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Literature summary for 2.7.11.20 extracted from

  • Liu, R.; Proud, C.G.
    Eukaryotic elongation factor 2 kinase as a drug target in cancer, and in cardiovascular and neurodegenerative diseases (2016), Acta Pharmacol. Sin., 37, 285-294 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.20

Activating Compound

Activating Compound Comment Organism Structure
Calmodulin
-
 Homo sapiens
oxidized low-density lipoprotein
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile
-
 Homo sapiens
2-((3-cyano-4-(4-methoxyphenyl)pyridine-2-ylthio)-2-phenylacetic)acid
-
 Homo sapiens
3-amino-4-(furan-2-yl)-6,7,8,9,10,11-hexahydro-5H-cyclonona[b]thieno[3,2-e]pyridine-2-carboxamide
-
 Homo sapiens
A484954 highly selective inhibitor, i.e. 7-amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide Homo sapiens
NH125 i.e. 1-benzyl-3-acetyl-2-methylimidazolium iodide Homo sapiens
rottlerin i.e. 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one, mallotoxin Homo sapiens
TS2 i.e. 4-ethyl-4-hydroxy-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens
TS4 i.e. 4-hydroxy-6-isopropyl-4-methyl-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens
TX1918 i.e. 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ activates Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [eukaryotic elongation factor 2] Homo sapiens
-
 ADP + [eukaryotic elongation factor 2] phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O00418
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein the enzyme undergoes autophosphorylation, with a major site being Thr348. The phosphorylation of Thr348 enhances the enzyme activity by increasing its affinity for a (peptide) substrate and its intrinsic catalytic activity. The 70 kDa ribosomal protein S6 kinase phosphorylates the enzyme at Ser366, inactivating it. Ser78 of the enzyme is also phosphorylated in an mTORC1-dependent manner. This phosphorylation impairs calmodulin binding, and thus, the activation of the enzyme. The Ras/Raf/MEK/ERK pathway also makes direct inputs into the inactivation of the enzyme via direct phosphorylation of the enzyme by ERK (at Ser359). Enzyme phosphorylation increases during hypoxia Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
carcinoma cell
-
 Homo sapiens
-
colonic cancer cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
Hep-G2 cell
-
 Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
MHCC97-L cell
-
 Homo sapiens
-
neuron
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [eukaryotic elongation factor 2]
-
 Homo sapiens ADP + [eukaryotic elongation factor 2] phosphate
-
 ?

Synonyms

Synonyms Comment Organism
eEF2 kinase
-
 Homo sapiens
eEF2K
-
 Homo sapiens
eukaryotic elongation factor 2 kinase
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function the enzyme protects cancer cells against acidosis and impedes tumorigenesis Homo sapiens