Target type: molecularfunction
Catalysis of the reaction: ATP + [elongation factor 2] = ADP + [elongation factor 2] phosphate. [EC:2.7.11.20, MetaCyc:2.7.11.20-RXN]
Elongation factor-2 kinase (eEF-2 kinase) is an enzyme that catalyzes the phosphorylation of eukaryotic elongation factor 2 (eEF-2), a key component of the ribosome's translational machinery. This phosphorylation event plays a critical role in regulating protein synthesis by controlling the rate of polypeptide chain elongation. Specifically, eEF-2 kinase phosphorylates a specific serine residue (Ser51) on eEF-2, which inactivates the factor's ability to translocate the ribosome along the mRNA molecule. Inactivation of eEF-2 leads to a stalling of translation, effectively reducing protein synthesis.
eEF-2 kinase activity is tightly regulated, and its activation is often triggered by cellular stress conditions such as nutrient deprivation, hypoxia, or viral infection. These stress signals activate various signaling pathways, ultimately leading to the phosphorylation and activation of eEF-2 kinase.
The regulation of eEF-2 kinase activity is crucial for maintaining cellular homeostasis and survival. By controlling protein synthesis, eEF-2 kinase allows cells to adapt to stressful conditions and conserve energy. Dysregulation of eEF-2 kinase activity has been implicated in various diseases, including cancer, neurodegenerative disorders, and diabetes.
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| Protein | Definition | Taxonomy |
|---|---|---|
| Eukaryotic elongation factor 2 kinase | An elongation factor 2 kinase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00418] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| rottlerin | rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis. rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1); | aromatic ketone; benzenetriol; chromenol; enone; methyl ketone | anti-allergic agent; antihypertensive agent; antineoplastic agent; apoptosis inducer; K-ATP channel agonist; metabolite |
| nh 125 | NH 125: structure in first source | ||
| a-484954 | A-484954: eEF2K inhibitor; structure in first source | ||
| entrectinib | entrectinib : A member of the class of indazoles that is 1H-indazole substituted by [4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzoyl]amino and 3,5-difluorobenzyl groups at positions 3 and 5, respectively. It is a potent inhibitor of TRKA, TRKB, TRKC, ROS1, and ALK (IC50 values of 0.1 to 1.7 nM), and used for the treatment of NTRK, ROS1 and ALK gene fusion-positive solid tumours. entrectinib: inhibits TRK, ROS1, and ALK receptor tyrosine kinases; structure in first source | benzamides; difluorobenzene; indazoles; N-methylpiperazine; oxanes; secondary amino compound; secondary carboxamide | antibacterial agent; antineoplastic agent; apoptosis inducer; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor |
| nms p937 | NMS P937: a polo-like kinase 1 inhibitor; structure in first source | ||
| nms-p118 | NMS-P118: a PARP-1 inhibitor; structure in first source | ||
| nms-e973 | NMS-E973: structure in first source |