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Literature summary for 2.7.11.25 extracted from

  • Xu, B.E.; Stippec, S.; Lenertz, L.; Lee, B.H.; Zhang, W.; Lee, Y.K.; Cobb, M.H.
    WNK1 activates ERK5 by an MEKK2/3-dependent mechanism (2004), J. Biol. Chem., 279, 7826-7831.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
additional information MEKK2 and MEKK3 are phosphorylated and thereby activated by kinase WNK1 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant MAP3Ks, MEKK1-4 and TAO2-1, in HEK293 cells, co-expression of ERK5 and WNK1 Homo sapiens

Protein Variants

Protein Variants Comment Organism
D169A site-directed mutagenesis, the kinase-dead mutation of TAO2-1 does not influence the ERK5 activation level Homo sapiens
K385M site-directed mutagenesis of MEKK2, inactive mutant enzyme Homo sapiens
K391M site-directed mutagenesis of MEKK3, inactive mutant enzyme Homo sapiens
additional information overexpression of WNK1 in HEK293 cells leads to increased enzyme activity, a kinase-dead mutation of MEKK1 does not influence the ERK5 activation level Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
U0126 inhibits MEKK2/MEKK3-dependent ERK5 phosphorylation/activation in vitro and in vivo Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + ERK5 Homo sapiens substrate of MEKK2 and MEKK3, activation of the ERK-dependent signaling pathway ADP + phosphorylated ERK5
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein MEKK2 and MEKK3 are phosphorylated at the N-terminus and thereby activated by kinase WNK1, residues K385 and K391, respectively, are involved Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + ERK5 substrate of MEKK2 and MEKK3, activation of the ERK-dependent signaling pathway Homo sapiens ADP + phosphorylated ERK5
-
?
ATP + ERK5 substrate of MEKK2 and MEKK3, no substrate of TAO2-1 Homo sapiens ADP + phosphorylated ERK5
-
?

Synonyms

Synonyms Comment Organism
MAP3K
-
Homo sapiens
MEKK2
-
Homo sapiens
MEKK3
-
Homo sapiens
TAO2-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens