Information on EC 2.7.10.1 - receptor protein-tyrosine kinase and Organism(s) Mus musculus and UniProt Accession Q03526

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Mus musculus
UNIPROT: Q03526


The taxonomic range for the selected organisms is: Mus musculus

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.10.1
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RECOMMENDED NAME
GeneOntology No.
receptor protein-tyrosine kinase
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
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-
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SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (receptor-type)
The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in Metazoans [1]. In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies.
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + cortactin-L-tyrosine
ADP + cortactin-L-tyrosine phosphate
show the reaction diagram
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-
-
-
?
ATP + insulin receptor substrate 1-L-tyrosine
ADP + insulin receptor substrate 1-L-tyrosine phosphate
show the reaction diagram
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-
tyrosine phosphorylation of insulin receptor substrate-1 by insulin receptor is decreased when insulin receptor substrate-1 is contained in high-molecular mass complexes prepared from 3T3-L1 adipocytes treated with tumor necrosis factor-alpha. Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
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?
ATP + p130Cas-L-tyrosine
ADP + p130Cas-L-tyrosine phosphate
show the reaction diagram
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-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + phospholipase C gamma-L-tyrosine
ADP + phospholipase C gamma-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
ATP + protein tyrosine
ADP + protein tyrosine phosphate
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]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + cortactin-L-tyrosine
ADP + cortactin-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + p130Cas-L-tyrosine
ADP + p130Cas-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + paxillin-L-tyrosine
ADP + paxillin-L-tyrosine phosphate
show the reaction diagram
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-
-
-
?
ATP + phospholipase C gamma-L-tyrosine
ADP + phospholipase C gamma-L-tyrosine phosphate
show the reaction diagram
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-
-
-
?
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
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IC50: 97 nM; IC50: less than 2 nM
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
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IC50: 3 nM; IC50: less than 2 nM
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
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IC50: 2 nM; IC50: less than 2 nM
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
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IC50: 2 nM; IC50: 327 nM
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
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IC50: 19 nM; IC50: 2580 nM
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
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IC50: 191 nM; IC50: 22 nM
3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one
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dynamin K44A
inhibits agrin-induced MuSK endocytosis
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genistein
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Herbimycin
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herceptin
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humanized monoclonal antibody
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significantly decreases tumor growth of murine xenografts from subcutaneously injected lung, colon, and pancreatic cancer cell lines in nude mice
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N-(4-chlorophenyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
dose dependent inhibition of Flk-1 phosphorylation
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
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IC50: 35 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole; IC50: 4 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole
PD153035
inhibits tyrosine kinase activity of EGFR and whereby blocks cellular responses of activated ErbB3. It inhibits heregulin-induced VEGFA expression
PKI-166
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protein tyrosine phosphatase 1B
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PTP1B, negative regulator of Met. Loss of protein tyrosine phosphatase 1B enhances heregulin-mediated phosphorylation of Met. Interaction with Met requires phosphorylation of twin tyrosines (Y1234/35) in the activation loop of the Met kinase domain
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rottlerin
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specific inhibitor of PKCdelta
shRNA
sh-ErbB3 cells normally metastasize to the lung, but the heregulin-induced increase in metastasis is completely abrogated. Inactivation of ErbB3 by shRNA does not directly influence the formation of metastatic colonies in the experimental metastasis model, although heregulin-induced enhancement is completely dependent on ErbB3. However, spontaneous metastasis by inoculating the cells without heregulin stimulation into the foot pad is significantly decreased
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siRNA
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sorafenib
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oral multikinase inhibitor, inhibits receptor tyrosine kinase autophosphorylation
Spry protein
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additional information
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
12-O-tetradecanoylphorbol-13-acetate
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upregulates Ron protein expression
agrin
MuSK becomes rapidly internalized in response to agrin, which appears to be required for induced acetylcholine receptor clustering
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capsaicin
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c-kit receptor expression is significantly up-regulated in medium-sized dorsal root ganglia neurons after neonatal capsaicin treatment
fibroblast growth factor
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activation occurs by phosphorylation on residues 653 and 654
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heregulin
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macrophage-stimulating protein
the ligand for RON, inhibits IFN-gamma-induced STAT1 phosphorylation and CIITA expression, resulting in reduced surface levels of MHC class II
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N-ethylmaleimide sensitive factor
an appropriate level of N-ethylmaleimide sensitive factor and its ATPase activity may be required for MuSK endocytosis and subsequent activation
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PorB
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PorB from Neisseria meningitidis is able to induce protein tyrosine kinase activity
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stem cell factor
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soluble and membrane-bound glycoprotein, activating ligand of the stem cell receptor i.e. the Kit protein-tyrosine kinase
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tumor necrosis factor-alpha
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tyrosine phosphorylation of insulin receptor substrate-1 by insulin receptor is decreased when insulin receptor substrate-1 is contained in high-molecular mass complexes prepared from 3T3-L1 adipocytes treated with tumor necrosis factor-alpha.Cytokine/hormone-induced formation of high-molecular mass complexes modulates availability of insulin receptor substrates to receptor tyrosine kinases
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additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000002 - 0.000097
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000002 - 0.000003
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000002
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
Mus musculus
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IC50: 2 nM; IC50: less than 2 nM
0.000002 - 0.000327
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000019 - 0.00258
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000022 - 0.000191
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000004 - 0.000035
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
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exclusively expressed in T lymphocytes
Manually annotated by BRENDA team
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increase in thymus during development from neonate to adult. Tsk is expressed in day 14 fetal thymus
Manually annotated by BRENDA team
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only one out of seven mature B cell lines expressed ltk and the in vitro maturation of pre-B into B cells is in one case accompanied by the inactivation of ltk expression
Manually annotated by BRENDA team
overexpression of functional ErbB3
Manually annotated by BRENDA team
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endothelium of blood vessel
Manually annotated by BRENDA team
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ossification centers of developing bone
Manually annotated by BRENDA team
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3LL carcinoma and T10 sarcoma, overexpression of PDGF-alpha receptor in high-metastatic clones
Manually annotated by BRENDA team
inner ear, expressed in the developing and adult cochlea
Manually annotated by BRENDA team
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in tissue surrounding the esophagus
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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expressed in definitive endoderm of the developing gut and extraembryonic endoderm of the yolk-sac from 8.5 to 14.5 days p.c.
Manually annotated by BRENDA team
in resting J774, scavenger receptor A is associated minimally with unphosphorylated (monomeric) Mertk
Manually annotated by BRENDA team
expressed at high levels in the hippocampus, tenia tecta, indusium griseum, and the piriform cortex, major components of the limbic system
Manually annotated by BRENDA team
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BAC1.2F5 macrophage cell line
Manually annotated by BRENDA team
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expression is induced during the proliferation of the mammary gland and down-regulated by its differentiation
Manually annotated by BRENDA team
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mature
Manually annotated by BRENDA team
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which surrounds the developing neuroepithelium
Manually annotated by BRENDA team
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C1300 cells
Manually annotated by BRENDA team
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of the neural tube of 10-day-old embryos
Manually annotated by BRENDA team
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; 4964LM cell; 4964PDA cell; 5143LM cell; 5143PDA cell
Manually annotated by BRENDA team
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the c-fms protooncogene, is selectively expressed in immature and mature mononuclear phagocytes and trophoblasts
Manually annotated by BRENDA team
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lymphoid ltk uses a CUG translational start codon and has a 110 amino acid putative extracellular domain. The predominant ltk mRNA in brain is alternatively spliced and predicts a protein with a substantially larger extracellular part
Manually annotated by BRENDA team
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3LL carcinoma and T10 sarcoma, overexpression of PDGF-alpha receptor in high-metastatic clones
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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postmeiotic male germ cells
Manually annotated by BRENDA team
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expression in CD3-T cells, CD4-T cells and CD8-T cells at a low level
Manually annotated by BRENDA team
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the c-fms protooncogene, is selectively expressed in immature and mature mononuclear phagocytes and trophoblasts
Manually annotated by BRENDA team
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paravertebral trunk of the sympathetic nervous system
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
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CD3epsilon chain induces the membrane colocalization of Emt/Itk with TCR/CD3
Manually annotated by BRENDA team
cell membrane-associated expression of HER2 significantly augments during the differentiation of preadipocytes
Manually annotated by BRENDA team
additional information
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two alternatively spliced mouse lymphocyte and brain ltk cDNAs predict small transmembrane tyrosine kinases that use CUG translational start codons and that differ upstream of their transmembrane segment. A human neuroblastoma ltk cDNA, includes a regular AUG start codon and predicts a more conventional receptor kinase with a larger N-terminal segment
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Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
72000
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35000
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1 * 150000 + 1 * 35000
66000
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SDS-PAGE
80000
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full-length enzyme, SDS-PAGE
109001
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x * 109001, calculation from nucleotide sequence
120000
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SDS-PAGE
130000
140000
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145000
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150000
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1 * 150000 + 1 * 35000
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
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x * 109001, calculation from nucleotide sequence
heterodimer
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1 * 150000 + 1 * 35000
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
glycoprotein
phosphoprotein
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
conotoxin IMI Sepharose affinity chromatography
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
; DTK gene maps to mouse chromosome 2, band F
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; endothelial-specific gene expression directed by the tie gene promoter in vivo
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a chimeric receptor consisting of the extracellular domain of insulin receptor and the intracellular domain of IRR is expressed in Chinese hamster ovary cells
application of the polymerase chain reaction to cloning
bacterially expressed gst-Sek kinase domain fusion protein autophosphorylated exclusively on tyrosine residues
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bek cDNA expression in receptor-negative Chinese hamster ovary cells and in 32D myeloid cells
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cDNA introduced into COS cells
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cloning and sequencing of the extracellular ligand binding domain of murine EGF-R
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cloning of a c-kit mRNA of 3.2 kb expressed in postmeiotic male germ cells
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coexpression of HA-tagged MuSK with Myc-tagged N-ethylmaleimide sensitive factor wild-type or mutant constructs in HEK-293 cells
determination of the primary structure of murine c-kit from a DNA clone isolated from a brain cDNA library
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expression cDNA cloning of the KGF receptor by creation of a transforming autocrine loop
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expression in CHO cells
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expression in Cos-1 cells
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expression in NIH3T3 cells
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fibroblast growth factor receptor 1 gene generates multiple messenger RNAs containing two open reading frames via alternative splicing
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gene is located on chromosome 6
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identification of the gene
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isolation of a full-length cDNA, encoding the mouse homologue of a previous by partially characterized Eek protein
isolation of cDNA
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isolation of mouse cDNA clones encoding Tyro 3
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leucine-rich motifs in TrkB are essential for ligand binding and signaling
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localized to chromosome 9
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maps to chromosome 4
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stable expression of wild-type and constitutively active murine Ron mutants in NIH3T3 mouse fibrobalst cells
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tek, which maps to mouse chromosome 4 between the brown and pmv-23 loci
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the c-fms clone is inserted into a retroviral vector containing a neomycin resistance gene and cell lines resistant to G418 are isolated, that express the protein
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translation of Jak2 mRNA in rabbit reticulocytes
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
high levels of epidermal growth factor receptor are expressed in response to exogenous epidermal growth factor
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D1232V
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is more active than the wild-type, produces tumors in nude mice and is highly metastatic
D314N
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no activity
DELTA(T573-H579)
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c-Kit mutant, juxtamembrane mutation
M1231T
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equivalent tumor latency and 100% tumor formation as the wild-type
M1254T
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is more active than the wild-type, produces tumors in nude mice and is highly metastatic
R318A
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no activity
Y719F
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c-Kit mutant, knock-in mouse, which does not show an apparent abnormality in hematopoiesis
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
medicine
additional information