Information on EC 2.7.10.2 - non-specific protein-tyrosine kinase and Organism(s) Mus musculus and UniProt Accession P05480

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Mus musculus
UNIPROT: P05480


The taxonomic range for the selected organisms is: Mus musculus

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.10.2
-
RECOMMENDED NAME
GeneOntology No.
non-specific protein-tyrosine kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
residue W1038 is essential for catalytic activity
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
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].
CAS REGISTRY NUMBER
COMMENTARY hide
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 hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
ATP + Akt tyrosine kinase
ADP + phosphotyrosinyl-Akt
show the reaction diagram
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 + Cbp
? + ADP
show the reaction diagram
-
murine Csk binding protein, Cbp, amino acids 74-474, substrate used in kinase activity assay
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
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 + KVEKIGEGTYGVVYK
? + ADP
show the reaction diagram
-
substrate peptide used in kinase activity assay, derived from p34cdc2
-
-
?
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 + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
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 + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + [disabled-1 adaptor protein]-L-tyrosine
ADP + [disabled-1 adaptor protein]-L-tyrosine phosphate
show the reaction diagram
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 + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
O70146
role for this kinase in spermatogenesis
-
-
-
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
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, 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 + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
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 + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
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 + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
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 + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
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
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
dependent on, PYK2 is involved in Ca2+ mobilization in muscle cells
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
4-(2-fluoro-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
-
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
-
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(isopropylamino)-9H-carbazole-1-carboxamide
-
-
4-(3-(5-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-(3-(5-fluoropicolinamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
-
-
4-(3-(6-fluoro-1-oxoisoindolin-2-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-(3-(6-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-(3-(7-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-(3-(8-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine
-
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
-
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
-
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-9H-carbazole-1-carboxamide
-
-
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
-
7-(2-hydroxypropan-2-yl)-4-(3-(4-oxoquinazolin-3(4H)-yl)-phenyl)-9H-carbazole-1-carboxamide
-
-
7-(2-hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide
-
BMS-935177
7-(hydroxymethyl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide
-
-
A-419259
-
high inhibition of SFKs
-
AMP-PNP
-
-
AZD-1480
-
Jak2 inhibitor
AZM 475271
-
-
bosutinib
-
previously SKI-606, inhibits ABL1
CGP 76030
-
-
CGP 77675
-
-
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690,550
-
has nanomolar potency in in vitro JAK2 and JAK3 kinase assays
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
dasatinib
geldanamycin
-
indirect pharmacological inhibitor
Gleevec
-
also known as STI-571 or imatinib
ibrutinib
-
-
imatinib
INCB018424
-
Jak2 inhibitor
INCB18424
-
Incyte
INNO-406
-
previously NS-187, inhibits ABL1
interferon-gamma
-
enzyme inhibition in leukemic bone marrow cells
-
ITF2357
-
Jak2 inhibitor
lestaurtinib
LFM-A13
LS104
-
Jak2 inhibitor
M 475271
-
-
MK-0457
-
Jak2 inhibitor
nilotinib
-
potent ABL1 inhibitor
PC-005
-
-
-
PCI-31523
-
-
peroxiredoxin 1
-
inhibits ABL1 intracellularly
-
piceatannol
PIP2
-
inhibits ABL1 intracellularly
PNU156804
-
Jak3 inhibitor
SB1518
-
Jak2 inhibitor
shRNA
-
-
-
siRNA
-
-
-
SKI-606
-
-
Src kinase inhibitor-1
-
i.e. SKI-1, a 4-anilinoquinazoline, moderate inhibition in vitro and vivo
-
SU-6656
-
-
SU6656
TG101209
-
Jak2 inhibitor
TG101348
-
Jak2 inhibitor
tyrphostin AG490
-
Jak3 inhibitor
WHI-P131
-
Jak3 inhibitor
WHI-P154
-
Jak3 inhibitor
XL019
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
CX3CL1
-
i.e. fractalkine, only member of the delta subclass of chemokines, induces Syk activity in cytoskeletal remodeling
-
cytokine receptors
-
-
-
erythropoietin
-
activates Fps/Fes tyrosine kinase
-
interleukin-2
-
enzyme activation in leukemic bone marrow cells
-
N,N'-ethylnitrosourea
-
enzyme activation in leukemic bone marrow cells
non-specific BRM sheep erythrocyte
-
BRM is biological response modifier, treatment leads to a slight enzyme activation in leukemic bone marrow cells
-
Reelin
-
extracellular, stimulates disabled-1 adaptor protein Dab1 tyrosine phosphorylation by Src family PTKs, downregulates Dab1 expression in vivo
-
stem cell factor SCF
-
activates Fps/Fes tyrosine kinase
-
tyrosine growth factor
-
the enzyme is activated by the tyrosine growth factor and seven transmembrane-spanning receptors
-
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000004
4-(2-fluoro-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000005
4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000005
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000011
4-(3-(4-fluorobenzamido)-2-methylphenyl)-7-(isopropylamino)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000005
4-(3-(5-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000009
4-(3-(5-fluoropicolinamido)-2-methylphenyl)-7-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000002
4-(3-(6-fluoro-1-oxoisoindolin-2-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000007
4-(3-(6-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000002
4-(3-(7-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000002
4-(3-(8-fluoro-4-oxoquinazolin-3(4H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000009
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
Mus musculus;
-
substrate Csk binding protein, Cbp
0.000003
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxo-3,4-dihydroisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000005
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoindolin-2-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000005
7-(2-hydroxypropan-2-yl)-4-(2-methyl-3-(1-oxoisoquinolin-2(1H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000044
7-(2-hydroxypropan-2-yl)-4-(3-(4-oxoquinazolin-3(4H)-yl)-phenyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000003
7-(2-hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000003
7-(hydroxymethyl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide
Mus musculus;
-
at pH 7.4 and 22C
0.000011
dasatinib
Mus musculus;
-
substrate Csk binding protein, Cbp
0.0000172
LFM-A13
Mus musculus;
-
-
0.000035
SU6656
Mus musculus;
-
substrate Csk binding protein, Cbp
additional information
additional information
Mus musculus;
-
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
-
in vitro c-Src kinase activity assay
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
30
-
kinase assay
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
lining of the alimentary canal
Manually annotated by BRENDA team
-
endothelial cells, PYK2
Manually annotated by BRENDA team
-
upregulated expression of syk is observed in aggressive, metastasizing mammary gland tumours but not in well differentiated, non-metastasizing tumors
Manually annotated by BRENDA team
expressed only in epithelial tissues, including the skin and lining of the alimentary canal
Manually annotated by BRENDA team
-
peripheral, in bone marrow and spleen, Fps/Fes tyrosine kinase expression in early erythroid progenitors/blasts and in mature red cells
Manually annotated by BRENDA team
-
ES cell D3 line, embryonic stem cell, expression of 7 different Src family kinases, 3 are involved in differentiation to embryoid bodies
Manually annotated by BRENDA team
-
retinal ganglion cell layer and the inner part of the inner nuclear layer. During retinal development, JAK1 protein is first detected in retinal ganglion cells and in their axons as early as embryonic day 14. Expression of JAK1 protein in amacrine cells and horizontal cells occurrs only postnatally
Manually annotated by BRENDA team
-
faintly
Manually annotated by BRENDA team
-
HL-1 cardiomyocyte
Manually annotated by BRENDA team
intestinal crypt cells
Manually annotated by BRENDA team
-
spinal microglia
Manually annotated by BRENDA team
-
faintly
Manually annotated by BRENDA team
-
derived from monocyte/macrophage cell line RAW 264.7
Manually annotated by BRENDA team
-
adult CD4-CD8-thymocytes
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
UNIPROT
ORGANISM
P05480
Mus musculus;
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
53000
-
alternative splicing variant, identified by SDS-PAGE and Western blot analysis
56000
-
identified by SDS-PAGE and Western blot analysis
60000
-
determined by SDS-PAGE and Western Blot analysis
60630
-
calculation from nucleotide sequence
75000
-
x * 75000, about, Syk, SDS-PAGE
87000
-
x * 87000, SDS-PAGE
130000
-
approximately
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
acetylation
-
normal activation of the ABL1 proteins requires acetylation
acylation
-
normal activation of the ABL1 proteins requires myristoylation
phosphoprotein
side-chain modification
additional information
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
crystal structure of the extracellular ligand-binding domain of the type II activin receptor
-
determination of the three-dimensional solution structure of the SH2 domain of blk kinase by nuclear magnetic resonance NMR spectroscopy
-
hanging drop vapor diffusion method, using 31% (w/v) methyl ether PEG 5000, 1% (w/v) PEG 8000, 0.2 M Tris-HCl, pH 8.5
-
high-resolution crystal structures of the complexes between the SH3 domains of Abl and Fyn tyrosine kinases, and two ten-residue proline-rich peptides derived from the SH3-binding proteins 3BP-1 and 3BP-2
-
in complex with gleevec
-
the crystal structures of the kinase domain of Lyn are determined in complex with three different inhibitors, AMP-PNP, 4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine and dasatinib, as well as the non-liganded form of the enzyme, at 2.5 to 2.7 A resolution
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
protein extracts from cells, transfected with plasmids containing the HCN4 gene, are prepared
-
using nickel-chelating resin, a HiTrap Q column and gel filtration
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
isolation of a c-src cDNA clone
; maps to the distal end of chromosome 2
-
application of the polymerase chain reaction to cloning
-
expression in COS cells
-
expression in Escherichia coli
expression of Abl in NIH 3T3 cells and in HEK-293 cells
-
expression of SFKs Hck, Fyn, Lck, and Yes in human 293T cells, expression of N-terminally His-tagged Hck in Spodoptera frugiperda Sf9 cells via baculovirus infection system
-
four new activin receptor isoforms
genetic analysis of mutations causing cell cycle deregulation, e.g. in mice lacking cyclin-D2, heterozygous D2+/- mice are resistant to BCR/ABL-induced proliferation, overview
-
isolation and structural analysis of murine c-fes cDNA clones
-
isolation of cDNA
-
Jak2, DNA and amino acid sequence determination and analysis, oc-expression of wild-type Jak2 with increasing amounts of mutant W1038G/E1024A or mutant W1038G/E1024R, the latter is more potent in reducing wild-type enzyme actiivty in a dominant-negative way, overview
lskT gene is rearranged and overexpressed in the murine T cell lymphoma LSTRA
-
retroviral expression in 293T cells prior to infection of RAW cells for stable Syk expression
-
Tec gene consists of 18 exons and spans more than 86 kb
-
Tec gene is tightly linked to the c-Kit gene on chromosome 5
-
testis-specific c-abl mRNAs arise as a result of 3' truncation. The v-abl gene has arisen from its cellular homologue as a result of an extensive deletional/mutational process
-
the murine Lyn kinase domain, amino acids 239-512, is subcloned into the baculovirus expression vector pFastBacHTA generating a His6-tagged fusion resulting in a 5 amino acid N-terminal extension to the Lyn kinase domain after tobacco etch virus cleavage
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the retroviral vector pMX-Tec-IRES-GFP is constructed
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the retroviral vectors pMX-Btk-IRES-GFP, pMX-Btk(R28C)-IRES-GFP and pMX-Btk(R525Q)-IRES-GFP are constructed
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two isoforms of murine hck, generated by utilization of alternative translational initiation codons
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
isoform Btk expression is up-regulated during maturation and activation of mouse natural killer cells
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K273R
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mutant protein is unable to transfer the gamma-phosphate of ATP but able to bind 8-azido-ATP with an efficiency similar to that of wild-type pp56lck
W1038G/E1046A
site-directed mutagenesis, an inactive dominant-negative mutant, construction of transgenic mice, heterologous mutants show reduced enzyme activity and an unaltered phenotype, overview
W1038G/E1046R
site-directed mutagenesis, an inactive dominant-negative mutant, construction of transgenic mice, heterologous mutants show reduced enzyme activity and an unaltered phenotype, overview
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
pharmacology
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the enzyme is a pharmaceutical target for inhibitors in therapy of acute inflammatory responses, e.g. acute lung injury, ischemic brain injury, brain injury, spinal cord compression, stroke, and myocardial infarction, detailed overview