Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | activated by phosphorylation | Homo sapiens |
Application | Comment | Organism |
---|---|---|
medicine | RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide | RO4927350 | Homo sapiens | |
FR180204 | ERK inhibitor, 5-(2-phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine | Homo sapiens | |
U0126 | MEK inhibitor | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | - |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
DU-145 cell | - |
Homo sapiens | - |
HT-29 cell | - |
Homo sapiens | - |
LOX cell | - |
Homo sapiens | - |
MCF-7 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
ATP + FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2 | FITC-labeled ERK substrate peptide | Homo sapiens | ADP + phosphorylated FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ERK1/2 | - |
Homo sapiens |
MAP kinase | - |
Homo sapiens |
MEK1/2 | - |
Homo sapiens |
mitogen-activated kinase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
kinase assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
kinase assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000023 | - |
MEK1 | Homo sapiens | (2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide |
General Information | Comment | Organism |
---|---|---|
physiological function | the MAPK pathway, via the Ras/Raf/MEK/ERK signal cascade, is responsible for transmitting and amplifying mitogenic signals from the cell surface to the nucleus where activated transcription factors regulate gene expression and determine cell fate | Homo sapiens |