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Literature summary for 2.7.10.1 extracted from
- Receptor tyrosine kinases and anticancer therapy (2005), Curr. Pharm. Des., 11, 1139-1149.
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | the receptor protein tyrosine kinases are drug targets in specific treatment of tumor angiogenesis and cancer, e.g. gastrointestinal stromal tumors, drugs are such as gemcitabine, cisplatin, doxorubicin, or erlotinib | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| AZD2171 | inhibits VEGFR2 | Homo sapiens |  |
| CEP-7055 | inhibits VEGFR1-3 | Homo sapiens | |
| cisplatin | anti-cancer drug inhibiting receptor tyrosine kinases | Homo sapiens | |
| doxorubicin | anti-cancer drug inhibiting receptor tyrosine kinases | Homo sapiens | |
| erlotinib | anti-cancer drug inhibiting receptor tyrosine kinases | Homo sapiens | |
| gefitinib | i.e. ZD1839, highly specific inhibitor of EGFR tyrosine kinase and of HER1 tyrosine kinase, clinical effects, overview | Homo sapiens | |
| gemcitabine | anti-cancer drug inhibiting receptor tyrosine kinases | Homo sapiens | |
| imatinib | inhibits c-Kit receptor and PDGF receptor tyrosine kinases | Homo sapiens | |
| additional information | clinical effects of enzyme inhibitors as anti-cancer drugs, overview, inhibitory antibodies, overview | Homo sapiens | |
| SU 11248 | inhibits VEGFR2 | Homo sapiens | |
| SU 6668 | inhibits VEGFR2 and PDGF receptor beta | Homo sapiens | |
| vatalanib | i.e. ZK 222584 or PTK 787, inhibits VEGFR1-3 | Homo sapiens | |
| ZD6474 | inhibits VEGFR2 | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | - |
Homo sapiens | 16020 | - |
| plasma membrane | EGFR tyrosine kinase, Her1 tyrosine kinase, ErbB1 tyrosine kinase | Homo sapiens | 5886 | - |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 170000 | - |
x * 170000, EGFR | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | the receptor protein tyrosine kinases are involved in cell signaling processes and signal transduction pathways in regulation of cell growth, differentiation, migration and metabolism by catalyzing protein phosphorylation and dephosphorylation, overview, EGFR tyrosine kinase regulates cell proliferation, IGFR tyrosine kinase regulates cell survival, VEGFR tyrosine kinase regulates tumor angiogenesis, mechanisms, overexpression of receptor protein tyrosine kinases in cancers | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| glycoprotein | EGFR | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| breast cancer cell | overexpression of Her2-receptor | Homo sapiens | - |
| colorectal cancer cell | overexpression of VEGFR1-3 | Homo sapiens | - |
| gastrointestinal tract | - |
Homo sapiens | - |
| glioblastoma cell | - |
Homo sapiens | - |
| additional information | EGFR is overexpressed in different cancers, overview | Homo sapiens | - |
| non-small cell lung cancer cell | - |
Homo sapiens | - |
| ovarian cancer cell | - |
Homo sapiens | - |
| pancreatic cancer cell | - |
Homo sapiens | - |
| squamous cell carcinoma cell | head and neck | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | the receptor protein tyrosine kinases are involved in cell signaling processes and signal transduction pathways in regulation of cell growth, differentiation, migration and metabolism by catalyzing protein phosphorylation and dephosphorylation, overview, EGFR tyrosine kinase regulates cell proliferation, IGFR tyrosine kinase regulates cell survival, VEGFR tyrosine kinase regulates tumor angiogenesis, mechanisms, overexpression of receptor protein tyrosine kinases in cancers | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 170000, EGFR | Homo sapiens |
| More | domain structure of EGFR | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| c-Kit receptor tyrosine kinase | - |
Homo sapiens |
| EGFR tyrosine kinase | - |
Homo sapiens |
| epidermal growth factor receptor | - |
Homo sapiens |
| ErbB1 tyrosine kinase | - |
Homo sapiens |
| Her1 tyrosine kinase | - |
Homo sapiens |
| IGFR tyrosine kinase | - |
Homo sapiens |
| More | EGFR tyrosine kinase, Her1 tyrosine kinase, ErbB1 tyrosine kinase are part of the plasma membrane receptor tyrosine kinase family | Homo sapiens |
| receptor protein tyrosine kinase | - |
Homo sapiens |
| vascular endothelial growth factor receptor | - |
Homo sapiens |
| vascular endothelial growth factor receptor tyrosine kinase | - |
Homo sapiens |
| VEGF factor receptor tyrosine kinase | - |
Homo sapiens |
| VEGFR tyrosine kinase | - |
Homo sapiens |
| VEGFR1-3 | - |
Homo sapiens |
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