-
protein tyrosine kinase-dependent modulation of voltage-dependent potassium channels by genistein in cardiac ventricular myocytes
-
-
-
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, BCR/ABL and several other constitutive protein tyrosine kinases are activated in myeloid malignancies, overview, protein deregulation probable due to fusion gene formation because of chromosomal translocations or as distinct gain-of-function point mutations, autophosporylation of BCR/ABL kinase at Tyr177 is essential for myeloid leukomogenesis in vivo, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
-
-
-
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
-
-
-
additional information
?
-
-
protein tyrosine kinases play a critical role in the modulation of a wide range of cellular events such as cell division, cell differentiation, and cell metabolism, over-stimulation of PTKs impairs normal cell growth, resulting in oncogenic transformation, regulation of enzyme activity occurs in dynamic oscillatory behaviour, patterns and mechanism, overview
-
-
-
additional information
?
-
-
PTKs are involved in cell signalling
-
-
-
additional information
?
-
-
spleen tyrosine kinase Syk modulates epidermal growth factor receptor EGFR signalling in mammary epithelial cells acting as a negative controle element, regulation of EGFR by activation of the autophosphorylation activity of EGFR, but not of HER2 and HER3, overview
-
-
-
additional information
?
-
-
Src activates an outwardly rectifying chloride current in myocytes being involved in osmotic swelling, enzyme inhibition also inhibits stretch-activated Cl- current, mechanism, overview
-
-
-
additional information
?
-
-
Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
-
-
-
additional information
?
-
-
Src family kinases Hck, Fyn and Src are constitutively expressed and are required for murine embryonic stem cell growth and differentiation, regulation of SFKs in response to leukemia inhibitory factor LIF and other growth factors, overview
-
-
-
additional information
?
-
-
Src-dependent outside-in signalling is a key step in the process of autoregulation of beta2 integrins in polymorphonuclear cells and required for adhesion of interleukin-8, Src PTKs are required for macrophage antigen-1-mediated adhesion, which is inhibited by cytochalasin D and involved F-actin and protein P-110, overview
-
-
-
additional information
?
-
-
Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development
-
-
-
additional information
?
-
-
Syk kinase is involved in cell motility and activation of phosphatidylinositol 3'-kinase, Syk kinase inhibits the tyrosine phosphorylation of IkappaBalpha and thus inhibits activation of NFkappaB via interaction of IkappaBalpha and phosphatidylinositol 3'-kinase, pathway regulation, overview
-
-
-
additional information
?
-
-
Tec family tyrosine kinases play a central role in hematopoietic cellular signaling
-
-
-
additional information
?
-
-
the enzyme is involved in regulation of sperm capacitation, signal transduction mechanism, capacitation mechanism, overview
-
-
-
additional information
?
-
-
the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has decreasing effect, opposing to receptor protein tyrosine kinase EGFR, on volume-sensitive chloride current in atrial myocytes, overview
-
-
-
additional information
?
-
-
the enzyme plays an important role in the self-renewal and as comitogen in the movement of stem cells out of the haematopoietic stem cell pool into the progeny pool, regulation of bone marrow cell migration
-
-
-
additional information
?
-
-
the Fes tyrosine kinase is regulated via its SH2 domain
-
-
-
additional information
?
-
-
the Janus kinase is involved in the JAK-STAT signaling cascade causing inflammatory activity in the brain
-
-
-
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in epithelium which induces chemokine KIP-2 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
-
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in lung epithelium which induces interleukin-8 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
-
additional information
?
-
-
the Syk family tyrosine kinase ZAP-70 is required to couple the activated T-cell antigen receptor TCR to downstream signaling pathways, binding of TCR via its SH2 domains, regulation mechanism, overview
-
-
-
additional information
?
-
A1A5H8
Yes kinase is required during development, overview
-
-
-
additional information
?
-
-
c-Fes interacts with soluble unpolymerized tubulin via its N-terminal Fes/CIP4 homology FCH domain
-
-
-
additional information
?
-
-
Csk-substrate interaction requires the SH2 and SH3 enzyme domains
-
-
-
additional information
?
-
-
low tyrosine autophosphorylation activities of chimeric Alk-NPM and ALK-TPM3
-
-
-
additional information
?
-
-
poor activity on free amino acids, consensus sequence of c-Src is E-EIYE/G-XF, that of v-Fps is E-IYE-XI/V, and that of Csk is IYM-F-F-F, specificity overview
-
-
-
additional information
?
-
-
Pyk2 performs autophosphorylation at Tyr402, fibroblast growth factor receptors FGFR1 and FGFR4 are no substrates of Pyk2
-
-
-
additional information
?
-
-
site specificity of tyrosine phosphorylation by Tec family members, overview
-
-
-
additional information
?
-
-
Syk kinase performs autophosphorylation
-
-
-
additional information
?
-
-
Syk performs autophosphorylation
-
-
-
additional information
?
-
-
the activation loop is not essential for enzyme activity
-
-
-
additional information
?
-
-
the BCR/ABL kinase performs tyrosine autophosphorylation, mechanism
-
-
-
additional information
?
-
A1A5H8
the Yes kinase performs autophosphorylation
-
-
-
additional information
?
-
-
Wee1: substrate specificity
-
-
-
additional information
?
-
-
a multisite model for Fyn binding and regulation, overview, subtype-selective modulation by tyrosine phosphorylation/dephosphorylation provides a mechanism for differential regulation of sodium channels by neurotrophins and tyrosine phosphorylation in unmyelinated axons and dendrites, where NaV1.2 channels are expressed in brain neurons, overview
-
-
-
additional information
?
-
-
Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
-
-
-
additional information
?
-
-
c-Abl activates p21 transcription via interaction with and regulation of the DNA-binding of p53, c-Abl also recruits p53 to the p21 promoter, overview
-
-
-
additional information
?
-
-
c-Abl is regulated by conformational changes through intramolecular interactions and phosphorylation, overview
-
-
-
additional information
?
-
-
c-Src is a physiologically relevant substrate for Methionine aminopeptidases, whose dysfunction is likely to account for the cell-cycle effects of MetAP inhibitors including bengamide A, overview
-
-
-
additional information
?
-
-
Csk is essential for mouse embryonic development, Csk plays a role in G protein-coupled receptor- and receptor tyrosine kinase-induced fibroblast cell migration, overview, modeling of Csk regulation of focal adhesion turnover
-
-
-
additional information
?
-
P00519
dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
-
-
-
additional information
?
-
Q06187
enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
-
-
-
additional information
?
-
-
enzyme-deficient endothelial cells shows reduced migration, as well as decreased cell proliferation and survival in vivo
-
-
-
additional information
?
-
-
Etk is essential for polymyxin resistance, while Wzc is not
-
-
-
additional information
?
-
-
FAK plays a role in the anoikis phenomenon or anchorage-dependent cell survival, and in angiogenesis and formation of new blood vessels, overview, downstream targets of the FAK and PYK2 are MAP kinases implicated in proliferative processes, PYK2 is an essential linker between G-protein coupled receptor and the MAPK cascade, overview
-
-
-
additional information
?
-
P07332
Fes is involved in the regulation of cell-cell and cell-matrix interactions mediated by adherens junctions and focal adhesions, the activated form of the kinase can induce cellular transformation, overview
-
-
-
additional information
?
-
-
Fyn tyrosine kinase is involved in actin stress fiber formation in fibroblasts
-
-
-
additional information
?
-
-
Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
-
-
-
additional information
?
-
-
p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
-
-
-
additional information
?
-
-
protein-tyrosine kinase Syk plays a central role in Fcgamma receptor-mediated phagocytosis in the adaptive immune system, and is required for pathogen engulfment in complement-mediated phagocytosis
-
-
-
additional information
?
-
-
PYK2 is involved in vascular endothelial growth factor-induced activities, such as cell migration, blood vessel formation, Pyk2 forms complexes with Src tyrosine kinase for activation of the Akt tyrosine kinase pathway, PYK2 is required in receptor- and ischemia-activated signaling events leading to endothelial NO synthase phosphorylation and modulation of endothelial NO synthase-mediated vasoactive function and angiogenic response, PYK2 is involved in Ca2+ mobilization in muscle cells, overview
-
-
-
additional information
?
-
-
spleen tyrosine kinase Syk is necessary for E-selectin-induced alpha(L)beta(2) integrin-mediated rolling on intercellular adhesion molecule-1, neutrophil activation pathways, overview
-
-
-
additional information
?
-
-
Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation
-
-
-
additional information
?
-
-
Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation, Abl/Rac and Abl/ERK5 pathways also operate in human MCF7 and BT549 breast cancer cells, where neoplastic transformation depends on Src-like activities, overview
-
-
-
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
-
additional information
?
-
-
Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
-
-
-
additional information
?
-
-
the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview
-
-
-
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
-
additional information
?
-
Q62120
the enzyme is involved in cytokine signaling
-
-
-
additional information
?
-
-
the enzyme tyrosine phosphorylates a wide range of proteins, especially nuclear matrix proteins
-
-
-
additional information
?
-
-
the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis
-
-
-
additional information
?
-
-
the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview
-
-
-
additional information
?
-
-
the Src-family tyrosine kinase fyn phosphorylates phosphatidylinositol 3-kinase enhancer-activating Akt, preventing its apoptotic cleavage and promoting cell survival, overview
-
-
-
additional information
?
-
-
Toll-like receptors TLR-8 and TLR-9 require activation/phosphorylation by Btk for acting incell signaling, overview, enzyme deficiency is involved in development of male immune disorder X-linked agammaglobulineamia, XLA
-
-
-
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor in to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
-
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
-
additional information
?
-
-
tyrosine kinase Src is a key enzyme in mammalian signal transduction and an important target for anticancer drug discovery
-
-
-
additional information
?
-
-
tyrosine kinases play a fundamental role in cell proliferation, survival, adhesion, and motility and have also been shown to mediate malignant cell transformation, Brk may play a key role in lymphomagenesis
-
-
-
additional information
?
-
-
Abl does not mediate tyrosine phosphorylation of Stat3 and Shc, two important regulators of Src oncogenic activity
-
-
-
additional information
?
-
-
Btk can interact with the TIR domains of Toll-like receptors TLR-8 and TLR-9
-
-
-
additional information
?
-
-
BTK performs autophosphorylation
-
-
-
additional information
?
-
-
Btk performs autophosphorylation on Tyr223
-
-
-
additional information
?
-
-
c-Abl performs autophosphorylation
-
-
-
additional information
?
-
-
Fak binds interaction partners, e.g. paxillin, talin, and p190RhoGEF, at the FAT domain, i.e. the focal adhesion targeting domain, at the C-terminal domain modulaing the Fak activity, overview
-
-
-
additional information
?
-
-
FAk binds interaction partners, e.g. paxillin, talin, and p190RhoGEF, at the FAT domain, i.e. the focal adhesion targeting domain, at the C-terminal domain modulating the Fak activity, overview
-
-
-
additional information
?
-
-
receptor-bound Jak2 allows the transphosphorylation of the dimeric receptor molecule one another
-
-
-
additional information
?
-
-
Src PTKs phosphorylate substrates in the cytosol or at the inner face of the plasma membrane, e.g. Shc, Rho GTPase-activating protein p190, and transcription factor STAT3, substrates at cell-matrix adhesions, e.g. cytoskeleton-associated proteins such as focal adhesion kinase FAK, Cas, paxillin, ezrin, and cortactin, and substrates at cell-cell adhesions, e.g. junctional proteins such as beta-catenin, p120, and plakoglobin
-
-
-
additional information
?
-
-
Syk affects actin dynamics around the C3bi-mediated phagosomes
-
-
-
additional information
?
-
-
the enzyme is activated by phosphorylation, and also performs autophosphorylation
-
-
-
additional information
?
-
-
the enzyme performs autophosphorylation at tyrosine residues
-
-
-
additional information
?
-
-
Lyn is an important B cell signaling kinase of the Src tyrosine kinase family with a broad range of functions from cytoskeletal changes to induction of apoptosis, Lyn and and its interaction with rafts and TLR2 are involved in the initial stages of Pseudomonas aeruginosa interaction with host cells and invasion of an alveolar epithelial cell line, primary lung cells, and rat lungs by Pseudomonas aeruginosa, overview
-
-
-
additional information
?
-
-
SH2 domain-based tyrosine kinase assay using biotin ligase modified with a terbium(III) complex. An SH2 domain from lymphocyte-specific tyrosine kinase is genetically fused to a truncated biotin carboxyl carrier protein, and the resulting fusion protein is labeled through biotinylation with biotin protein ligase carrying multiple copies of a luminescent Tb3+ complex. The labeled SH2 fusion proteins are employed to detect a phosphorylated peptide immobilized on the surface of the microtiter plate, where the phosphorylated peptide is produced by phosphorylation to the substrate peptide by Src tyrosine kinase. The assay allows for a reliable determination of the activity of Src kinase lower than 10 ng/mL
-
-
-
additional information
?
-
Mus musculus C57BL/6
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
-
additional information
?
-
Moloney murine sarcoma virus HT-1
P07331
p40mos binds ATP analog p-fluorosulfonylbenzoyladenosine and exhibits ATPase activity
-
-
-
additional information
?
-
P00541
oncogene v-fps induces fibrosarcomas in birds
-
-
-
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
-
enzyme plays an important role in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
ILK is a receptor-proximal protein kinase regulating integrin-mediated signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme is upregulated in HT-144 melanoma cells following TGF-beta1 stimulation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q13418
ILK is involved in agonist stimulated, Pi(3)K-dependent, PKB/AKT activation. ILK is thus a receptor-proximal effector for the Pi(3)K-dependent, extracellular matrix and growth factor mediated, activation of PKB/AKT, and inhibition of GSK-3
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
the enzyme controls shoot and floral meristem size
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme contributes to signal transduction
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q15569
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q63572
TESK1 has a specific function in spermatogenesis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
P53666
it is likely that LIMK is involved in developmental or oncogenic processes through interactions with these LIM-containing proteins
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q924U5
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q96S53
the enzyme induces formation of actin stress fibers and focal adhesions
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O70146
role for this kinase in spermatogenesis
-
-
-
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O43187
proximal mediators of IL-1 signaling
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
Q9Y572
apoptosis-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O43353
NF-kappaB-activating and cell death-inducing kinase
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
the enzyme is a downstream effector of activated Ras. Interaction with Ras leads to Raf-1 activation and results in transduction of cell growth and differentiation signals
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme functions as an intermediary in TNFalpha-induced apoptosis
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
enzyme is required in early larval development
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
P10398
enzyme plays a critical role in cell growth and development
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
O60674
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
activation of Syk is responsible for K-Cl cotransport in SS cells by relieving Src-mediated inhibition of the transporter
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells, Abl is also required for Src-induced transformation of mouse fibroblasts, overview
-
-
?
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
show the reaction diagram
-
tyrosine kinase Akt is phosphorylated by PYK2 for activation of the Akt signaling pathway, overview
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + cdc2
ADP + phosphorylated cdc2
show the reaction diagram
-
the Cdc2-inhibitory kinase is required for preventing premature activation of the mitotic program. Maternally provided Dwee1 is sufficient for regulating Cdc2 during embryogenesis
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
P30291
Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p32-L-tyrosine
ADP + p32-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
-
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
P41239
phosphorylates the regulatory C-terminal tyrosine residue present on cytoplasmic tyrosine kinases of the Src family
-
-
?
ATP + protein
?
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
P32577
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain, specifically phosphorylates a negative regulatory site of p60c-src
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
P42679
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
-
proto-oncogenic PTK protein substrate
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
show the reaction diagram
Mus musculus, Mus musculus C57BL6J/129Sv
-
activation of disabled-1 adaptor protein Dab1, which is responsible for regulation of neuronal migrations during mammalian brain development, Reelin induces tyrosine-phosphorylated-Dab1 degradation and downregulates Dab1 expression in primary cortical neurons, mutant non-phosphorylated Dab1 are not degraded, pathway regulation, overview
-
-
?
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion
-
?
ATP + [FAK]-L-tyrosine
ADP + [FAK]-L-tyrosine phosphate
show the reaction diagram
A1A5H8
activation of FAK during epiboly and gastrulation by dynamic phosphorylation at Tyr861
-
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein kinase C zeta]-L-tyrosine
ADP + [protein kinase C zeta]-L-tyrosine phosphate
show the reaction diagram
Q9WUD9
-
Src kinase plays an important role in angiotensin II-elicited protein kinase C zeta activation and the subsequent downstream signaling including ERK1/2 activation and vascular smooth muscle cell proliferation
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q35346
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
P58764
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q07014
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q06187
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q9WUD9
-
-
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
Q38KH2
-
-
-
?
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism
-
-
?
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
P00522
-
-
-
-
additional information
?
-
P42679
-
-
-
-
additional information
?
-
-
PTK6 may function as an intracellular signal transducer in specific tissues
-
-
-
additional information
?
-
Q62137
role for JAK3 in hematopoiesis and T- and B-cell development
-
-
-
additional information
?
-
-
transcriptionally induced in normal T cells by interleukin 2 stimulation, roles in T cell proliferation and differentiation
-
-
-
additional information
?
-
-
involvement of the Jak-3 Janus kinase in signalling by interleukins 2 and 4 in lymphoid and myeloid cells
-
-
-
additional information
?
-
-
JAK3 kinase is associated with terminal differentiation of hematopoietic cells
-
-
-
additional information
?
-
-
sensitizes mammary epithelial cells to epidermal growth factor
-
-
-
additional information
?
-
Q24592
required maternally for the establishment of the normal array of embryonic segments
-
-
-
additional information
?
-
Q9U5Y2
plays important roles in cell adhesion, functions downstream of integrins, enzyme is involved in integrin-mediated cell adhesion signaling
-
-
-
additional information
?
-
-
is likely to participate in a variety of integrin-extracellular-matrix-dependent signaling events during morphogenesis
-
-
-
additional information
?
-
P34152
the enzyme transduces signals initiated by integrin engagement and G protein-coupled receptors. Several splice isoforms of FAK are preferentially expressed in rat brain, some of which have an increased autophosphorylation activity
-
-
-
additional information
?
-
-
activation of FadK may be an important early step in intracellular signal transduction pathways triggered in response to cell interactions with the extracellular matrix
-
-
-
additional information
?
-
Q91738
participate in signalling pathways activated in response to cell interaction, role for FAK in gastrulation
-
-
-
additional information
?
-
P00541
oncogene v-fps induces fibrosarcomas in birds
-
-
-
additional information
?
-
-
associated with breast cancer and osteoporosis
-
-
-
additional information
?
-
-
mutations in the gene encoding the Drosophila tyrosine kinase Abelson substantially enhanced the severity of the CNS phenotype of armadillo mutations, consistent with these proteins functioning co-operatively at adherens junctions in both the CNS and the epidermis
-
-
-
additional information
?
-
-
enzyme plays a critical role in a variety of signal transduction pathways
-
-
-
additional information
?
-
-
lskT-encoded protein-tyrosine kinase may aid in transducing proliferative or differentiative signals unique to lymphocytes, enzyme is implicated in neoplastic transformation
-
-
-
additional information
?
-
-
enzyme is involved in pathway for signaling through glycosyl-phosphatidylinositol (GPI)-anchored membrane proteins
-
-
-
additional information
?
-
-
involved in signal transduction by association with a number of membrane receptors
-
-
-
additional information
?
-
-
elevated levels of p56tck can contribute to the malignant properties of LSTRA cells
-
-
-
additional information
?
-
-
p56lck can positively regulate T-cell functions and it mediates at least some of the effects of CD4 and CD8 on T-cell activation
-
-
-
additional information
?
-
P06240
p56lck participates in lymphocyte-specific signal transduction pathways. Disturbances in lck expression may contribute to the pathogenesis of some human neoplastic diseases
-
-
-
additional information
?
-
P10936
yes gene product is likely to play an important role in oogenesis or early development
-
-
-
additional information
?
-
-
enzyme may serve specialized functions in hemopoietic cells, it is possible that damage to HCK may contribute to the pathogenesis of some human leukemias
-
-
-
additional information
?
-
-
Hck is involved in a number of cell signal transduction pathways, frequently in pathways associated with immune response
-
-
-
additional information
?
-
-
participates in signal transduction events regulating the growth, differentiation and function of phagocytes
-
-
-
additional information
?
-
P16591
it may be involved in key regulatory processes
-
-
-
additional information
?
-
-
may be specifically involved in the cell growth of hepatocytes or in the step of hepatocarcinogenesis
-
-
-
additional information
?
-
-
may interact with the intracellular domain of cell surface receptors
-
-
-
additional information
?
-
-
participates in the signalling pathways of a broad range of cytokines
-
-
-
additional information
?
-
-
enzyme is crucial for B cell development. Loss of kinase activity results in the human immunodeficiency, X-linked agammaglobulinemia, characterized by a failure to produce B cells
-
-
-
additional information
?
-
P27446, P27447
possible function during secondary steps of tumor progression
-
-
-
additional information
?
-
-
directly implicated in the pathogenesis of X-linked agammaglobulinaemia
-
-
-
additional information
?
-
P32577
specifically phosphorylates Tyr527 of p60c-src from neonatal rat brain. Specifically phosphorylates a negative regulatory site of p60c-src
-
-
-
additional information
?
-
-
deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia
-
-
-
additional information
?
-
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R. Tyk2 protein functions as part of a receptor complex to initiate intracellular signaling in response to type I interferons
-
-
-
additional information
?
-
-
CSK is involved in regulation of src family kinases
-
-
-
additional information
?
-
P43403
ZAP-70 that associates with T cell antigen receptor zeta chain and undergoes tyrosine phosphorylation following TCR stimulation
-
-
-
additional information
?
-
-
tandem ZAP-70 SH2 domains bind phosphorylated, but not nonphosphorylated, T cell antigen receptor zeta cyt. The NH2-terminal ZAP-70 SH2 domain also binds to T cell antigen receptor zeta cyt but with 100-fold lower affinity. No binding is observed with the COOH-terminal ZAP-70 SH2 domain. Similar studies demonstrate that the ZAP-70 tandem SH2 domain can bind a T cell antigen receptor zeta 3 TAM peptide in which both tyrosine residues are phosphorylated: Little or no binding is observed with peptides phosphorylated at only one tyrosine residue, or a nonphosphorylated peptide. Binding of the tandem SH2 domains to the other two TCR zeta TAM peptides and to a CD3 epsilon TAM peptide is also observed. All four doubly tyrosine phosphorylated TAM peptides cross-compete with each other for binding to the tandem SH2 domains of ZAP-70. The affinity of these peptides for the tandem SH2 construct demonstrates a hierarchy of TAM zeta 1, TAM zeta 2, TAM epsilon, TAM zeta 3
-
-
-
additional information
?
-
-
perinatal lethality and blocked B-cell development in mice lacking the tyrosine kinase Syk. Syk-deficient radiation chimaeras fail to accumulate mature B cells, Syk-deficient mice show impaired development of thymocytes using the V gamma 3 variable region gene, Syk is not required for signalling through the IL-2 and G-CSF receptors
-
-
-
additional information
?
-
-
mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency
-
-
-
additional information
?
-
-
Rlk has potential functions in intrathymic T cell development and mature T cell signaling
-
-
-
additional information
?
-
P52333
JAK3 deficiency in a patient with severe combined immunodeficiency over 20 years after bone marrow transplantation: persistence of genetically and biochemically defective autologous B cells, associated with reconstitution of cellular and humoral immunity, suggests that integrity of the gammac-JAK3 signalling pathway is not strictly required for immunoglobulin production
-
-
-
additional information
?
-
-
JAK3 deficiency in humans results in autosomal recessive T-B+ severe combined immunodeficiency disease
-
-
-
additional information
?
-
-
HYL plays a significant role in the signal transduction of hematopoietic cells
-
-
-
additional information
?
-
-
enzyme plays a pivotal role in cell signal transduction
-
-
-
additional information
?
-
-
Ntk may play an inhibitory role in the control of T-cell proliferation
-
-
-
additional information
?
-
-
may play an important role in thymopoiesis, role in controlling cellular growth and differentiation
-
-
-
additional information
?
-
-
role for JAK1 kinase in the differentiation or function of a subset of CNS neurons
-
-
-
additional information
?
-
P51813
effector of phosphatidylinositol 3'-kinase and is involved in interleukin 6-induced neuroendocrine differentiation of prostate cancer cells
-
-
-
additional information
?
-
-
autosomal recessive form of severe combined immunodeficiency disease in which ZAP-70 is absent as a result of mutations in the ZAP-70 gene. This absence is associated with defects in TCR signal transduction. Integral role in T cell activation and differentiation
-
-
-
additional information
?
-
-
may play a role in the growth and differentiation of hematopoietic cells
-
-
-
additional information
?
-
P42685
may have a role in human cancer
-
-
-
additional information
?
-
P41243
Batk may function as a brain-specific regulator of kinases involved in the development and maintenance of the nervous system
-
-
-
additional information
?
-
-
JAK3 splice isoforms are functional in JAK3 signaling and may enrich the complexity of the intracellular response functional in IL-2 or cytokine signaling
-
-
-
additional information
?
-
P43404
activating motif occurs in four discrete steps: binding of p59fyn, phosphorylation of the motif, binding of ZAP-70, and activation of ZAP-70 kinase activity
-
-
-
additional information
?
-
-
Ctk is involved in the regulation of neural function and differentiation of male germ cells through interactions with members of the Src family kinases
-
-
-
additional information
?
-
-
mutations of the Janus family kinase JAK3 are responsible for autosomal recessive severe combined immunodeficiency. Abnormalities in tyrosine phosphorylation of JAK3 in response to interleukin-2 (IL-2) and IL-4 is present in all patients. In one patient carrying a single amino acid change, Glu481Gly, in the JH3 domain of JAK3, a partially conserved IL-2 responses is observed resulting in reduced but detectable levels of JAK3 and STAT5 phosphorylation. A single cysteine to arginine substitution, Cys759Arg, results in high basal levels of constitutive JAK3 tyrosine phosphorylation unresponsive to either downregulation by serum starvation or cytokine-mediated upregulation
-
-
-
additional information
?
-
Q04736
could be responsible for the tyrosine phosphorylation observed in a murine thymic medullary epithelial cell line E-5 following complex formation with thymocytes
-
-
-
additional information
?
-
Q07014
appear to play a role in B-cell-IgM and FcERI receptor signaling
-
-
-
additional information
?
-
-
functions during reinitiation of meiotic division
-
-
-
additional information
?
-
-
TGF-beta RII expression is down-regulated in cells treated with exogenous TGF-beta1
-
-
-
additional information
?
-
-
type II receptor isoforma exist which play preferential binding to TGF-beta2 and have their own defined role in debvelopment
-
-
-
additional information
?
-
P12965
the kinase induces progression through the cell cycle for both meiotic and mitotic cells
-
-
-
additional information
?
-
-
the receptor shares two-hit inactivation mechanism with tumor suppressor genes and mutation of it may occur in the early stage of tumorgenesis
-
-
-
additional information
?
-
-
mutations in the activin receptor-like kinase 1 gene in hereditary haemorrhagic telangiectasia type 2
-
-
-
additional information
?
-
P27037
activin and its receptor play an important role in development
-
-
-
additional information
?
-
P37023
the activin receptor-like kinase 1 gene is the second locus for the autosomal dominant vascular disease hereditary hemorrhagic telangiectasia
-
-
-
additional information
?
-
-
signal transduction by TGF bet involves the formation of a heteromeric complex of two different serine/threonine kinase receptors
-
-
-
additional information
?
-
P27041
involved in signal transduction
-
-
-
additional information
?
-
-
insensitivity to anti-mullerian hormone is due to a mutation in the human anti-mullerian hormone receptor
-
-
-
additional information
?
-
P36897
transforming growth factor-beta regulates cell cycle progression by a unique signaling mechanism that involves its binding to the type II TGF beta receptor and activation of type I
-
-
-
additional information
?
-
P50488
the receptor controls dauer larva development
-
-
-
additional information
?
-
P27039
importance of the function of activin receptor in the regulatory mechanism for body axis formation
-
-
-
additional information
?
-
Q09488
enzyme is involved in TGFbeta signaling
-
-
-
additional information
?
-
Q95126
enzyme can have a protein-protein interaction, through its putative SH3 binding site, with at least two intracellular SH3-containing proteins
-
-
-
additional information
?
-
P36894
enzyme is involved in bone morphogenetic protein signaling
-
-
-
additional information
?
-
Q62893
mullerian inhibiting substance causes regression of the fetal Mullerian duct on binding a heteromeric complex of types I and II cell-surface receptors in the fetal urogenital ridge. The anti-mullerian hormone type II receptor provides specificity for mullerian inhibiting substance
-
-
-
additional information
?
-
P20792
cell-surface receptor required for transduction of environmental signals into an appropriate developmental response, controls dauer larva development
-
-
-
additional information
?
-
Q9QZl0
mRIP3 uses a novel mechanism to induce death
-
-
-
additional information
?
-
O43353
RIP2 interacts with members of the TNFR-1 signaling complex, including inhibitor of apoptosis protein cIAP1 and with members of the TNFR-associated factor family, specifically TRAF1, TRAF5, and TRAF6, but not with TRAF2, TRAF3, or TRAF4
-
-
-
additional information
?
-
-
CARDIAK may be involved in NF-kappa B/JNK signaling and in the generation of the proinflammatory cytokine IL-1 beta through activation of caspase-1
-
-
-
additional information
?
-
-
in a cell cycle the wee1 kinase is phosphorylated at M-phase, phosphorylation occurs in the N-terminal domain resulting in inactivation of the kinase activity. The N-terminal domain, or the entire molecule is extensively phosphorylated by cdc2-cyclin B kinase
-
-
-
additional information
?
-
-
blocks cell division when overexpressed in Hela cells
-
-
-
additional information
?
-
P30291
activity of WEE1Hu is regulated by phosphorylation and proteolytic degradation, WEE1Hu plays a role in inhibiting mitosis before M phase by phosphorylating cyclin B1-Cdc2
-
-
-
additional information
?
-
P47817
down-regulation of Wee1-like kinase activity by phosphorylation at mitosis is a multistep process that occurs after other biochemical reactions have signaled the successful completion of S phase
-
-
-
additional information
?
-
-
active c-Fes tyrosine kinase binds tubulin and microtubules through separate domains and promotes microtubule assembly, c-Fes colocalization with microtubules in vivo requires the SH2 enzyme domain, implication in the differentiation of vascular, endothelial, myeloid, hematopoietic, and neuronal cells, overview
-
-
-
additional information
?
-
-
ALK-MYH9 performs tyrosine autophosphorylation in vivo, but not in vitro, possible mechanism
-
-
-
additional information
?
-
-
antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases, overview
-
-
-
additional information
?
-
-
CX3CL1, i.e. fractalkine, only member of the delta subclass of chemokines, triggers PTK Syk activity in monocytes/macrophages localized in F-actin-enriched cell protrusions, which are formed due to CX3CL1 treatment and subsequent increase in F-actin, Syk deficiency results in strong impairment of RAW cell migration to CX3CL1, overview
-
-
-
additional information
?
-
-
enzyme is involved in cell growth, differentiation, and apoptosis
-
-
-
additional information
?
-
-
Fes tyrosine kinase promotes survival and terminal granulocyte differentiation of factor-dependent myeloid progenitors (32D) and activates lineage-specific transcription factors, e.g. CCAAT/enhancer-binding protein-alpha and STAT3, down-regulation of macrophage marker F4/80
-
-
-
additional information
?
-
-
Fps/Fes and Fer protein-tyrosine kinases play redundant roles in regulating hematopoiesis
-
-
-
additional information
?
-
-
Fps/Fes tyrosine kinase is involved in regulation of erythropoiesis and of myeloid differentiation and survival
-
-
-
additional information
?
-
-
IP3 production in the hypersensitive response of lemon seedlings against Alternaria alternata involves active protein tyrosine kinases but not a G-protein, overview
-
-
-
additional information
?
-
-
JAK2 is an important intracellular mediator of cytokine signalling, JAK2 deficiency may lead to hematologic cancers, and a number of immune diseases
-
-
-
additional information
?
-
-
protein kinases and protein phosphatases regulate enzyme activities in the cell, overview
-
-
-
additional information
?
-
-
protein tyrosine kinase-dependent modulation of voltage-dependent potassium channels by genistein in cardiac ventricular myocytes
-
-
-
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, BCR/ABL and several other constitutive protein tyrosine kinases are activated in myeloid malignancies, overview, protein deregulation probable due to fusion gene formation because of chromosomal translocations or as distinct gain-of-function point mutations, autophosporylation of BCR/ABL kinase at Tyr177 is essential for myeloid leukomogenesis in vivo, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
-
-
-
additional information
?
-
-
protein tyrosine kinases are involved in downstream signaling pathways, e.g. BCR/ABL kinase in the phosphatidylinositol 3'-kinase pathway, required for regulation of cell differentiation and cell cycle regulation, expression of BCR/ABL kinase leads to functional downregulation of the basal transcription factor TFIIH involved in nucleotide excision DNA repair pathway, and to activation of RAD51 also involved in DNA repair, overview
-
-
-
additional information
?
-
-
protein tyrosine kinases play a critical role in the modulation of a wide range of cellular events such as cell division, cell differentiation, and cell metabolism, over-stimulation of PTKs impairs normal cell growth, resulting in oncogenic transformation, regulation of enzyme activity occurs in dynamic oscillatory behaviour, patterns and mechanism, overview
-
-
-
additional information
?
-
-
PTKs are involved in cell signalling
-
-
-
additional information
?
-
-
spleen tyrosine kinase Syk modulates epidermal growth factor receptor EGFR signalling in mammary epithelial cells acting as a negative controle element, regulation of EGFR by activation of the autophosphorylation activity of EGFR, but not of HER2 and HER3, overview
-
-
-
additional information
?
-
-
Src activates an outwardly rectifying chloride current in myocytes being involved in osmotic swelling, enzyme inhibition also inhibits stretch-activated Cl- current, mechanism, overview
-
-
-
additional information
?
-
-
Src and Src-family protein-tyrosine kinases are proto-oncogenes important in cell morphology, motility, proliferation, and survival, regulation by reversible phosphorylation, overview
-
-
-
additional information
?
-
-
Src family kinases Hck, Fyn and Src are constitutively expressed and are required for murine embryonic stem cell growth and differentiation, regulation of SFKs in response to leukemia inhibitory factor LIF and other growth factors, overview
-
-
-
additional information
?
-
-
Src-dependent outside-in signalling is a key step in the process of autoregulation of beta2 integrins in polymorphonuclear cells and required for adhesion of interleukin-8, Src PTKs are required for macrophage antigen-1-mediated adhesion, which is inhibited by cytochalasin D and involved F-actin and protein P-110, overview
-
-
-
additional information
?
-
-
Src-family protein tyrosine kinases are proto-oncogenic enzymes controlling mammalian cell growth and proliferation, the enzymes are regulated by activation through autophosphorylation of their kinase domain and by inhibition through phosphorylation of their regulatory tyrosine residue near the C-terminus, mechanism, overview, abberrant SFK activation contributes to cancer development
-
-
-
additional information
?
-
-
Syk kinase is involved in cell motility and activation of phosphatidylinositol 3'-kinase, Syk kinase inhibits the tyrosine phosphorylation of IkappaBalpha and thus inhibits activation of NFkappaB via interaction of IkappaBalpha and phosphatidylinositol 3'-kinase, pathway regulation, overview
-
-
-
additional information
?
-
-
Tec family tyrosine kinases play a central role in hematopoietic cellular signaling
-
-
-
additional information
?
-
-
the enzyme is involved in regulation of sperm capacitation, signal transduction mechanism, capacitation mechanism, overview
-
-
-
additional information
?
-
-
the enzyme is regulated in balance with protein tyrosine phosphatase, complex regulation mechanism, overview, the enzyme has decreasing effect, opposing to receptor protein tyrosine kinase EGFR, on volume-sensitive chloride current in atrial myocytes, overview
-
-
-
additional information
?
-
-
the enzyme plays an important role in the self-renewal and as comitogen in the movement of stem cells out of the haematopoietic stem cell pool into the progeny pool, regulation of bone marrow cell migration
-
-
-
additional information
?
-
-
the Fes tyrosine kinase is regulated via its SH2 domain
-
-
-
additional information
?
-
-
the Janus kinase is involved in the JAK-STAT signaling cascade causing inflammatory activity in the brain
-
-
-
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in epithelium which induces chemokine KIP-2 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
-
additional information
?
-
-
the Src tyrosine kinase regulates and stimulates silica particle formation in lung epithelium which induces interleukin-8 release activating the signaling cascade via phosphorylation of MAPK and ERK, overview
-
-
-
additional information
?
-
-
the Syk family tyrosine kinase ZAP-70 is required to couple the activated T-cell antigen receptor TCR to downstream signaling pathways, binding of TCR via its SH2 domains, regulation mechanism, overview
-
-
-
additional information
?
-
A1A5H8
Yes kinase is required during development, overview
-
-
-
additional information
?
-
-
a multisite model for Fyn binding and regulation, overview, subtype-selective modulation by tyrosine phosphorylation/dephosphorylation provides a mechanism for differential regulation of sodium channels by neurotrophins and tyrosine phosphorylation in unmyelinated axons and dendrites, where NaV1.2 channels are expressed in brain neurons, overview
-
-
-
additional information
?
-
-
Brutons tyrosine kinase is involved in B lymphocyte chemotaxis and homing, overview
-
-
-
additional information
?
-
-
c-Abl activates p21 transcription via interaction with and regulation of the DNA-binding of p53, c-Abl also recruits p53 to the p21 promoter, overview
-
-
-
additional information
?
-
-
c-Abl is regulated by conformational changes through intramolecular interactions and phosphorylation, overview
-
-
-
additional information
?
-
-
c-Src is a physiologically relevant substrate for Methionine aminopeptidases, whose dysfunction is likely to account for the cell-cycle effects of MetAP inhibitors including bengamide A, overview
-
-
-
additional information
?
-
-
Csk is essential for mouse embryonic development, Csk plays a role in G protein-coupled receptor- and receptor tyrosine kinase-induced fibroblast cell migration, overview, modeling of Csk regulation of focal adhesion turnover
-
-
-
additional information
?
-
P00519
dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors, overview
-
-
-
additional information
?
-
Q06187
enzyme deficiency leads to X-linked agammaglobulinemia, XLA, a humoral primary immunodeficiency in which affected patients have very low levels of peripheral B cells and a profound deficiency of all immunoglobulin isotypes, overview
-
-
-
additional information
?
-
-
enzyme-deficient endothelial cells shows reduced migration, as well as decreased cell proliferation and survival in vivo
-
-
-
additional information
?
-
-
Etk is essential for polymyxin resistance, while Wzc is not
-
-
-
additional information
?
-
-
FAK plays a role in the anoikis phenomenon or anchorage-dependent cell survival, and in angiogenesis and formation of new blood vessels, overview, downstream targets of the FAK and PYK2 are MAP kinases implicated in proliferative processes, PYK2 is an essential linker between G-protein coupled receptor and the MAPK cascade, overview
-
-
-
additional information
?
-
P07332
Fes is involved in the regulation of cell-cell and cell-matrix interactions mediated by adherens junctions and focal adhesions, the activated form of the kinase can induce cellular transformation, overview
-
-
-
additional information
?
-
-
Fyn tyrosine kinase is involved in actin stress fiber formation in fibroblasts
-
-
-
additional information
?
-
-
Jak2 is involved in transcriptional signaling and ligand-independent gene expression, and increases the activity of erythropoietin receptor cell-surface expression, overview, enzyme deficiency is involved in lymphoid leukemia, overview
-
-
-
additional information
?
-
-
p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
-
-
-
additional information
?
-
-
protein-tyrosine kinase Syk plays a central role in Fcgamma receptor-mediated phagocytosis in the adaptive immune system, and is required for pathogen engulfment in complement-mediated phagocytosis
-
-
-
additional information
?
-
-
PYK2 is involved in vascular endothelial growth factor-induced activities, such as cell migration, blood vessel formation, Pyk2 forms complexes with Src tyrosine kinase for activation of the Akt tyrosine kinase pathway, PYK2 is required in receptor- and ischemia-activated signaling events leading to endothelial NO synthase phosphorylation and modulation of endothelial NO synthase-mediated vasoactive function and angiogenic response, PYK2 is involved in Ca2+ mobilization in muscle cells, overview
-
-
-
additional information
?
-
-
spleen tyrosine kinase Syk is necessary for E-selectin-induced alpha(L)beta(2) integrin-mediated rolling on intercellular adhesion molecule-1, neutrophil activation pathways, overview
-
-
-
additional information
?
-
-
Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation
-
-
-
additional information
?
-
-
Src and Abl regulation, overview, cytoplasmic tyrosine kinase Src is involved in signal transduction induced by growth factors and integrins, Src also shows oncogenic activity when it is deregulated, Abl mediates Src-induced extracellular regulated kinase 5, ERK5, activation to drive cell transformation, Abl/Rac and Abl/ERK5 pathways also operate in human MCF7 and BT549 breast cancer cells, where neoplastic transformation depends on Src-like activities, overview
-
-
-
additional information
?
-
-
Src PTK plays a role in NF-kappaB activation in epithelial cells, Src PTKs are important in regulation of vascular permeability and acute inflammatory responses, and are essential for the recruitment and activation of monocytes, macrophages, neutrophils, and other immune cells, Src PTKs can also regulate the functional activity of these receptors and is involved in cell signaling, biological functions, cellular and molecular mechanisms, overview
-
-
-
additional information
?
-
-
Syk protein tyrosine kinase is involved in lipopolysaccharide-induced responses and intracellular signaling leading to release of pro-inflammatory mediators in macrophages, overview
-
-
-
additional information
?
-
-
the BCR-ABL tyrosine kinase is inhibited in Philadelphia chromosome-positive chronic myeloid leukemia, CML, overview
-
-
-
additional information
?
-
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
-
additional information
?
-
Q62120
the enzyme is involved in cytokine signaling
-
-
-
additional information
?
-
-
the enzyme tyrosine phosphorylates a wide range of proteins, especially nuclear matrix proteins
-
-
-
additional information
?
-
-
the Src family of protein kinases mediates mitogenic signal transduction, and constitutive activation of the enzymes is associated with tumorigenesis
-
-
-
additional information
?
-
-
the Src protein tyrosine kinase p56Lck plays a critical role in the O2 sensitivity of Kv1.3 channels and in signalling during hypoxia in T lymphocytes, overview
-
-
-
additional information
?
-
-
the Src-family tyrosine kinase fyn phosphorylates phosphatidylinositol 3-kinase enhancer-activating Akt, preventing its apoptotic cleavage and promoting cell survival, overview
-
-
-
additional information
?
-
-
Toll-like receptors TLR-8 and TLR-9 require activation/phosphorylation by Btk for acting incell signaling, overview, enzyme deficiency is involved in development of male immune disorder X-linked agammaglobulineamia, XLA
-
-
-
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor in to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
-
additional information
?
-
-
tyrosine kinase Fyn determines the specific localization of TrkB brain-derived neurotrophic factor, BDNF, receptor to intracellular lipid rafts in cortical and hippocampal membranes, this process is critically dependent on the tyrosine kinase Fyn, overview, role for lipid rafts in neurotrophin signaling
-
-
-
additional information
?
-
-
tyrosine kinase Src is a key enzyme in mammalian signal transduction and an important target for anticancer drug discovery
-
-
-
additional information
?
-
-
tyrosine kinases play a fundamental role in cell proliferation, survival, adhesion, and motility and have also been shown to mediate malignant cell transformation, Brk may play a key role in lymphomagenesis
-
-
-
additional information
?
-
-
Lyn is an important B cell signaling kinase of the Src tyrosine kinase family with a broad range of functions from cytoskeletal changes to induction of apoptosis, Lyn and and its interaction with rafts and TLR2 are involved in the initial stages of Pseudomonas aeruginosa interaction with host cells and invasion of an alveolar epithelial cell line, primary lung cells, and rat lungs by Pseudomonas aeruginosa, overview
-
-
-
additional information
?
-
Mus musculus C57BL/6
-
the Brutons tyrosine kinase is a critical signaling mediator downstream of the B cell Ag receptor, plays a role in regulating TLR-induced cytokine production, and is required for TLR-induced IL-10 production in multiple macrophage populations and in TLR signaling, overview, X-linked agammaglobulinemia is caused by mutations in Btk resulting in multiple defects in B cell development and function, and recurrent bacterial infections, Btk-dependent induction of NFkappaB and AP-1 DNA binding activity
-
-
-
additional information
?
-
P00541
oncogene v-fps induces fibrosarcomas in birds
-
-
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ATP
-
-
ATP
-
the binding site is a deep pocket lined by hydrophobic residues, enzyme affinity of v-Fps for ATP is not influenced by phosphorylation of the activation loop
ATP
-
dependent on
ATP
-
as MgATP2-, binding site structure
ATP
-
as MgATP-, binding site structure
ATP
-
as MgATP2-, binding site structure
ATP
-
binding lobe structure
ATP
-
-
ATP
-
structure-activity-relationship, overview
ATP
-
as MgATP-
ATP
-
Abl binding structure
ATP
-
preactivation of the enzyme by incubation in the presence of 8.3 mM ATP and 16.6 mM MgCl2
ATP
P58764
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
bicarbonate
-
required by TK-32 for sperm capacitation activity
Ca2+
-
required by TK-32 for tyrosine phosphorylation and sperm capacitation activities
Ca2+
-
dependent on, PYK2 is involved in Ca2+ mobilization in muscle cells
Cd2+
-
can partially substitue Mg2+
Co2+
-
can partially substitue Mg2+
Cu2+
-
increases tyrosine phosphorylation in vivo, prevented by preincubation with genistein
Hg2+
-
increases tyrosine phosphorylation in vivo, genistein decreases the activating effect
Mg2+
-
dependent on, Mg2+ is the physiologic metal ion, other divalent cations are able to support nucleotide binding, but only Mn2+, Co2+, and Cd2+ can substitute Mg2+ in supporting the catalytic activity
Mg2+
-
significantly greater activity in the presence of Mn2+ than Mg2+
Mg2+
-
as MgATP2-
Mg2+
-
as MgATP2-, binds to Asp404, physiological cation, can be substituted by Mn2+
Mg2+
-
as MgATP-
Mg2+
-
essential, 2 Mg2+ are required, one Mg2+ binds to ATP as MgATP-, the other Mg2+ acts as an essential activator on the enzyme, whose binding is pH-sensitive between pH 6.0 and pH 7.0, M2 binding involves Glu236 and Asp332, binding structure, overview
Mg2+
-
Syk requires 20 mM, Fyn and Abl require 10 mM
Mg2+
-
Chk requires about 10 mM Mg2+ for full activity
Mg2+
-
preactivation of the enzyme by incubation in the presence of 8.3 mM ATP and 16.6 mM MgCl2
Mg2+
-
required for activity
Mn2+
-
can partially substitue Mg2+
Mn2+
-
significantly greater activity in the presence of Mn2+ than Mg2+
Mn2+
-
binds to Asp404, can substitute for Mg2+
Mn2+
-
activates, required for interaction between the Src family protein tyrosine kinase and the beta2-integrin macrophage antigen-1
Mn2+
A1A5H8
-
Mn2+
-
Syk requires 5 mM, Fyn requires 10 mM
Mn2+
-
optimal at 0.5 mM, inhibitory above 1 mM
Zn2+
-
-
additional information
-
the ability of metal cations to interact with Csk correlates with a combination of ionic radius and the coordination number
additional information
-
no requirement for Fe2+
additional information
-
isoform Pyk2 is not a Ca2+-dependent kinase in T cells but instead, increased intracellular Ca2+ induces Pyk2 phosphorylation through production of reactive oxygen species. Ca2+-stimulated Pyk2 phosphorylation is dependent on Src-family kinase activity, even at the Pyk2 autophosphorylation site. Pyk2 phosphorylation in cytotoxic T-lymphocytes is not absolutely Ca2+-dependent but relies on the strength of T-cell receptor stimulation
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
(2E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
-
WP1066
(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
LS104
(2E,4E)-N-benzyl-2-cyano-5-(3,4-dihydroxyphenyl)penta-2,4-dienamide
-
AG490, potent JAK2 inhibitor
(4E,6Z,8S,9S,10E,12S,13R,14S,16S,17R)-8,13,14,17-tetramethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
-
indirect pharmacological inhibitor
1-azaanthraquinones
-
-
-
1-methyl-emodin
-
inhibition of p56lck and c-Src
-
2,5-dihydroxy methyl cinnamate
-
i.e. DHMC, PTK inhibitor, prevents the IP3 production in lemon seedlings in response to fungal attack and blocks the development of hypersensitive response
2,5-dihydroxy-3-(3,4-dihydroxyphenyl)-6-phenyl-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,5-dihydroxy-3-phenyl-6-(3,4,5-trihydroxyphenyl)-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,7,8-trihydroxy-3-phenyl-1,4-dibenzofurandione
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
-
i.e. JAK inhibitor-I
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-omega-hydroxy-emodin
-
inhibition of p56lck and c-Src
-
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
;
2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-one
-
potent pan-JAK inhibitor
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
-
;
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
-
CP-690,550 JAK3-specific inhibitor
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
Q9WUD9
PP2
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
A1A5H8
i.e. pp2, inhibits Src family PTKs, inhibition of zebrafish egg/embryo development by Yes kinase inhibition
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, broad spectrum SFK inhibitor, competitive to ATP, in vitro and in vivo
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibition of Csk involves Thr265, no inhibition of Chk
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, ihibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp2, inhibits Src family PTKs
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. PP2, abolishes the hypoxia-induced inhibition of Kv1.3 channels in primaryhumanT lymphocytes
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
enzyme inhibition prevents internalization of the organism into host cells
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp2, Lck inhibitor
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. PP2, inhibits Src
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp2, inhibits Src family members like Lyn, no inhibition of Syk
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
selective Src-kinase inhibitors 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine and 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine, at 5 microM, attenuate acetylcholine-induced ionic currents and intracellular Ca2+ ion concentration transients in major pelvic ganglion neurons
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
application completely abolishes thrombin-induced non-capacitative cation entry into platelets, a Ca2+ entry pathway that is independent of Ca2+ store depletion. Src family tyrosine kinase activation is a required step in non-capacitative cation entry activation
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp1, synthetic inhibitor, inhibits SFKs by binding competitively to the ATP-binding site
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
i.e. pp1, inhibits Src family PTKs
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp1, inhibits Src family members like Lyn, no inhibition of Syk
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
selective Src-kinase inhibitors 4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine and 4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine, at 5 microM, attenuate acetylcholine-induced ionic currents and intracellular Ca2+ ion concentration transients in major pelvic ganglion neurons
-
4-amino-7-phenylpyrazolo[3,4-d] pyrimidine
A1A5H8
i.e. pp3, inhibits Src family PTKs, slight inhibition of zebrafish egg/embryo development by Yes kinase inhibition
-
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
-
inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo
8-methyl-emodin
-
inhibition of p56lck and c-Src
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
-
;
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
-
;
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
;
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
;
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
;
A-419259
-
high inhibition of SFKs
-
acacetin
-
inhibition of p56lck
AcpYEEI
-
ATP-phosphopeptide conjugate
-
ADP
-
competitive versus ATP, noncompetitive versus S1 peptide
AG-490
-
inhibits JAK2 tyrosine kinase
AG1024
-
-
AG490
-
potent JAK2 inhibitor
alsterpaullone
-
at 0.01 mM: 66% inhibition of CHK, 81% inhibition of LCK, and 10% inhibition of CSK
AMN107
-
a specific BCR-ABL tyrosine kinase inhibitor, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
AMP-PNP
-
-
AP23464
-
ineffective against Abl mutant T315I, but inhibitory against imatinib-resistant mutants M351I, E255K, Q252H, and Y253F, and activation loop mutant H396P
AP23464
-
;
apigenin
-
inhibition of p56lck
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-gamma-S
-
-
AZ960
-
potent and selective ATP competitive inhibitor of JAK2 enzyme activity
AZD-1480
-
Jak2 inhibitor
AZD0530
-
;
BAY61-3606
-
-
Bcr protein
-
negative regulator
-
bengamide A
-
c-Src from bengamide A-treated cells retains its N-terminal methionine and suffers a decrease in N-terminal myristoylation, which is accompanied by a shift of its subcellular distribution from the plasma membrane to the cytosol, and decreased tyrosine kinase activities of c-Src both in vitro and in vivo and eventually delayed cell-cycle progression through G2/M, overview, bengamide A reduced tyrosine phosphorylation on a few proteins, and is not a general tyrosine kinase inhibitor
bisindolylmaleimide I
-
blocks alboaggregin-A activation of Fyn
bistyrphostin
-
complete inhibition of TK-32
bosutinib
P00519
i.e. SKI-606, a dual Src/Abl inhibitor
bosutinib
-
;
bosutinib
-
previously SKI-606, inhibits ABL1
bosutinib
-
two distinct chemical compounds are currently being sold under the name bosutinib, spectroscopic and structural characterizations of both
C-terminal Src kinase
-
i.e. CSK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
catenarin
-
i.e. 4-hydroxy-emodin, inhibition of p56lck and c-Src
caveolin
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
CGP76030
-
growth-inhibitory in vivo
Chk
-
i.e. Csk-homologous kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, Chk is also a 'non-catalytic inhibitor' binding directly to the SFK forming stable complexes and inhibiting it, mechanism, overview
-
chrysin
-
inhibition of p56lck
CMP6
-
i.e. 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, specific for JAK2, kinase domain binding structure and mechanism
-
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690,550
-
orally active JAK inhibitor that potently inhibits JAK3
CP-690,550
-
has nanomolar potency in in vitro JAK2 and JAK3 kinase assays
CP-690,550
-
JAK3-specific inhibitor
CP690,550
-
targeting Jak3
Csk
-
i.e. C-terminal Src kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, mechanism, overview
-
CSK-homologous kinase
-
i.e. CHK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, a second non-catalytic inhibitory mechanism involves tight binding of CHK to the enzmyes SFKs. The binding alone is sufficient to inhibit SFKs inhibition, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
curcumin
-
inhibits the JAK-STAT signaling cascade via activation of SHP-2, a SH2 domain-containing phosphatase, and increase in JAK-SHP-2 interaction contributing to anti-inflammatory activity in the brain, suppresses STAT-responsive inflammatory gene expression
curcumin
-
downregulates and inhibits tyrosine kinase Syk, which leads to inhibition of Akt, in lymphoma cells, curcumin causes growth inhibition of B lymphoma, mechanism, overview
damnacanthal
-
an anthraquinone, strong and selective inhibition of p56lck
dasatinib
P00519
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
dasatinib
-
i.e. BMS-354825, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
dasatinib
-
i.e. BMS-354825, a Bcr-Abl inhibitor, used for the treatment of imatinib-resistant chronic myelogenous leukemia, inhibits Abl and Src kinases, and the Tec kinases Btk at Th474 and Tec at Thr442, but not Itk, the mutant BtkT474I ans TecT442I are resistant to dasatinib, while mutantion of the insensitive wild-type Itk to ItkF435T renders the enzyme sensitive to dasatinib, overview, autophosphorylation of Btk at Tyr223 is inhibited only by dasatinib but not by imatinib or nilotinib
dasatinib
-
;
dasatinib
-
-
dasatinib
-
Jak2 inhibitor, at high doses (0.001 mM), dasatinib can inhibit Jak2 activity in vitro
dasatinib
-
potent ABL1 inhibitor
datiscetin
-
inhibition of p56lck
emodic acid
-
inhibition of p56lck and c-Src
emodin
-
inhibition of p56lck and c-Src
emodin
-
i.e. 6-methyl-1,3,8-trihydroxyanthraquinone, Lck inhibitor
emodin derivatives
-
synthetic analogues, inhibition of p56lck and Src, overview
-
endocrocin
-
inhibition of p56lck and c-Src
epihematoxylol
-
-
F-actin
-
negative regulator
-
fisetin
-
inhibition of p56lck
flavone derivatives
-
inhibition of p56lck, overview
-
Fus1 protein
-
negative regulator
-
galangin
-
inhibition of p56lck
geldanamycin
-
indirect pharmacological inhibitor
genistein
-
protein tyrosine kinase inhibitor
genistein
-
broad spectrum PTK inhibitor
genistein
-
-
genistein
-
isoflavone, inhibits PTKs, and reversibly inhibits voltage-dependent transient outward and rectifier inward K+-currents in myocytes, overview
genistein
-
broad-spectrum PTK inhibitor, increases volume-sensitive chloride current in atrial myocytes, is antagonized by pretreatment with VO43-
genistein
-
-
genistein
-
-
genkwanin
-
inhibition of p56lck
haematoxylene
-
-
haematoxylone
-
-
hematoxylin
-
-
Hg2+
-
at PO2 of about 20 mM
imatinib
P00519
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
imatinib
-
i.e. STI-571, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
imatinib
-
-
imatinib
-
-
imatinib
-
inhibits ABL1autophosphorylation as well as substrate phosphorylation
imatinib
-
a c-Abl-family kinase inhibitor, prevents the phosphorylation of substrate parkin, maintaining parkin in a catalytically active and protective state. The protective effects require parkin
imatinib mesylate
-
2-phenylaminopyrimidine derivate, i.e. CGP-57148, inhibits BCR/ABL kinase, used in antityrosine kinase therapy of myeloid leukemia
imatinib mesylate
-
-
imatinib mesylate
-
Gleevec
INCB018424
-
Jak2 inhibitor
INCB018424
-
Jak2 inhibitor
INCB16562
-
selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3
INCB18424
-
Incyte
INCB18424
-
targeting Jak1/2
INCB20
-
potently inhibits all members of the JAK family with a 100-1000fold selectivity for JAKs over more than 70 other kinases, potent and specific Pan-JAK inhibitor
-
indirubin-3'-monoxime
-
at 0.01 mM: 62% inhibition of CHK, 89% inhibition of LCK, but no inhibition of CSK
INNO-406
-
previously NS-187, inhibits ABL1
interdomain B
-
connects the enzyme's catalytic kinase domain with its SH2 domain, is responsible for regulatory autoinhibition of ZAP-70 involving Tyr315 and Tyr319, deletion of the interdomain B preserves enzyme function, the regulation mechanism is similar to receptor protein tyrosine kinase EphB2, EC 2.7.10.1, overview
-
interferon-gamma
-
enzyme inhibition in leukemic bone marrow cells
-
ITF2357
-
Jak2 inhibitor
JAK-inhibitor I
-
40% JAK2 residual activity in the presence of 0.002 mM JAK-inhibitor I and 0.02 mM ATP
-
kaempferide
-
inhibition of p56lck
kaempferol
-
inhibition of p56lck
kaempferol-3-O-arabinoside
-
slight inhibition of p56lck
-
kaempferol-3-O-rhamnoside
-
slight inhibition of p56lck
kenpaullone
-
at 0.01 mM: 35% inhibition of CHK, 85% inhibition of LCK, and 14% inhibition of CSK
lavendustin A
-
PTK inhibitor, prevents the IP3 production in lemon seedlings in response to fungal attack and blocks the development of hypersensitive response
lestaurtinib
-
Jak2 inhibitor
lestaurtinib
-
formerly CEP701, JAK2 inhibitor
LFM-A13
-
significantly impairs CXCL12-induced human B lymphoma cell line, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LFM-A13
-
significantly impairs CXCL12-induced mouse B cell chemotaxis, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LFM-A13
-
;
LFM-A13
-
-
LS104
-
Jak2 inhibitor
LS104
-
i.e. [(E,E)-2-(benzylaminocarbonyl)-3-(3,4-dihydroxystyryl)acrylonitrite], non-ATP-competitive small-molecule inhibitor of JAK2, 20% residual activity of mutant V617F in the resence of 0.02 mM LS104 and 0.02 mM ATP
LS104
-
-
luteolin
-
inhibition of p56lck
methyl 2,5-dihydroxycinnamate
-
i.e. DHC, inhibition of Syk and Lyn
MK-0457
-
Jak2 inhibitor
morin
-
inhibition of p56lck
myricetin
-
inhibition of p56lck
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)-1,3,5-triazine-2,4-diamine
-
-
N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)pyrimidine-4,6-diamine
-
-
N-tert-butyl-3-([5-methyl-2-[(4-piperazin-1-ylphenyl)amino]pyrimidin-4-yl]amino)benzenesulfonamide
-
TG101209
N-tert-butyl-3-[(5-methyl-2-[[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino]pyrimidin-4-yl)amino]benzenesulfonamide
-
TG101348, JAK2-specific inhibitor
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
;
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
-
;
N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
;
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
-
;
N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
-
;
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-chlorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-fluorophenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-phenylpyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[2-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[3-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[4-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
-
N6-Dimethylaminopurine
-
unspecific inhibitor of protein kinases
nevadensin
-
inhibition of p56lck
nilotinib
P00519
response of enzymes with BCR-ABL kinase domain in in vivo study are similar for patients with different mutations, except for T315I, which is more resistant
nilotinib
-
potent ABL1 inhibitor
NS-187
-
a specific dual ABL-LYN inhibitor
ON012380
-
inhibits wild-type and mutant Abls, substrate-competitive, ATP-incompetitive
p-fluorosulfonylbenzoyl 5'-adenosine
-
inactivates tyrosine protein kinase activity of p60src by reacting with lysine 295
paeciloquinone A
-
inhibition of p56lck and c-Src
Paeciloquinone B
-
inhibition of p56lck and c-Src
paeciloquinone C
-
inhibition of p56lck and c-Src
-
paeciloquinone D
-
inhibition of p56lck and c-Src
PAG protein
-
negative regulator
-
PC-005
-
-
-
PCI-31523
-
-
PD166326
-
-
PD166326
-
;
PD173955
-
-
PD180970
-
-
peroxiredoxin 1
-
inhibits ABL1 intracellularly
-
phosphoinositide
-
negative regulator
piceatannol
-
inhibition of p56lck
piceatannol
-
Syk kinase inhibitor
piceatannol
-
Syk inhibitor in vitro and in vivo
piceatannol
-
-
piceatannol
-
-
PIP2
-
inhibits ABL1 intracellularly
PNU156804
-
Jak3 inhibitor
PP1
-
growth-inhibitory in vivo
protein tyrosine phosphatases
-
e.g. T-cell protein tyrosine phosphatase, catalytic inhibitor of SFKs dephosphorylating the autoactivation tyrosine residue of SFK which leads to inhibition of SFK
-
purpurin
-
inhibition of p56lck and c-Src
purvalanol
-
at 0.01 mM: 22% inhibition of CHK, 80% inhibition of LCK and CSK
Pyk2-specific siRNA
-
-
-
quercetin
-
inhibition of p56lck
R112
-
-
R406
-
-
RACK1
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
resokaempferol
-
inhibition of p56lck
-
resveratrol
-
inhibition of p56lck
RNAi
-
knockdown of Btk results in decreased tumor necrosis factor-alpha
-
SB1518
-
Jak2 inhibitor
shRNA
-
-
-
siRNA
-
-
-
siRNA
-
;
-
SKI-606
-
cytotoxic inhibitor of BCR-ABL
Src kinase inhibitor-1
-
i.e. SKI-1, a 4-anilinoquinazoline, moderate inhibition in vitro and vivo
-
staurosporine
-
unspecific inhibitor of protein kinases
staurosporine
-
i.e. ST, inhibition of Syk and Lyn, IC50 for Syk is 0.008 mM
staurosporine
-
competitive versus ATP, noncompetitive versus S1 peptide
stilbene derivatives
-
inhibition of p56lck, overview
-
SU6656
-
more specific for Yes kinase than for other SFKs
syringetin
-
inhibition of p56lck
T47
-
57% inhibition of Syk at 0.1 mM
-
TG101209
-
Jak2 inhibitor
TG101209
-
Jak2 inhibitor
TG101209
-
-
TG101348
-
Jak2 inhibitor
TG101348
-
JAK2-specific inhibitor
tyrophostin A25
-
-
tyrphostin 25
-
p38 MAP kinase inhibitor SB203580 and protein tyrosine kinase inhibitor tyrphostin 25 combined can be used for inhibition of matrix metalloproteinase-9 expression, overview
tyrphostin A23
-
inhibits PTKs
tyrphostin A23
-
broad-spectrum PTK inhibitor, slight inhibition of Src
tyrphostin A25
-
broad-spectrum PTK inhibitor, slight inhibition of Src
tyrphostin A9
-
-
tyrphostin AG490
-
Jak3 inhibitor
vanadate
-
-
WASP
-
a non-catalytic inhibitor of SFKs, e.g. c-Src, mechanism, transient inhibition
-
WHI-P131
-
Jak3 inhibitor
WHI-P154
-
Jak3 inhibitor
Wortmannin
-
-
WP1066
-
-
XL019
-
Exelixis
XL019
-
Jak2 inhibitor
YM193306
-
-
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
Mn2+
-
inhibitory above 1 mM
additional information
-
no inhibition by daidzein
-
additional information
-
Abl-SH3 domain is implicated in negative regulation of the Abl kinase by mediating protein-protein interactions
-
additional information
-
completely inhibited by an excess of substrate peptide
-
additional information
-
no inhibition of Src with pp3, i.e. 4-amino-7-phenylpyrazolo[3,4-d] pyrimidine
-
additional information
-
no or poor inhibition of CHK1, LCK, and CSK by roscovitine
-
additional information
-
enzyme interaction studies using inhibitory antibodies, overview
-
additional information
-
SFKs are regulated involving autophosphorylation for activation and inhibition by diverse endogenous catalytic and non-catalytic inhibitors acting directly or via down-regulation of SFKs, recognition and mechanisms involving Csk and Chk, overview
-
additional information
-
synthesis, inhibitory potency, and mechanism of ATP-SH2-domain-derived phosphopeptide conjugates with short or long linkers binding at the ATP-binding site, structure-activity-relationship, overview
-
additional information
-
epidermal growth factor receptor EGFR induces Syk inhibition
-
additional information
-
daidzein is no inhibitor of PTKs, no direct Src kinase inhibition by tyrphostin AG17, tyrphosptin AG879 and genistein
-
additional information
-
analysis of inhibitory potential and cytotoxic effects of a large number of plant-derived secondary metabolites on PTKs and human tumor cell lines, respectively, overview
-
additional information
-
regulation of Lck by phosphorylation at Tyr505 by C-terminal Scr protein-tyrosine kinase which inhibits the enzyme
-
additional information
-
effects of inhibitors in vivo in SS cells on K-Cl cotransport, overview
-
additional information
-
inhibition of the Src phosphorylation by peptides mimicking the substrate binding site, overview
-
additional information
-
enzyme is cleaved by several proteases such as thrombin
-
additional information
P00519
development and evaluation of tyrosine kinase inhibitors
-
additional information
-
inhibition of epidermal growth factor stimulation inhibits fyn enzyme activity
-
additional information
-
inhibition evaluation study using Src family tyrosine kinase inhibitors and Abl tyrosine kinase, overview
-
additional information
-
no inhibition by 4-amino-7-phenylpyrazolo[3,4-d] pyrimidine, i.e. PP3
-
additional information
-
c-Abl is inactivated by interactions made by its SH3 and SH2 domains with the distal surface of the kinase domain, a critical N-terminal cap segment, phosphorylated on a serine residue that interacts with the connector between the SH3 and SH2 domains, buttresses the SH3-SH2 substructure in the autoinhibited state and locks it onto the distal surface of the kinase domain, overview
-
additional information
-
pY213 phosphopeptide of Abi1 inhibits c-Abl kinase activity by a noncompetitive mechanism
-
additional information
-
phosphorylation of Tyr508 in Lyn inhibits activity of the enzyme
-
additional information
-
c-Abl is downregulated in part by intramolecular interactions that provide autoinhibitory kinase effects
-
additional information
-
phosphorylation of Y527 leads to the inactivation of c-Src, negative regulation
-
additional information
-
ABL1 is autoinhibited in an intramolecular fashion that is similar to SRC kinases, where the SH3 domain is engaged with a single proline residue in the spacer region between the SRC homology 2 and tyrosine kinase domains
-
additional information
-
JAK2 is not inhibited by STI571
-
additional information
-
exposure of BE(2)-C cells to the heavy metals Cd2+ and Hg2+ and to rotenone inhibits interleukin-6, interferon-gamma and ciliary neurotrophic factor-mediated Jak/STAT signaling, reduces Jak1 and Jak2 autophosphorylation and induces Jak tyrosine nitration by mitochondrial disruption. Identical exposure of HepG2 hepatoma cells produces no inhibition of these cytokine responses.
-
additional information
P12931
use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases; use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
alboaggregin-A
-
Trimeresurus albolabris venom, activates Fyn activity and translocation
-
AMpYSSV
-
CBP-based phosphopeptide, activates
angiotensin subtype 1 receptor
-
AT-1 receptor
-
Ca2+
-
G-protein coupled receptor PAC1 regulates the tyrosine phosphorylation of isoform PYK2 in NCI-H838 nonsmall cell lung cancer cells. PYK2 phosphorylation is dependent upon Ca2+. The ability of PAC1 to regulate PYK2 is dependent on phospolipase and Src, and partially dependent on proteinkinase C
CD45
-
transmembrane receptor-like protein tyrosine phosphatase activating the SFK by dephosphorylation of the regulatory tyrosine residue
-
CX3CL1
-
i.e. fractalkine, only member of the delta subclass of chemokines, induces Syk activity in cytoskeletal remodeling
-
Epidermal growth factor
-
activates fyn
Epidermal growth factor
-
-
Epidermal growth factor
-
EGF
Epidermal growth factor
-
epidermal growth factor increases levels of tyrosine phosphorylation of Jak2
epidermal growth factor receptor
-
the Abl nonreceptor tyrosine kinase is activated by ligand-stimulated EGFR
-
epithelial growth factor receptor
-
-
-
EPQYEEIPIYL
-
a src kinase activating peptide, binds to the SH2 domain of the src-kinase and activates it, activation of endogenous src-PTKs does not inhibit Kv1.3 channels in T lymphocytes, overview
erythropoietin
-
activates Fps/Fes tyrosine kinase
-
H2O2
-
increases tyrosine phosphorylation in vivo, genistein decreases the activating effect
insulin-like growth factor 1 receptor
-
-
-
interleukin 5
-
activates Janus kinases JAK1 and JAK2
-
interleukin-2
-
enzyme activation in leukemic bone marrow cells
-
lipopolysaccharide
-
-
lipopolysaccharide
-
LPS
Lyn kinase
-
as part of the activation process Lyn phosphorylates Btk in Tyr551, which is subsequently autophosphorylated in Tyr223
-
lysophosphatidic acid
-
activates fyn
N,N'-ethylnitrosourea
-
enzyme activation in leukemic bone marrow cells
NGF
-
rapidly stimulates both Ser and Thr phosphorylation in vivo and autophosphorylation activity in vitro of the B-Raf protein
-
non-specific BRM sheep erythrocyte
-
BRM is biological response modifier, treatment leads to a slight enzyme activation in leukemic bone marrow cells
-
pervanadate
P16591
activation of isoform Fer by reactive oxygen species causes increased phosphorylation of RhoGDIalpha, regulator of the small GTPase Rac, and pervanadate treatment further augmented this
-
platelet-derived growth factor
-
PDGF
-
platelet-derived growth factor receptor
-
-
-
prolactin
-
activates Jak2
-
pseudolaric acid B
-
pseudolaric acid B, PAB, activates PTK to induce apoptosis
reactive oxygen species
P16591
activation of isoform Fer by reactive oxygen species causes increased phosphorylation of RhoGDIalpha, regulator of the small GTPase Rac, and pervanadate treatment further augmented this
-
Reelin
-
extracellular, stimulates disabled-1 adaptor protein Dab1 tyrosine phosphorylation by Src family PTKs, downregulates Dab1 expression in vivo
-
sphingosylphosphorylcholine
-
activates fyn
Src
-
activated Src kinase in aggressive breast cancer cell lines can activate c-Abl kinase
-
stem cell factor SCF
-
activates Fps/Fes tyrosine kinase
-
transforming growth factor beta receptor
-
TGF-beta receptor
-
tyrosine growth factor
-
the enzyme is activated by the tyrosine growth factor and seven transmembrane-spanning receptors
-
macrophage antigen-1
-
i.e. Mac1, a beta2-integrin activates Src PTKs Hck and Lyn, interaction of both requires Mn2+
-
additional information
-
Abl-SH3 domain is implicated in negative regulation of the Abl kinase by mediating protein-protein interactions. High-affinity SH3 ligands can compete for these interactions and specifically activate the Abl kinase
-
additional information
P00545
cellular counterpart of the viral v-fms oncogene product, the c-fms product, is the receptor for colony-stimulating factor 1 of macrophages, CSF-1. CSF-1 appeares to activate the serine/threonine kinase
-
additional information
-
tyrosine phosphorylation and association of ZAP-70 with zeta require the presence of src family PTKs
-
additional information
-
Jak-3 activation requires the serine-rich, membrane-proximal domain of the interleukin-2 receptor beta-chain, but does not require the acidic domain that is required for association and activation of Src family kinases
-
additional information
-
ILK activity is rapidly, but transiently, stimulated upon attachment of cells to fibronectin, as well as by insulin, in a phosphoinositide-3-OH kinase-dependent manner. Furthermore, phosphatidylinositol(3,4,5)trisphosphate specifically stimulates the activity of ILK in vitro, and in addition, membrane targeted constitutively active Pi(3)K activates ILK in vivo
-
additional information
-
activation loop structure of Src and of Csk, autophosphorylation sites
-
additional information
-
enzyme activity is induced by interleukin-8 in polymorphonuclear cells
-
additional information
-
Tec family tyrosine kinase is activated by tyrosine phosphorylation
-
additional information
-
phosphorylation of the autoactivation tyrosine residue leads to activation of SFK, displacement of the PPII linker from the SH3 domain and the regulatory tyrosine residue from the SH2 domain, activation mechanisms, overview
-
additional information
-
JAK2 activation loop structure, residues 994-1023, with phosphorylation sites Y1007 and Y1008, JAK2 switches between active and inactive forms involving the switch motif Asp994-Phe2995-Gly996 proximal to the active site, overview
-
additional information
-
Csk and CHK require conserved hydrophobicity in the SH2-kinase linker for catalytic activity
-
additional information
-
a treatment of leukemic bone marrow cells with a mixture of interleukin-2, interferon-gamma, and non-specific BRM sheep erythrocytes leads to an increase in enzyme activity
-
additional information
-
Csk is tyrosine autophosphorylated in the activation loop, structure
-
additional information
-
hypoxia/reoxygenation induces tyrosine phosphorylation of Lck and Lck activity in breast cancer cells and of IkappaBalpha, but not of IkappaBalpha serine phosphorylation, activation is inhibited by emodin and pp2
-
additional information
-
Src is activated by mechanical stretch of beta1 integrin, cell swelling and integrin clustering
-
additional information
-
all-trans retinoic acid alters PTK activity and rhythm characteristics, period and amplitude of activity oscillations, overview
-
additional information
-
the leukemia inhibitory factor LIF and other growth factors are linked to Src family kinase activation
-
additional information
-
deoxygenation of SS cells increases Syk and Lyn PTK activities, overview
-
additional information
-
the enzyme performs self-activation by autophosphorylation at tyrosine residues
-
additional information
-
the enzyme is activated by phosphorylation, and also performs autophosphorylation
-
additional information
-
Syk is activated by phosphorylation
-
additional information
-
different activation mechanisms for Jak2
-
additional information
-
PYK2 is phosphorylated for activation involving the vascular endothelial growth factor, overview
-
additional information
-
FAK and PYK2 are activated in response to motogenic and mitogenic factors by phosphorylation and autophosphorylation
-
additional information
-
constitutive SFK activation is associated with tumorigenesis, Hck and Lyn perform autophosphorylation for activation
-
additional information
-
activation mechanism, autophosphorylation of Tyr551 causes a 10-fold increase in BTK activity
-
additional information
-
Akt is activated by phosphorylation at Ser473 and at Thr308
-
additional information
-
brain-derived neurotrophic factor BDNF induces the association and colocalization of TrkB with the lipid raft-resident protein Fyn, in situ study
-
additional information
-
activation of Lck by prolonged hypoxia leading to increased phosphorylation of Kv1.3 channels
-
additional information
-
c-Abl is regulated also by phosphorylation
-
additional information
P58764
protein kinase activation through an intra-molecular autophosphorylation process
-
additional information
-
nerve injury induces the activation of Src family kinases, Lyn is the predominant kinase
-
additional information
Q07014
nerve injury induces the activation of Src family kinases, Lyn is the predominant kinase
-
additional information
-
phosphorylation of Tyr397 in Lyn results in activation of the enzyme
-
additional information
-
phosphorylation of Etk on Y40 is required for Etk activation
-
additional information
-
Btk activation is induced by FcgammaR signaling, activation requires binding to phosphatidylinositol 3,4,5-trisphosphate; Tec activation is induced by FcgammaR signaling, activation requires binding to phosphatidylinositol 3,4,5-trisphosphate
-
additional information
Q35346
FAK is activated by autophosphorylation at Y397; SFK members are activated by phosphorylation and autophosphorylation
-
additional information
-
phosphorylation of Tyr418 is responsible for c-Src activation
-
additional information
-
phosphorylation of Y245 and Y412 leads to the activation of Abl kinase
-
additional information
-
autophosphorylation of Y416 leads to the activation of c-Src
-
additional information
-
SH2-Bb and dimerized receptors synergistically promote Jak2 trans-activation in the context of intracellular signaling, SH2-B and receptor dimers constitute a bipolar clamp that stabilizes the active configuration of two Jak2 molecules in the same macro-complex
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.014
ATP
-
-
0.075
ATP
-
pH 8.0, 30C, recombinant wild-type enzyme
0.084 - 0.09
ATP
-
preactivated wild-type BTK
0.106
ATP
-
untreated wild-type BTK
0.124
ATP
-
preactivated BTK mutant Y551
0.253
ATP
-
pH 8.0, 30C, recombinant mutant H384Y/Y527F
0.309
ATP
-
pH 8.0, 30C, recombinant mutant H384Y
0.327
ATP
-
pH 8.0, 30C, recombinant mutant H384Q
0.335
ATP
-
pH 8.0, 30C, recombinant mutant H384Y/Y416F
0.34
ATP
-
pH 8.0, 30C, recombinant mutant H384A
0.345
ATP
-
pH 8.0, 30C, recombinant mutant H384Q/Y416F
17.64
ATP
-
untreated BTK mutant Y551
0.057
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
-
0.01
kdSrc kinase
-
pH 8.0, 30C, recombinant mutant E338A Csk; pH 8.0, 30C, recombinant wild-type Csk
-
0.018
poly(Glu4-Tyr)
-
recombinant GST-fusion Chk, 12 mM Mg2+, no Mn2+
0.095
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant wild-type enzyme
0.15
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant wild-type Csk
0.164
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant DSH2 Csk mutant
0.204
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant W188A Csk mutant
0.274
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant mutant R281A/R283A
0.299
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant W188F Csk mutant
0.322
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant mutant S280A/R281A/R283A/F381A
0.328
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant DSH3 Csk mutant
0.659
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant K361G/K362A Csk mutant
0.037
S1 peptide
-
BTK
0.0057
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant wild-type enzyme
-
0.0139
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant mutant R281A/R283A
-
0.015
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant wild-type Csk
-
0.017
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant W188F Csk mutant
-
0.0229
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant mutant S280A/R281A/R283A/F381A
-
0.027
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant DSH3 Csk mutant
-
0.032
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant K361G/K362A Csk mutant
-
0.042
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant DSH2 Csk mutant
-
0.068
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant W188A Csk mutant
-
0.24
kdSrc kinase
-
pH 8.0, 30C, recombinant Csk residue-339-deletion mutant
-
additional information
additional information
-
the overall activity kcat of the catalytic domain Src, Src-CD, including the C-terminal tail for two exogenous substrates, the Src substrate peptide AEEEIYGEFEAKKKK and denatured enolase is about 10 times higher than that of wild-type Src. The kcat values for phosphorylation of the Src substrate peptide are similar for the unphosphorylated and monophosphorylated Src-CD, 50 min-1, but the apparent Km values differ significantly, approximately 0.003 mM and 0.010 mM, respectively
-
additional information
additional information
-
c-Src, Csk: random kinetic mechanism, reaction kinetic can be influenced by the sort of substrate, high affinity for ADP
-
additional information
additional information
-
-
-
additional information
additional information
-
kinetics
-
additional information
additional information
Abelson leukaemia virus
-
thermodynamics
-
additional information
additional information
-
-
-
additional information
additional information
-
BTK steady state kinetics, kinetic mechanism, wild-type BTK and mutant Y551F
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.16
ATP
-
pH 8.0, 30C, recombinant mutant H384Y/Y416F
0.21
ATP
-
pH 8.0, 30C, recombinant mutant H384A
0.4
ATP
-
pH 8.0, 30C, recombinant mutant H384Q/Y416F
0.53
ATP
-
pH 8.0, 30C, recombinant mutant H384Y
0.98
ATP
-
pH 8.0, 30C, recombinant mutant H384Y/Y527F
1.93
ATP
-
pH 8.0, 30C, recombinant mutant H384Q
3.13
ATP
-
pH 8.0, 30C, recombinant wild-type enzyme
3.52
ATP
-
pH 8.0, 30C, recombinant wild-type enzyme
55
ATP
-
-
0.072
EEEEY
-
pH 8.0, 30C, recombinant mutant H384Y/Y416F
0.1
EEEEY
-
pH 8.0, 30C, recombinant mutant H384A
0.15
EEEEY
-
pH 8.0, 30C, recombinant mutant H384Q/Y416F
0.22
EEEEY
-
pH 8.0, 30C, recombinant mutant H384Y
0.43
EEEEY
-
pH 8.0, 30C, recombinant mutant H384Y/Y527F
0.8
EEEEY
-
pH 8.0, 30C, recombinant mutant H384Q
2.27
EEEEY
-
pH 8.0, 30C, recombinant wild-type enzyme
396
EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
-
-
0.35
kdSrc kinase
-
pH 8.0, 30C, recombinant Csk residue-339-deletion mutant
-
0.82
kdSrc kinase
-
pH 8.0, 30C, recombinant mutant E338A Csk
-
0.01
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant Csk residue-339-deletion mutant
0.1
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant mutant E338A Csk
0.57
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant wild-type Csk
1.49
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant wild-type enzyme
1.85
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant mutant S280A/R281A/R283A/F381A
2.07
poly(Glu4-Tyr)
-
pH 8.0, 30C, recombinant mutant R281A/R283A
0.11
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant mutant R281A/R283A
-
0.13
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant mutant S280A/R281A/R283A/F381A
-
0.9
[kdSrc kinase]-L-tyrosine
-
pH 8.0, 30C, recombinant wild-type enzyme
-
1.88
kdSrc kinase
-
pH 8.0, 30C, recombinant wild-type Csk
-
additional information
additional information
-
the overall activity kcat of the catalytic domain Src, Src-CD, including the C-terminal tail for two exogenous substrates, the Src substrate peptide AEEEIYGEFEAKKKK and denatured enolase is about 10 times higher than that of wild-type Src. The kcat values for phosphorylation of the Src substrate peptide are similar for the unphosphorylated and monophosphorylated Src-CD, 50 min-1
-
additional information
additional information
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00001
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
0.000004
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
0.000032
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
0.000169
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.00076
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000272
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000718
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000406
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.0009
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000272
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.00126
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000083
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000219
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.00021
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
0.000009
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
0.000022
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
0.00005
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
0.000026
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
0.000044
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
0.000073
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000195
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000064
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000217
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000104
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.0002
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000189
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000199
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000092
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000165
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000167
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000569
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000044
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000354
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000195
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.000263
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.00017
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.00021
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
0.001817
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.1414
AcpYEEI
-
30C, Src
-
0.0026
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
-
30C, Src
-
0.03
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0017
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.0253
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0161
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.0426
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0158
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.0472
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0115
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.0455
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0141
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.0355
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0101
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Src
-
0.1078
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
-
30C, Lck
-
0.0571
ATP-gamma-S
-
30C, Src
0.000013
imatinib
-
-
0.000014
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000008
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000056
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000023
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000082
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00063
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
-
0.000028
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.000023
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00011
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
0.00092
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
0.001137
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
0.00007
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.000334
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.0004
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.000464
N-[5-(benzylsulfanyl)-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.000247
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
0.000369
N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
0.000225
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
0.000522
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-2-chlorobenzamide
-
-
0.000047
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.000217
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-chlorobenzamide
-
-
0.000089
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
0.000221
N-[5-[(4-bromobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-4-fluorobenzamide
-
-
0.000033
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
0.00001
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
-
0.0031
imatinib
-
-
additional information
additional information
-
-
-
additional information
additional information
-
substrate inhibition kinetics and analysis
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0355
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
0.02049
2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
-
0.00000129
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine