Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.20 extracted from

  • Arora, S.; Yang, J.M.; Kinzy, T.G.; Utsumi, R.; Okamoto, T.; Kitayama, T.; Ortiz, P.A.; Hait, W.N.
    Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines (2003), Cancer Res., 63, 6894-6899.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
Calmodulin
-
Homo sapiens

Application

Application Comment Organism
pharmacology the enzyme is a target for development of anticancer drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
overexpression of the enzyme in glioma T98-G cells causes a 10fold increased resistance to inhibitor NH125 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information non-specific inhibitors of the enzyme cause cell death Homo sapiens
NH125 an imidazolium histidine kinase inhibitor also inhibits the eukaryotic eEF-2 kinase enzyme in vitro and in vivo, IC50 is 60 nM, decreases viability of cancer cell lines with IC50S of 0.0007 to 0.0048 mM, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+
-
Homo sapiens
Mg2+
-
Homo sapiens

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
-
?
additional information Homo sapiens the enzyme expression and activity is increased in several forms of malignancy and human cancer, non-specific inhibitors of the enzyme cause cell death ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-172 cell glioblastoma cell line Homo sapiens
-
A-2780 cell ovarian carcinoma cell line Homo sapiens
-
HeLa cell cervical carcinoma cell line Homo sapiens
-
MCF-7 cell breast carcinoma cell line Homo sapiens
-
additional information the enzyme expression and activity is increased in several forms of malignancy Homo sapiens
-
OVCAR-3 cell ovarian carcinoma cell line Homo sapiens
-
PC-3 cell prostate carcinoma cell line Homo sapiens
-
T-98G cell glioblastoma cell line Homo sapiens
-
U-138MG cell glioblastoma cell line Homo sapiens
-
U-87MG cell glioblastoma cell line Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [elongation factor 2]
-
Homo sapiens ADP + [elongation factor 2]phosphate
-
?
additional information the enzyme expression and activity is increased in several forms of malignancy and human cancer, non-specific inhibitors of the enzyme cause cell death Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
eEF-2 kinase
-
Homo sapiens
eukaryotic elongation factor 2 kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
an imidazolium histidine kinase inhibitor also inhibits the eukaryotic eEF-2 kinase enzyme in vitro and in vivo, IC50 is 60 nM Homo sapiens NH125
0.0007 0.0048 decreases viability of cancer cell lines with IC50S of 0.0007 to 0.0048 mM, overview Homo sapiens NH125