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Literature summary for 2.7.11.20 extracted from

  • Kenney, J.W.; Genheden, M.; Moon, K.M.; Wang, X.; Foster, L.J.; Proud, C.G.
    Eukaryotic elongation factor 2 kinase regulates thesynthesis of microtubule-related proteins in neurons (2016), J. Neurochem., 136, 276-284.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
bicuculline elevation of eEF2K activity with bicuculline, a GABA receptor antagonist Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
JAN-384 a JAN-384 highly selective eEF2K inhibitor, comparison to inhibition of other protein kinases Mus musculus
JAN-452 slight inhibition Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
microtubule
-
Mus musculus 5874
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Mus musculus
Mg2+ required Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [elongation factor 2] Mus musculus phosphorylation at Thr56 ADP + [elongation factor 2] phosphate
-
?
ATP + [elongation factor 2] Mus musculus C57/BL6J phosphorylation at Thr56 ADP + [elongation factor 2] phosphate
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus O08796
-
-
Mus musculus C57/BL6J O08796
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neuron primary cortical neurons Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [elongation factor 2] phosphorylation at Thr56 Mus musculus ADP + [elongation factor 2] phosphate
-
?
ATP + [elongation factor 2] phosphorylation at Thr56 Mus musculus C57/BL6J ADP + [elongation factor 2] phosphate
-
?

Synonyms

Synonyms Comment Organism
eEF2K
-
Mus musculus
eukaryotic elongation factor 2 kinase
-
Mus musculus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
pH and temperature not specified in the publication Mus musculus JAN-384
0.03
-
pH and temperature not specified in the publication Mus musculus JAN-452

General Information

General Information Comment Organism
malfunction processes related to microtubules are particularly sensitive to eEF2K inhibition Mus musculus
physiological function eEF2K likely contributes to neuronal function by regulating the synthesis of microtubule-related proteins. Phosphorylation of elongation factor 2, EF2, results in slower elongation which then result in the increased synthesis of specific proteins. Expression levels of eEF2K targets with unaltered, enhanced, and reduced eEF2K enzyme activity, overview. Synthesis of MAP1B, ARC, and CAMKIIa is sensitive to eEF2K inhibition Mus musculus