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Literature summary for 2.7.11.20 extracted from
- Eukaryotic elongation factor 2 kinase regulates the development of hypertension through oxidative stress-dependent vascular inflammation (2013), Am. J. Physiol. Heart Circ. Physiol., 305, H756-H768.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| Calmodulin | a central mediator of Ca2+-dependent signaling, the enzyme is dependent on calmodulin | Homo sapiens |  |
| Calmodulin | a central mediator of Ca2+-dependent signaling, the enzyme is dependent on calmodulin | Rattus norvegicus | |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | generation of enzyme knoockout mice, silencing of the enzyme by siRNA expression | Rattus norvegicus |
| additional information | knockdown of eEF2K gene by small interfering RNA (siRNA) | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-benzyl-3-cetyl-2-methylimidazolium iodide | i.e. NH125, inhibits eEF2K activity via inhibition of alpha-kinase, a catalytic domain of eEF2K | Homo sapiens | |
| 1-benzyl-3-cetyl-2-methylimidazolium iodide | i.e. NH125, inhibits eEF2K activity via inhibition of alpha-kinase, a catalytic domain of eEF2K. In mesenteric artery from spontaneously hypertensive rats, the acetylcholine-induced endothelium-dependent relaxation is significantly impaired after long-term treatment with the inhibitor | Rattus norvegicus | |
| 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d] pyrimidine-6-carboxamide | i.e. A-484954, a pyrido-pyrimidinedione derivative that inhibits eEF2K in an ATP-competitive but CaM-independent manner | Homo sapiens | |
| 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d] pyrimidine-6-carboxamide | i.e. A-484954, a pyrido-pyrimidinedione derivative that inhibits eEF2K in an ATP-competitive but CaM-independent manner | Rattus norvegicus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | a Ca2+/calmodulin-dependent protein kinase | Homo sapiens | |
| Ca2+ | a Ca2+/calmodulin-dependent protein kinase | Rattus norvegicus | |
| Mg2+ | required | Homo sapiens | |
| Mg2+ | required | Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [elongation factor 2] | Homo sapiens | - |
ADP + [elongation factor 2] phosphate | - |
? | |
| ATP + [elongation factor 2] | Rattus norvegicus | - |
ADP + [elongation factor 2] phosphate | - |
? | |
| ATP + [elongation factor 2] | Rattus norvegicus Wistar | - |
ADP + [elongation factor 2] phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O00418 | - |
- |
| Rattus norvegicus | P70531 | - |
- |
| Rattus norvegicus Wistar | P70531 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| additional information | activity of eEF2K is selectively increased in proliferating cells | Homo sapiens | - |
| additional information | activity of eEF2K is selectively increased in proliferating cells | Rattus norvegicus | - |
| U-937 cell | - |
Homo sapiens | - |
| umbilical vein endothelial cell | - |
Homo sapiens | - |
| vascular endothelial cell | - |
Rattus norvegicus | - |
| vascular smooth muscle cell | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [elongation factor 2] | - |
Homo sapiens | ADP + [elongation factor 2] phosphate | - |
? | |
| ATP + [elongation factor 2] | - |
Rattus norvegicus | ADP + [elongation factor 2] phosphate | - |
? | |
| ATP + [elongation factor 2] | - |
Rattus norvegicus Wistar | ADP + [elongation factor 2] phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| eEF2K | - |
Homo sapiens |
| eEF2K | - |
Rattus norvegicus |
| eukaryotic elongation factor 2 kinase | - |
Homo sapiens |
| eukaryotic elongation factor 2 kinase | - |
Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| ATP | - |
Rattus norvegicus | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | eEF2K gene knockdown on TNF-alpha-induced inflammatory responses in HUVECs | Homo sapiens |
| malfunction | enzyme silencing with eEF2K siRNA inhibits phosphorylation of JNK and NF-kappaB p65 as well as reactive oxygen species (ROS) production by TNF-alpha. In vascular smooth muscle cells, eEF2K siRNA also inhibits VCAM-1 induction and phosphorylation of JNK and NF-kappaB by TNF-alpha. In vascular endothelial cells, siRNA against eEF2K inhibited induction of VCAM-1 and endothelial-selectin as well as monocyte adhesion by TNF-alpha. Phenotypes, overview | Rattus norvegicus |
| physiological function | eukaryotic elongation factor 2 kinase (eEF2K) prevents binding of eEF to the ribosome via phosphorylation of eEF and thus prevents further translation. The enzyme regulates the development of hypertension through oxidative stress-dependent vascular inflammation | Homo sapiens |
| physiological function | eukaryotic elongation factor 2 kinase (eEF2K) prevents binding of eEF to the ribosome via phosphorylation of eEF and thus prevents further translation. The enzyme regulates the development of hypertension through oxidative stress-dependent vascular inflammation. eEF2K protein increases in mesenteric artery from spontaneously hypertensive rats. Enzyme eEF2K mediates TNF-alpha-induced vascular inflammation via reactive oxygen species-dependent mechanism, which is at least partly responsible for the development of hypertension in spontaneously hypertensive rats | Rattus norvegicus |
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