Inhibitors | Comment | Organism | Structure |
---|---|---|---|
luteolin | i.e. 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4-chromenone, directly inhibits TPL2 activity, luteolin binds to TPL2 in an ATP-competitive manner, binding mode of luteolin, molecular modeling and docking study, overview. Luteolin easily docks to the ATP binding site of TPL2, which is located between the N-lobe and C-lobe of the kinase domain. In a cellular system, phosphorylation of TPL2 is increased by luteolin treatment, and luteolin suppresses TNF-alpha-induced TPL2 activity in JB6 P+ cells | Mus musculus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | phosphorylation of TPL2 is increased by luteolin treatment and inhibits the enzyme activity | Mus musculus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
epidermis | - |
Mus musculus | - |
JB6 cell | tumour-promotion-sensitive P+ | Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + myelin basic protein | - |
Mus musculus | ADP + phosphorylated myelin basic protein | - |
? | |
additional information | TPL2 inhibitor suppresses MEK/ERK/p90RSK, MKK4/JNK/c-Jun, and Akt/p70S6K, whereas the phosphorylation of p38 is unchanged | Mus musculus | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
TPL2 | - |
Mus musculus |
tumor progression locus 2 serine/threonine kinase | - |
Mus musculus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Mus musculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | the ATP binding site of TPL2 is located between the N-lobe and C-lobe of the kinase domain | Mus musculus |
General Information | Comment | Organism |
---|---|---|
malfunction | TPL2 inhibitor suppresses MEK/ERK/p90RSK, MKK4/JNK/c-Jun, and Akt/p70S6K, whereas the phosphorylation of p38 is unchanged | Mus musculus |
additional information | molecular modeling, docking study and structural analysis, homology model for TPL2, overview | Mus musculus |
physiological function | TPL2 regulates MEK and MKK4 without affecting p38 in the TNF-alpha-induced signaling pathway. TPL2 is involved in TNF-alpha-induced COX-2 upregulation | Mus musculus |