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Literature summary 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

Activating Compound

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.20 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile
-
 Homo sapiens
2.7.11.20 2-((3-cyano-4-(4-methoxyphenyl)pyridine-2-ylthio)-2-phenylacetic)acid
-
 Homo sapiens
2.7.11.20 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
2.7.11.20 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
2.7.11.20 NH125 i.e. 1-benzyl-3-acetyl-2-methylimidazolium iodide Homo sapiens
2.7.11.20 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
2.7.11.20 TS2 i.e. 4-ethyl-4-hydroxy-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens
2.7.11.20 TS4 i.e. 4-hydroxy-6-isopropyl-4-methyl-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens
2.7.11.20 TX1918 i.e. 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.20 Ca2+ activates Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.20 Homo sapiens O00418
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.20 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

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

Substrates and Products (Substrate)

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

Synonyms

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

General Information

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