Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | constitutive activation of RTKs is provoked by several mechanisms including chromosomal translocations and various mutations involving their regulatory regions. Missense, insertion or deletion mutations in the regulatory regions, such as juxtamembrane domain, activation loop, and extracellular domain, also cause constitutive activation of RTKs mainly by preventing the auto-inhibitory regulation | Homo sapiens |
Application | Comment | Organism |
---|---|---|
medicine | patients with PDGFRbeta rearrangement reveal common clinical features resembling chronic myelogenous leukemia or chronic myelomonocytic leukemia. FGFR3 is involved peripheral T cell lymphoma | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D816F | c-Kit mutant, in patients with aggressive mastocytosis or AML patients | Homo sapiens |
D816H | c-Kit mutant, in patients with aggressive mastocytosis or AML patients | Homo sapiens |
D816V | c-Kit mutant, in patients with aggressive mastocytosis or AML patients | Homo sapiens |
D816V | FLT3 mutant, in 7% of AML patients | Homo sapiens |
D816Y | c-Kit mutant, in patients with aggressive mastocytosis or AML patients | Homo sapiens |
D835Y | FLT3 mutant, in 7% of AML patients | Homo sapiens |
DELTA(T573-H579) | c-Kit mutant, juxtamembrane mutation | Mus musculus |
K650E | FGFR3 mutant, activating mutation | Homo sapiens |
additional information | c-Kit mutant, juxtamembrane mutation | Canis lupus familiaris |
additional information | c-Kit mutants harboring extracellular domain mutations are not constitutively active, whereas extracellular domain mutants of c-FMS are constitutively active and oncogenic. Extracellular domain mutation of FGFR disturbs the autoinhibitory mechanism, resulting in constitutive acitvation | Homo sapiens |
V560G | c-Kit mutant, juxtamembrane mutation | Homo sapiens |
Y719F | c-Kit mutant, does not abolish kinase activity | Homo sapiens |
Y719F | c-Kit mutant, knock-in mouse, which does not show an apparent abnormality in hematopoiesis | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
CEP701 | inhibits FLT3 | Homo sapiens | |
imatinib | inhibits c-Kit and PDGFR | Homo sapiens | |
MLN518 | inhibits FLT3 | Homo sapiens | |
PKC412 | inhibits FLT3 | Homo sapiens | |
SU11248 | inhibits FLT3 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | RTKs consist of an extracellular ligand-binding domain, a transmembrane domain, a highly conserved intracellular kinase domain and a C-terminal tail | Homo sapiens | 16020 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Canis lupus familiaris | O97799 | - |
- |
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
FM3A cell | - |
Mus musculus | - |
HMC-1 cell | - |
Homo sapiens | - |
additional information | mast cell tumor cell | Canis lupus familiaris | - |
Synonyms | Comment | Organism |
---|---|---|
c-fms | - |
Homo sapiens |
c-kit | - |
Mus musculus |
c-kit | - |
Homo sapiens |
c-kit | - |
Canis lupus familiaris |
CSF-1R | - |
Homo sapiens |
epidermal growth factor receptor | - |
Homo sapiens |
FGFR3 | - |
Homo sapiens |
fibroblast growth factor receptor | - |
Homo sapiens |
FLT3 | - |
Homo sapiens |
IGF-1 receptor | - |
Homo sapiens |
insulin-growth factor-1 receptor | - |
Homo sapiens |
PDGF receptor | - |
Homo sapiens |
PDGFRalpha | - |
Homo sapiens |
PDGFRbeta | - |
Homo sapiens |
platelet-derived growth factor receptor | - |
Homo sapiens |
receptor for macrophage colony-stimulating factor | - |
Homo sapiens |
receptor for stem cell factor | - |
Homo sapiens |
receptor tyrosine kinase | - |
Mus musculus |
receptor tyrosine kinase | - |
Homo sapiens |
receptor tyrosine kinase | - |
Canis lupus familiaris |
RTKs | - |
Mus musculus |
RTKs | - |
Homo sapiens |
RTKs | - |
Canis lupus familiaris |