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Literature summary for 2.7.11.1 extracted from

  • Kim, J.; Son, J.; Jang, Y.; Lee, D.; Kang, N.; Jung, S.; Heo, Y.; Lee, K.; Lee, H.
    Luteolin, a novel natural inhibitor of tumor progression locus 2 serine/threonine kinase, inhibits tumor necrosis factor-alpha-induced cyclooxygenase-2 expression in JB6 mouse epidermis cells (2011), J. Pharmacol. Exp. Ther., 338, 1013-1022.
    View publication on PubMed
Search for more literature for 2.7.11.1

Inhibitors

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

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein phosphorylation of TPL2 is increased by luteolin treatment and inhibits the enzyme activity Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
epidermis
-
 Mus musculus
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JB6 cell tumour-promotion-sensitive P+ Mus musculus
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
TPL2
-
 Mus musculus
tumor progression locus 2 serine/threonine kinase
-
 Mus musculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Mus musculus

Cofactor

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

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