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Literature summary for 2.7.1.32 extracted from

  • Ramirez de Molina, A.; Sarmentero-Estrada, J.; Belda-Iniesta, C.; Taron, M.; Ramirez de Molina, V.; Cejas, P.; Skrzypski, M.; Gallego-Ortega, D.; de Castro, J.; Casado, E.; Garcia-Cabezas, M.A.; Sanchez, J.J.; Nistal, M.; Rosell, R.; Gonzalez-Baron, M.; Lacal, J.C.
    Expression of choline kinase alpha to predict outcome in patients with early-stage non-small-cell lung cancer: a retrospective study (2007), Lancet Oncol., 8, 889-897.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
additional information ChoKalpha mRNA levels are increased in tumour cell lines in terms of their corresponding normal human primary BEC. ChoKalpha is overexpressed with a consequent increase in phosphorylcholine production in lung-cancer cells. Homo sapiens

Application

Application Comment Organism
diagnostics choline kinase alpha expression is a new prognostic factor that could be used to help identify patients with earlystage non-small-cell lung cancer who might be at high risk of recurrence, and to identify patients with favourable prognosis who could receive less aggressive treatment options or avoid adjuvant systemic treatment. Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
MN58b specific for choline kinase Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
choline + ATP Homo sapiens
-
phosphocholine + ADP
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
association between gene expression and survival in patients with non-small-cell lung cancer
-

Source Tissue

Source Tissue Comment Organism Textmining
BEC cell IBEC (CC-2541), primary bronchial epithelial cell Homo sapiens
-
HMEC-1 cell CC-2551, primary mammary epithelial cell Homo sapiens
-
lung cancer tissue, frozen tissue samples are homogenised and lysed in buffer that contained 1.5 mmol/l magnesium chloride, 0.2 mmol/l EDTA, 0.3 M sodium chloride, 25 mmol/l HEPES at pH 7.5, 20 mmol/l beta-glycerophosphate, and 0.1% Triton X-100. Cells are lysed in ice-cold lysis buffer. Nuclei and detergent-insoluble material are removed by centrifugation. Homo sapiens
-
NCI-H1299 cell non-small cell lung cancer epithelial cell line Homo sapiens
-
NCI-H460 cell non-small cell lung cancer epithelial cell line Homo sapiens
-
NCI-H510 cell small cell lung cancer cell line Homo sapiens
-
NCI-H82 cell small cell lung cancer cell line Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
increase in mRNA levels results in an increase in protein expression and ChoK enzymatic activity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
choline + ATP
-
Homo sapiens phosphocholine + ADP
-
?

Synonyms

Synonyms Comment Organism
ChoKalpha
-
Homo sapiens
choline kinase
-
Homo sapiens
choline kinase alpha
-
Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
H510 cell, 144 h Homo sapiens MN58b
0.00027
-
H82 cell, 144 h Homo sapiens MN58b
0.0004
-
H510 cell, 72 h Homo sapiens MN58b
0.0008
-
H82 cell, 72 h Homo sapiens MN58b
0.0009
-
H1299 cell, 144 h Homo sapiens MN58b
0.0011
-
H460 cell, 144 h Homo sapiens MN58b
0.0011
-
H510 cell, 48 h Homo sapiens MN58b
0.0019
-
H82 cell, 48 h Homo sapiens MN58b
0.0026
-
H460 cell, 72 h Homo sapiens MN58b
0.0027
-
H1299 cell, 72 h Homo sapiens MN58b
0.0034
-
primary HMEC cell, 144 h Homo sapiens MN58b
0.0042
-
primary BEC cell, 144 h Homo sapiens MN58b
0.00703
-
H460 cell, 48 h Homo sapiens MN58b
0.0103
-
H1299 cell, 48 h Homo sapiens MN58b
0.0183
-
primary BEC cell, 72 h Homo sapiens MN58b
0.0209
-
primary HMEC cell, 72 h Homo sapiens MN58b
0.0405
-
primary BEC cell, 48 h Homo sapiens MN58b
0.0447
-
primary HMEC cell, 48 h Homo sapiens MN58b