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EEF2 is the ribosome's motor for moving along messenger RNA; the CML drug omacetaxine stalls protein production by acting at this step.
Eukaryotic elongation factor 2 (EEF2) drives the translocation step of protein synthesis, moving the ribosome one codon along the messenger RNA after each amino acid is added. Omacetaxine mepesuccinate (homoharringtonine) binds the ribosome's A-site and blocks the first elongation steps, so short-lived proteins such as BCR-ABL1 and MCL1 fall quickly; the drug is approved for chronic myeloid leukaemia after two tyrosine kinase inhibitors.
In plain words · EEF2 is the ribosome's motor for moving along messenger RNA; the CML drug omacetaxine stalls protein production by acting at this step.
EEF2 is the ribosome's motor for moving along messenger RNA; the CML drug omacetaxine stalls protein production by acting at this step.
A GTPase of the translation machinery; its activity is switched off by phosphorylation from eEF2 kinase under stress and starvation, one of the ways cells throttle protein synthesis.
1 product aims at Elongation factor 2 (EEF2): small molecules. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Broadly expressed or essential: HPA lists EEF2 among essential proteins and finds the RNA at low tissue specificity; the 2 medicines aimed at it (Omacetaxine mepesuccinate, Plitidepsin) act on the wild-type protein, so normal tissue is exposed and the therapeutic window comes from the tumour's faster division or its dependence on the protein. HPA EEF2: RNA low tissue specificity; high antibody staining in 33 normal tissues; highest cancer staining endometrial cancer (11 of 11 high). Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Leukaemia); approvals of single-target medicines aimed at it also list Multiple myeloma, not counted; Open Targets associates it with 2 specific cancer types at or above 0.5 (primary cutaneous T-cell non-Hodgkin lymphoma, hairy cell leukemia); the corpus evidence decides and the Open Targets list is quoted for comparison. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas EEF2 tissue; Open Targets ENSG00000167658 associations
First described 1988. Earliest sequence paper UniProt cites for the protein: Rapp et al, Biol. Chem. Hoppe-Seyler, 1988, "Cloning and sequence analysis of a cDNA from human ovarian granulosa cells encoding the C-terminal part of human elongation factor 2". Source.
A GTPase of the translation machinery; its activity is switched off by phosphorylation from eEF2 kinase under stress and starvation, one of the ways cells throttle protein synthesis.
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adrenal gland, Caudate, Cerebellum, Colon, Heart muscle, Hippocampus, Liver, Oral mucosa.
Medium only: lung cancer.
HPA EEF2 tissue · HPA EEF2 pathology · HPA protein class: Essential proteins, FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | all% | Housekeeping enzyme present in every dividing cell (protein synthesis); not a selection marker, which is why these drugs are given by cancer type rather than by test. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Plitidepsin is a chemotherapy derived from a Mediterranean sea squirt, approved in Australia in 2018 with dexamethasone for multiple myeloma after several other treatments; the European regulator refused it, and it drew attention in 2021 as a possible COVID-19 antiviral.
Query for this target: (TITLE:"Elongation factor 2" OR ABSTRACT:"Elongation factor 2" OR TITLE:"EEF2" OR ABSTRACT:"EEF2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Elongation factor 2 (EEF2), not a curated reading list.