Information on EC 2.7.1.32 - choline kinase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY
2.7.1.32
-
RECOMMENDED NAME
GeneOntology No.
choline kinase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
ATP + choline = ADP + phosphocholine
show the reaction diagram
ethanolamine and its methyl and ethyl derivatives can also act as acceptors
-
-
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase may not have a common active site in a single enzyme protein
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase are 2 distinct enzymes
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
ethanolamine kinase II and choline kinase do not use a common active site
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase are 2 distinct enzymes
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase activities are mediated by 2 distinct active sites, possibly on a single protein
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
random bi-bi mechanism
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
forward reaction: ordered mechanism with MgATP2- binding first, followed by choline
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase activities reside on the same protein and occur at the same active site
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase activities reside on the same protein and occur at the same active site
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
forward reaction follows a sequentially ordered mechanism
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
choline kinase and ethanolamine kinase are identical
-
ATP + choline = ADP + phosphocholine
show the reaction diagram
sequential bi bi reaction
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
phospho group transfer
-
-
-
-
Phosphorylation
-
-
Phosphorylation
-
-
Phosphorylation
O54804
;
Phosphorylation
-
-
Phosphorylation
-
-
Phosphorylation
-
-
PATHWAY
KEGG Link
MetaCyc Link
Glycerophospholipid metabolism
-
Metabolic pathways
-
phosphatidylcholine biosynthesis I
-
SYSTEMATIC NAME
IUBMB Comments
ATP:choline phosphotransferase
Ethanolamine and its methyl and ethyl derivatives can also act as acceptors.
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
ATP:choline phosphotransferase
-
-
CHETK-alpha
-
-
-
-
chk-alpha
-
-
Chka
-
-
Chka
P35790
-
CHKA2
P35790
isoform
ChKalpha
-
-
ChoK
-
-
-
-
ChoK
P35790
-
ChoK
Saccharomyces cerevisiae KS106
-
-
-
ChoK alpha
-
-
ChoKalpha
-
-
ChoKalpha
P35790
-
CHOKalpha1
-
-
CHOKalpha1
P35790
isoform
ChoKalpha2
P35790
isoform
ChoKbeta1
Q9Y259
isoform
choline kinase
B0URY8
-
choline kinase
-, O54804
-
choline kinase
-
-
choline kinase
Q8IM71
-
choline kinase
-
-
choline kinase
-
-
choline kinase alpa
-
-
choline kinase alpha
-
-
choline kinase alpha
P35790
-
choline kinase alpha
-
-
choline kinase alpha
-
isoform
choline kinase alpha
O54804
-
choline kinase alpha
-
-
choline kinase alpha1
-
-
choline kinase alpha1
P35790
-
choline kinase alpha2
P35790
-
choline kinase beta
-
isoform
choline kinase beta1
Q9Y259
-
choline kinase isoform alpha2
-
-
choline phosphokinase
-
-
-
-
choline-ethanolamine kinase
-
-
-
-
choline/ethanolamine kinase
-
-
-
-
choline/ethanolamine kinase 2
-
-
CK-alpha
-
-
CK-alpha
-
-
CK-alpha1
O54804
-
CK-alpha1/beta
-
-
CK-alpha2
O54804
-
CK-beta
-
-
CK-beta
O54804
-
CKalpha
-
isoform
CKalpha1
-
isoform
CKalpha2
-
-
CKalpha2
-
isoform
CKbeta
-
isoform
CKbeta1
-
isoform
CKI1-encoded choline kinase
-
-
EtnK
-
-
-
-
putative choline kinase
-
-
kinase, choline (phosphorylating)
-
-
-
-
additional information
-
at least four genes encoding active choline kinase
additional information
-
alpha and beta subtype
additional information
Q54AG5
two subtypes identified which are named alpha and beta (ChoKalpha and ChoKbeta), alpha subtype displays two splicing variants names alpha1 and alpha2
additional information
-
alpha and beta subtype
CAS REGISTRY NUMBER
COMMENTARY
9026-67-9
-
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
ecotype Columbia
-
-
Manually annotated by BRENDA team
canola
-
-
Manually annotated by BRENDA team
African green monkey
-
-
Manually annotated by BRENDA team
pigeon
-
-
Manually annotated by BRENDA team
Culex pipiens fatigans
-
-
-
Manually annotated by BRENDA team
chicken
-
-
Manually annotated by BRENDA team
soy bean
-
-
Manually annotated by BRENDA team
Hemidactylus sp.
lizard
-
-
Manually annotated by BRENDA team
association between gene expression and survival in patients with non-small-cell lung cancer
-
-
Manually annotated by BRENDA team
choline kinase alpha isoform
UniProt
Manually annotated by BRENDA team
commentary
-
-
Manually annotated by BRENDA team
subunit CKalpha
UniProt
Manually annotated by BRENDA team
subunit CKbetha
SwissProt
Manually annotated by BRENDA team
embryo
-
-
Manually annotated by BRENDA team
isoforms alpha, beta
GenBank
Manually annotated by BRENDA team
isoforms alpha1, alpha2, beta
-
-
Manually annotated by BRENDA team
knock-out mice, heterozygous, +/-choline kinase alpha deficient
-
-
Manually annotated by BRENDA team
subtype alpha; subtype beta
SwissProt
Manually annotated by BRENDA team
; clone NF-54 and wild type
-
-
Manually annotated by BRENDA team
clone NF54
-
-
Manually annotated by BRENDA team
two isoforms
-
-
Manually annotated by BRENDA team
strain KS106
-
-
Manually annotated by BRENDA team
Saccharomyces cerevisiae KS106
strain KS106
-
-
Manually annotated by BRENDA team
protozoan parasite which causes African sleeping sickness
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
malfunction
-
deletion of choline kinase gene Chkb results in neonatal forelimb bone deformity and hindlimb muscular dystrophy. The virtual elimination of all choline kinase activity in hindlimb muscle of Chkb-/- mice is not compensated by isoform CKalpha activity and muscular dystrophy develops. In contrast, in forelimb muscles of these mice, the 50% of total choline kinase activity remaining (due to isoform CKalpha), and the increased activity of CTP:phosphocholine cytidylyltransferase, ensure that the amount of phosphocholine is not reduced so that only minimal signs of muscular dystrophy develop as the mice age
malfunction
-
silencing of CKalpha leads to a lethal phenotype with aberrant mitotic arrest and subsequent apoptosis, and is rescued by simultaneous knockdown of CKalpha and CKbeta isoforms
malfunction
-
the parasite compensates for the loss of full-length enzyme by two potential 53- and 44 kDa isoforms
malfunction
-
enzyme knockdown in MCF-7 and MCF-10A cells reduces epidermal growth factor-dependent cell proliferation
physiological function
-
levels of CKalpa and CKbeta play an essential role in progression through mitosis, but not in resting cells or during DNA replication
physiological function
-
the enzyme is required for maximum epidermal growth factor-dependent cell growth in mammary epithelium-derived cell lines MCF-7 and MCF-10A
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2-(dimethylamino)-ethanol + ATP
ADP + 2-(dimethylamino)-ethyl phosphate
show the reaction diagram
-
-
-
-
?
2-(dimethylamino)-ethanol + ATP
ADP + 2-(dimethylamino)-ethyl phosphate
show the reaction diagram
-
-
-
-
?
2-aminoethanol + ATP
ADP + 2-aminoethyl phosphate
show the reaction diagram
-
-
-
-
?
2-methylaminoethanol + ATP
ADP + 2-methylaminoethyl phosphate
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
P35790
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
r
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
r
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Culex pipiens fatigans
-
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q54AG5
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q9Y259
-
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
both isoforms
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
choline pathway or CDP-ethanolamine pathway is so-called Kennedy pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction and cell stress regulation
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, involved in cell stress response
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, possible role in carcinogenesis
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, increased activity under salt stress and cold conditions
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q54AG5
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q9Y259
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, the product O-phosphocholine serves as second messenger and is essential for cell growth, enzyme plays a role in tumor generation
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Saccharomyces cerevisiae KS106
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
P35790, Q9Y259
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
P35790
-
-
-
?
ATP + choline
ADP + phosphocholine
show the reaction diagram
-
-
-
-
?
ATP + dimethylethanolamine
ADP + phosphodimethylethanolamine
show the reaction diagram
-
-
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
show the reaction diagram
-
-
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
show the reaction diagram
-
poor substrate compared to choline
-
-
-
ATP + ethanolamine
ADP + ethanolamine phosphate
show the reaction diagram
-
poor substrate compared to choline
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
show the reaction diagram
-
not: basic isoform
-
-
?
ATP + ethanolamine
ADP + ethanolamine phosphate
show the reaction diagram
-
can not phosphorylate ethanolamine efficiently
-
-
?
ATP + ethanolamine
ADP + phosphoethanolamine
show the reaction diagram
-
-
-
-
?
beta-methylcholine + ATP
ADP + beta-methylcholine phosphate
show the reaction diagram
-
-
-
-
?
choline + ATP
O-phosphocholine + ADP
show the reaction diagram
Q8IM71
-
-
-
?
choline + ATP
O-phosphocholine + ADP
show the reaction diagram
-
first step in the biosynthesis of the glycerophospholipid glycerophosphocholine
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
-
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
catalyzes the first phosphorylation reaction in the Kennedy pathway (biosynthesis of the major membrane phospholipid phosphatidylcholine)
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
choline kinase may have a regulatory role in phosphatidylcholine biosynthesis
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
O54804
first enzyme in the CDP-choline (Kennedy) pathway for the biosynthesis of phosphatidylcholine
choline kinase supply phosphocholine for the biosynthesis of phosphatidylcholine that is essential for growth and cell division
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
The induction of CKI1 expression in zinc-depleted cells translated into increased choline kinase activity in vitro and in vivo and in an increase in phosphatidylcholine synthesis via the Kennedy pathway
-
-
?
choline + ATP
phosphorylcholine + ADP
show the reaction diagram
B0URY8, -
-
-
-
?
CTP + choline
CDP + choline phosphate
show the reaction diagram
-
12% of the activity with ATP
-
-
?
diethanolamine + ATP
ADP + O-phospho-diethanolamine
show the reaction diagram
-
-
-
-
?
ethanolamine + ATP
ADP + ethanolamine phosphate
show the reaction diagram
-
-
-
-
?
ethanolamine + ATP
ADP + ethanolamine phosphate
show the reaction diagram
-
-
-
-
?
ethanolamine + ATP
O-phosphoethanolamine + ADP
show the reaction diagram
-
first step in the biosynthesis of the glycerophospholipid glycerophosphoethanolamine
-
-
?
ethanolamine + ATP
phosphoethanolamine + ADP
show the reaction diagram
-
-
-
-
?
GTP + choline
GDP + choline phosphate
show the reaction diagram
-
poor substrate
-
-
?
GTP + choline
GDP + choline phosphate
show the reaction diagram
-
at 50% of the activity with ATP
-
-
?
N,N,N-triethylethanolamine + ATP
ADP + N,N,N-triethylethanolamine phosphate
show the reaction diagram
-
weak
-
-
?
N,N-diethyl-N-methylethanolamine + ATP
ADP + N,N-diethyl-N-methylethanolamine phosphate
show the reaction diagram
-
weak
-
-
?
N,N-diethylethanolamine + ATP
ADP + N,N-diethylethanolamine phosphate
show the reaction diagram
-
-
-
-
-
N,N-diethylethanolamine + ATP
ADP + N,N-diethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-diethylethanolamine + ATP
ADP + N,N-diethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-diethylethanolamine + ATP
ADP + O-phospho-N-diethylethanolamine
show the reaction diagram
-
-
-
-
?
N,N-diisopropylethanolamine + ATP
ADP + N,N-diisopropylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethyl-N-propylethanolamine + ATP
ADP + N,N-dimethyl-N-propylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylaminopropanol + ATP
ADP + N,N-dimethylaminopropyl phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylethanolamine + ATP
ADP + N,N-dimethylethanolamine phosphate
show the reaction diagram
-
not: basic isoform
-
-
?
N,N-dimethylethanolamine + ATP
ADP + O-phospho-N,N-dimethylethanolamine
show the reaction diagram
-
-
-
-
?
N,N-dimethylethylcholine + ATP
ADP + N,N-dimethylethylcholine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylisopropylcholine + ATP
ADP + N,N-dimethylisopropylcholine phosphate
show the reaction diagram
-
-
-
-
?
N,N-dimethylpropylcholine + ATP
ADP + N,N-dimethylpropylcholine phosphate
show the reaction diagram
-
-
-
-
?
N-ethylethanolamine + ATP
ADP + O-phospho-N-ethylethanolamine
show the reaction diagram
-
-
-
-
?
N-methylethanolamine + ATP
ADP + N-methylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N-methylethanolamine + ATP
ADP + N-methylethanolamine phosphate
show the reaction diagram
-
not: basic isoform
-
-
?
N-methylethanolamine + ATP
ADP + O-phospho-N-methylethanolamine
show the reaction diagram
-
-
-
-
?
N-monoethylethanolamine + ATP
ADP + N-monoethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N-monomethylethanolamine + ATP
ADP + N-monomethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
N-monomethylethanolamine + ATP
ADP + N-monomethylethanolamine phosphate
show the reaction diagram
-
-
-
-
?
UTP + choline
UDP + choline phosphate
show the reaction diagram
-
poor substrate
-
-
?
UTP + choline
UDP + choline phosphate
show the reaction diagram
-
at 20% of the activity with ATP
-
-
?
UTP + choline
UDP + choline phosphate
show the reaction diagram
-
at 20% of the activity with ATP
-
-
?
GTP + choline
GDP + choline phosphate
show the reaction diagram
-
at 50% of the activity with ATP
-
-
?
additional information
?
-
-
specificity overview
-
-
-
additional information
?
-
-
specificity overview
-
-
-
additional information
?
-
-
specificity overview
-
-
-
additional information
?
-
-
microarray analysis detected changes in the expression of 33 proliferation-related genes with Chk down-regulation
-
-
-
additional information
?
-
-
Further substrate specificity analysis reveals that TbC/EK2 are able to tolerate various modifications at the amino group, with the exception of a quaternary amine for TbEK1 (choline). The enzyme recognizes analogues with substituents on C-2, but substitutions on C-1 and elongations of the carbon chain are not well tolerate. Secondary and tertiary amino modifications are better than choline. A reduction of activity is seen with the elongation of the carbon chain, but it is not abolished even when increased by an ethylene unit. Modifications at the hydroxy group result in no detectable reactivity.
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial enzyme of the CDP-choline pathway and the CDP-ethanolamine pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
choline pathway or CDP-ethanolamine pathway is so-called Kennedy pathway
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
enzyme of the CDP-choline pathway of lecithin biosynthesis
-
-
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction and cell stress regulation
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, involved in cell stress response
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the CDP-choline pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, possible role in carcinogenesis
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
-
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, increased activity under salt stress and cold conditions
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q54AG5
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction
-
-
?
ATP + choline
ADP + O-phosphocholine
show the reaction diagram
Q9Y259
initial step of the Kennedy pathway, that yields phosphatidylcholine as final product, involved in mitogenic signaling transduction, the product O-phosphocholine serves as second messenger and is essential for cell growth, enzyme plays a role in tumor generation
-
-
?
choline + ATP
O-phosphocholine + ADP
show the reaction diagram
-
first step in the biosynthesis of the glycerophospholipid glycerophosphocholine
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
-
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
catalyzes the first phosphorylation reaction in the Kennedy pathway (biosynthesis of the major membrane phospholipid phosphatidylcholine)
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
choline kinase may have a regulatory role in phosphatidylcholine biosynthesis
-
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
O54804
first enzyme in the CDP-choline (Kennedy) pathway for the biosynthesis of phosphatidylcholine
choline kinase supply phosphocholine for the biosynthesis of phosphatidylcholine that is essential for growth and cell division
-
?
choline + ATP
phosphocholine + ADP
show the reaction diagram
-
The induction of CKI1 expression in zinc-depleted cells translated into increased choline kinase activity in vitro and in vivo and in an increase in phosphatidylcholine synthesis via the Kennedy pathway
-
-
?
ethanolamine + ATP
O-phosphoethanolamine + ADP
show the reaction diagram
-
first step in the biosynthesis of the glycerophospholipid glycerophosphoethanolamine
-
-
?
additional information
?
-
-
microarray analysis detected changes in the expression of 33 proliferation-related genes with Chk down-regulation
-
-
-
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Carpronium chloride
-
stimulates
Chlorocholine chloride
-
stimulates
K+
-
KCl activates
K+
-
stimulates
Li+
-
stimulates
Mg2+
-
ATP concentration 1.25-2.5 mM: reaction requires free Mg2+ rather than MgATP2-, ATP concentration exceeding that of Mg2+: strong inhibition; Km MgATP2-: 10 mM, in presence of equimolar amounts of ATP and Mg2+, Km MgATP2-: 1.5 mM, in 2.5 fold higher concentration of Mg2+ than ATP
Mg2+
-
Mg2+:ATP ratio for optimal activity is 30:10 mM
Mg2+
-
10 mM MgSO4 required for maximal activity
Mg2+
Culex pipiens fatigans
-
required
Mg2+
-
maximal activity at equimolar concentration of ATP and Mg2+; MgATP2- is the true substrate; stimulates most efficiently of divalent cations
Mg2+
-
optimal stimulation at 13 mM in the presence of 10 mM ATP; requires free Mg2+ as well as MgATP2-
Mg2+
-
maximal activity at equimolar concentration of ATP and Mg2+; required; stimulates most efficiently of divalent cations
Mg2+
-
required
Mg2+
-
-
Mg2+
-
required for activity
Mg2+
-
required
Mg2+
P35790, Q9Y259
required; required
MgCl2
-
assay at
Mn2+
-
cannot substitute for Mg2+
Mn2+
-
one-sixth as effective as Mg2+
Na+
-
NaCl activates
Na+
-
8.7-35 mM: slight activation, 70 mM: inactivation
Na+
-
stimulates
NH4+
-
stimulates
Mn2+
-
poor substitute for Mg2+
additional information
-
Co2+, Cd2+: almost completely ineffective, Ca2+, Ni2+, Zn2+: totally ineffective
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
1,1',1''-(benzene-1,3,5-triylmethylene)tris[(4-dimethylamino)pyridinium] tribromide
-
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(3,5-dichloro-N-methylanilino)pyridinium] tribromide
-
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(4-chloro-N-methylanilino)pyridinium] tribromide
-
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(N-methylanilino)pyridinium] tribromide
-
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(piperidino)pyridinium] tribromide
-
-
1,1',1''-(benzene-1,3,5-triylmethylene)tris[4-(pyrrolidino)pyridinium] tribromide
-
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0528 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0842 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0084 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0072 mM
1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0375 mM
1,1'-(benzene-1,3-diylmethylene)bis[(4-dimethylamino)pyridinium] dibromide
-
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(N-methylanilino)pyridinium] dibromide
-
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(piperidino)pyridinium] dibromide
-
-
1,1'-(benzene-1,3-diylmethylene)bis[4-(pyrrolidino)pyridinium] dibromide
-
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0377 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.024 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0097 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0029 mM
1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.015 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: 0.0119 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0206 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0012 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0005 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0019 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0058 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0026 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0015 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0021 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.147 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0012 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0044 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0013 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.00043 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0004 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0568 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0096 mM
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0031 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: above 0.2 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0633 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0811 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0022 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0088 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0111 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0034 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0018 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.002 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0461 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0198 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0114 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0397 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0178 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0043 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.003 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0961 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0206 mM
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0114 mM
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)
-
-
1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)
-
-
1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)
-
-
1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)
-
-
1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
-
1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)
-
-
1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)
-
-
1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)
-
-
1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
-
1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.098 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: above 0.1 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0482 mM; IC50: above 0.1 mM
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: above 0.1 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: above 0.2 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide
-
IC50: 0.08 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.006 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0048 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0575 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.001 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0102 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0023 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0014 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.133 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.009 mM
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0035 mM
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide
P35790
0.1% inhibition at 0.01 mM, 24.8% inhibition at 0.05 mM
-
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
P35790
62.3% inhibition at 0.01 mM, 71.4% inhibition at 0.05 mM
-
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-(dimethylamino)pyridinium bromide
P35790
38.6% inhibition at 0.01 mM, 81% inhibition at 0.05 mM
-
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenethyl]benzyl)-4-pyrrolidinopyridinium bromide
P35790
28.6% inhibition at 0.01 mM, 46.9% inhibition at 0.05 mM
-
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
P35790
37.6% inhibition at 0.01 mM, 51% inhibition at 0.05 mM
-
1-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]benzyl)-4-pyrrolidinopyridinium bromide
P35790
50.2% inhibition at 0.01 mM, 72.8% inhibition at 0.05 mM
-
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
P35790
61.3% inhibition at 0.01 mM, 68.2% inhibition at 0.05 mM
-
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide
P35790
22.6% inhibition at 0.01 mM, 59.9% inhibition at 0.05 mM
-
1-[4-(4-[4-[(6-amino-9H-purin-8-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
-
-
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
P35790
66.7% inhibition at 0.01 mM, 89.7% inhibition at 0.05 mM
-
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-pyrrolidinopyridinium bromide
P35790
36.9% inhibition at 0.01 mM, 41.9% inhibition at 0.05 mM
-
1-[4-[(6-amino-3H-purin-3-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide
P35790
25% inhibition at 0.01 mM, 50.2% inhibition at 0.05 mM
-
1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-(dimethylamino)pyridinium bromide
P35790
46.7% inhibition at 0.01 mM, 54.1% inhibition at 0.05 mM
-
1-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-4-pyrrolidinopyridinium bromide
P35790
27% inhibition at 0.05 mM
-
12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide
-
IC50: 0.0132 mM
12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0021 mM
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM, most potent inhibitor
2-amino-1-butanol
Q8IM71
-
3-Trimethylammonio-1-propanol
-
-
4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazol
-
-
-
4-chloro-N-methylanilino
-
IC50: 0.0014 mM
5'-dithio-bis-(2-nitrobenzoic acid)
-
modest inhibitory activity
5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide
-
IC50: 0.0248 mM
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
Q54AG5
-
5-Fluorouracil
-
Investigation of the effect of combining transient siRNA-chk transfection with the anticancer drug 5-fluorouracil on cell viability and proliferation. Choline kinase down-regulation with 5-fluorouracil treatment increased cell kill in cancer cells.
7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium
-
-
Acetylcholine
-
-
adenosine
-
competitive with MgATP2-
adenosine
Q54AG5
competitive with MgATP2-
ADP
Culex pipiens fatigans
-
-
ADP
-
50% inhibition at 0.32 mM, in a positive cooperative manner
ATP
-
at 4.9 mM and 8.0 mM 30% inhibition; optimum concentration: 3.2-4.0 mM
Choline analogues
-
-
Choline analogues
-
several compounds tested and found to be inhibitory
Choline analogues
Q54AG5
several compounds tested and found to be inhibitory
choline kinase inhibitor Mn58b
-
-
-
choline kinase inhibitor Mn58b
-
;
-
choline kinase inhibitor TCD828
-
-
-
choline phosphate
-
-
cyclophane
-
-
Cytidine diphosphocholine
-
-
Diethylmethylcholine
-
-
dimethylethanolamine
-
-
ethanolamine
-
weak competitive inhibitor
ethanolamine
Culex pipiens fatigans
-
no significant effect
ethanolamine
-
inhibition only at very high concentration, 100-150 mM
ethanolamine
-
weak
ethanolamine
-
poor inhibitor
H-89
-
no activity on choline kinase at 5 mM ATP, decreasing the ATP concentration to 100 microM has no effect on choline kinase
HC-3
-
poor inhibition of 16% and 18% is observed at 50 microM and 150 microM, respectively, at both 100 and 250 microM choline
hemicholinium
-
-
hemicholinium
-
HC-3
hemicholinium
Q54AG5
HC-3
hemicholinium
-
-
hemicholinium-3
-
poor inhibition of 16% and 18% at 0.050 mM and 0.15 mM, respectively, not significantly inhibited by hemicholinium-3 up to 0.025 mM
hemicholinium-3
-
-
hemicholinium-3
-
weak inhibitor, IC50: 0.057 mM
hemicholinium-3
Q8IM71
-
hemicholinium-3
-
-
hemicholinium-3
P35790, Q9Y259
competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform; competitive inhibitor, the inhibitory effect of hemicholinium-3 is about 500times higher toward the ChoKalpha isoforms than ChoKbeta isoform
Hexadecyltrimethylammonium bromide
-
60% inhibition at 0.1 mM; HDTAB, structural resemblance to hexadecylphosphocholine, exhibits an antimalarial effect and inhibits choline kinase in a dose-dependent manner. For purified protein: 60% inhibition at 100 microM (in presence of 250 microM choline), 60% inhibition at 50 microM (in presence of 100 microM choline). HDTAB may compete with choline for the choline binding site of choline kinase and may offer competitive inhibition with respect to choline. The concentration of HDTAB required to inhibit Plasmodium falciparum growth by 62% was 10times lower than the concentration required to inhibit purified choline kinase by 60% in vitro
MN58b
-
specific inhibitor, IC50: 0.0005-0.072 mM depending on cell type
-
N-ethylmaleimide
-
-
N-ethylmaleimide
-
-
N-ethylmaleimide
Q54AG5
-
N-ethylmaleimide
-
modest inhibitory activity
N-Methyl-N,N-diisopropylethanolamine
Culex pipiens fatigans
-
-
N-Methyl-N-isopropylethanolamine
Culex pipiens fatigans
-
-
N-[2-bromocinnamyl(amino)ethyl]-5-isoquinoline sulfonamide
-
-
NaCl
-
8.7-35 mM: slight activation, 70 mM: inactivation
o-phenanthroline
-
-
p-chloromercuribenzoate
Culex pipiens fatigans
-
-
p-hydroxymercuribenzoate
-
-
phosphocholine
-
40% and 66% inhibition at 2.5 mM and 10 mM, respectively
phosphorylcholine
-
-
phosphorylcholine
-
-
phosphorylcholine
-
-
physostigmine
-
-
piperazine
-
modest inhibitory activity
purinyl-6-histamine
-
modest inhibitory activity
Quinacrine
-
indirect inhibitor
serine
Culex pipiens fatigans
-
not
stearoyl-CoA
-
weak
stearoyl-CoA
-
-
stearoyl-CoA
Q54AG5
-
Triethanolammonio-1-choline
-
-
-
V-11-023907
-
-
-
MN58b
-
specific for choline kinase
-
additional information
-
not: CTP, ethanolamine phosphate
-
additional information
-
not: neostigmine
-
additional information
-
-
-
additional information
-
not: p-chloromercuribenzoate, N-ethylmaleeimide
-
additional information
-
the lethality of the homozygous choline kinase alpha knock-out mice embryos indicates the indispensable role of CK-alphain early embryogenesis
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
2-Chloroethylammonium chloride
-
stimulates
Acetylcholine
-
stimulates
atropine
-
stimulates
c-Src
-
isoform CHKA2 total cellular activity and protein levels are regulated by c-Src
-
carbon tetrachloride
O54804
CCl4, major increase in the transcript for choline kinase alpha expression in livers from mice 3 h and 6 h after administration of carbon tetrachloride. CK-beta is unaffected by the carbon tetrachloride treatment. Choline kinase activity is induced in murine livers by carbon tetrachloride as a result of an increase in the expression of the mRNA for CK-alpha and Ck-alpha protein.; CK activity is induced by carbon tetrachloride as a result of an increase in the expression of the mRNA for CK alpha and CK alpha protein. The transcriptional activity of CK alpha was markedly increased 3 h and 6 h after treatment with carbon tetrachloride. Carbon tetrachloride promotes the expression of the transcription factor activator protein 1 (AP-1) that increases CK expression and activity.
Choline esters
-
activate
cysteine
-
omission of cysteine decreases the reaction rate by 40%
epidermal growth factor receptor
-
isoform CHKA2 total cellular activity and protein levels are regulated by epidermal growth factor receptor. In the presence of co-transfected epidermal growth factor receptor, the activity of wild type isoform CHKA2 is increased 2.5 fold
-
gibberellic acid
-
stimulates
putrescine
-
slight stimulation
-
spermidine
-
stimulates
spermine
-
required for maximal activity
spermine
-
in presence of sufficient amounts of Mg2+; stimulates
spermine
-
stimulates
Zinc
-
intacellular zinc depletion resulted in a concentration-dependent induction of CKI1 expression
isopropyl-beta-D-thiogalactoside
-
recombinant protein expression is induced with 1 mM
additional information
-
activation of choline kinase is essential for building membranes, cell growth, cell proliferationand for rebuilding phospholipids that are degraded in the process of signal transductiony
-
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.
-
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.04
-
ATP
-
liver enzyme
0.09
-
ATP
-
pH 9.5, 30C
0.14
-
ATP
-
pH 8.5, 25C
0.4
-
ATP
P35790, Q9Y259
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication; wild type isoform ChoKalpha2, pH and temperature not specified in the publication; wild type isoform ChoKbeta, pH and temperature not specified in the publication
0.486
-
ATP
-
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25C
0.55
-
ATP
P35790, Q9Y259
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
0.65
-
ATP
P35790, Q9Y259
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
0.7
-
ATP
-
isozyme CKB-2, pH 10.0, 37C
0.7
-
ATP
P35790, Q9Y259
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
0.76
-
ATP
P35790, Q9Y259
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
0.95
-
ATP
Culex pipiens fatigans
-
-
1
-
ATP
-
30C, pH 8.0
1
-
ATP
-
C252S mutant enzyme, pH 10, 37C; N308Q mutant enzyme, pH 10, 37C
1
-
ATP
-
brain enzyme
1.2
-
ATP
-
N354A mutant enzyme, pH 10, 37C
1.3
-
ATP
-
D255D mutant enzyme, pH 10, 37C
1.5
-
ATP
-
N308D mutant enzyme, pH 10, 37C
1.5
-
ATP
-
kidney enzyme
1.7
-
ATP
-
E134A mutant enzyme, pH 10, 37C; N87A mutant enzyme, pH 10, 37C; wild type enzyme including His-tag, pH 10, 37C
1.9
-
ATP
-
H253A mutant enzyme, pH 10, 37C; S85T mutant enzyme, pH 10, 37C
2
-
ATP
-
N308A mutant enzyme, pH 10, 37C
2.2
-
ATP
-
E125D mutant enzyme, pH 10, 37C; R149A mutant enzyme, pH 10, 37C; W387A mutant enzyme, pH 10, 37C
2.3
-
ATP
-
R149K mutant enzyme, pH 10, 37C
2.4
-
ATP
-
isozyme CKA-2, pH 10.0, 37C
2.4
-
ATP
-
wild type enzyme, pH 10, 37C
2.5
-
ATP
-
S86A mutant enzyme, pH 10, 37C
2.5
-
ATP
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37C
3.1
-
ATP
-
N260A mutant enzyme, pH 10, 37C
3.2
-
ATP
-
E125A mutant enzyme, pH 10, 37C
4.2
-
ATP
-
E125Q mutant enzyme, pH 10, 37C
4.5
-
ATP
-
E151A mutant enzyme, pH 10, 37C
5.4
-
ATP
-
E303A mutant enzyme, pH 10, 37C
6.9
-
ATP
-
E303D mutant enzyme, pH 10, 37C
7
-
ATP
-
R111A mutant enzyme, pH 10, 37C
8.8
-
ATP
-
E303Q mutant enzyme, pH 10, 37C
45
-
ATP
-
E320A mutant enzyme, pH 10, 37C
0.444
-
beta-Methylcholine
-
30C, pH 8.0
0.444
-
beta-Methylcholine
-
30C
0.002
-
choline
-
dimer
0.013
-
choline
-
pH 8.5, 37C
0.013
-
choline
-
liver enzyme
0.014
-
choline
-
brain enzyme
0.021
-
choline
P35790, Q9Y259
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication
0.03
-
choline
-
-
0.0314
-
choline
-
-
0.032
-
choline
-
isozyme CK-beta
0.033
-
choline
-
-
0.033
-
choline
P35790, Q9Y259
wild type isoform ChoKbeta, pH and temperature not specified in the publication
0.041
-
choline
P35790, Q9Y259
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
0.043
-
choline
-
pH 9.0
0.055
-
choline
-
isozyme CK-alpha1/beta
0.07
-
choline
-
in 100 mM Tris-HCl buffer (pH 7.5) containing 100 mM KCl, 10 mM MgCl2, 0.5 mM phosphoenolpyruvate, 0.25 mM NADH, 4 units pyruvate kinase, and 5 units lactate dehydrogenase
0.083
-
choline
-
isozyme CK-alpha
0.086
-
choline
P35790, Q9Y259
wild type isoform ChoKalpha2, pH and temperature not specified in the publication
0.1
-
choline
-
kidney enzyme
0.102
-
choline
P35790, Q9Y259
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
0.107
-
choline
P35790, Q9Y259
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
0.1353
-
choline
Q8IM71
recombinant protein
0.145
-
choline
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37C
0.157
-
choline
-
N-terminal truncated enzyme version of CK-beta
0.18
-
choline
P35790, Q9Y259
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
0.188
-
choline
-
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25C
0.2
-
choline
-
-
0.27
-
choline
-
pH 9.5, 30C
0.4
-
choline
-
N260A mutant enzyme, pH 10, 37C
0.42
-
choline
-
-
0.57
-
choline
-
-
0.7
-
choline
-
R149A mutant enzyme, pH 10, 37C; S85T mutant enzyme, pH 10, 37C
0.77
-
choline
-
in 100 mM Tris-HCl (pH 8.5), at 37C
0.8
-
choline
-
E125D mutant enzyme, pH 10, 37C; N308Q mutant enzyme, pH 10, 37C
1
-
choline
-
C252S mutant enzyme, pH 10, 37C; N308D mutant enzyme, pH 10, 37C; N354A mutant enzyme, pH 10, 37C; wild type enzyme including His-tag, pH 10, 37C
1.1
-
choline
-
E125A mutant enzyme, pH 10, 37C
1.2
-
choline
-
R149K mutant enzyme, pH 10, 37C; W387A mutant enzyme, pH 10, 37C
1.5
-
choline
-
N308A mutant enzyme, pH 10, 37C
1.6
-
choline
-
isozyme CKA-2, pH 10.0, 37C
1.6
-
choline
-
E125Q mutant enzyme, pH 10, 37C; H253A mutant enzyme, pH 10, 37C; wild type enzyme, pH 10, 37C
1.7
-
choline
-
R111A mutant enzyme, pH 10, 37C
1.8
-
choline
-
E134A mutant enzyme, pH 10, 37C; N87A mutant enzyme, pH 10, 37C
2.2
-
choline
-
E151A mutant enzyme, pH 10, 37C
2.6
-
choline
-
-
3
-
choline
-
E320A mutant enzyme, pH 10, 37C
3.4
-
choline
-
E303Q mutant enzyme, pH 10, 37C
3.6
-
choline
-
E303D mutant enzyme, pH 10, 37C
5
-
choline
-
S86A mutant enzyme, pH 10, 37C
5.4
-
choline
-
D255D mutant enzyme, pH 10, 37C
10
-
choline
-
E303A mutant enzyme, pH 10, 37C
13
-
choline
-
isozyme CKB-2, pH 10.0, 37C
0.787
-
ethanolamine
-
30C, pH 8.0
0.787
-
ethanolamine
-
30C
1.2
-
ethanolamine
-
30C, pH 8.0
1.2
-
ethanolamine
-
pH 8.5, 37C
1.2
-
ethanolamine
-
30C
2.01
-
ethanolamine
-
-
2.56
-
ethanolamine
-
-
5
-
ethanolamine
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37C
8.1
-
ethanolamine
-
pH 9.0
0.025
-
N,N-diethylethanolamine
-
30C, pH 8.0
0.025
-
N,N-diethylethanolamine
-
pH 9.6, 37C
0.4
-
N,N-Diisopropylethanolamine
-
30C, pH 8.0
0.4
-
N,N-Diisopropylethanolamine
-
30C
0.208
-
N,N-Dimethylaminopropanol
-
30C, pH 8.0
0.208
-
N,N-Dimethylaminopropanol
-
30C
0.022
-
N,N-dimethylethanolamine
-
30C, pH 8.0
0.022
-
N,N-dimethylethanolamine
-
30C
0.085
-
N,N-dimethylethanolamine
-
pH 9.0
0.118
-
N-Monomethylethanolamine
-
30C, pH 8.0
0.118
-
N-Monomethylethanolamine
-
30C
3.7
-
N-Monomethylethanolamine
-
cosubstrate ATP
3.7
-
N-Monomethylethanolamine
-
-
0.94
-
dimethylethanolamine
-
in 100 mM Tris-HCl (pH 8.5), at 37C
additional information
-
ethanolamine
Q8IM71
above 500 mM
12.01
-
ethanolamine
-
-
additional information
-
additional information
-
Km of MgATP2-: 10 mM, in presence of equimolar amounts of ATP and Mg2+, 1.5 mM, in 2.5-fold higher concentration of Mg2+ than ATP
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
Culex pipiens fatigans
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
TURNOVER NUMBER [1/s]
TURNOVER NUMBER MAXIMUM[1/s]
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.24
-
choline
-
N260A mutant enzyme, pH 10, 37C
0.25
-
choline
-
D255D mutant enzyme, pH 10, 37C
2.4
-
choline
-
W387A mutant enzyme, pH 10, 37C
2.55
-
choline
-
per subunit
2.6
-
choline
-
N354A mutant enzyme, pH 10, 37C
2.92
-
choline
P35790, Q9Y259
wild type isoform ChoKbeta, pH and temperature not specified in the publication
4.58
-
choline
P35790, Q9Y259
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
7
-
choline
-
E303A mutant enzyme, pH 10, 37C
9.5
-
choline
P35790, Q9Y259
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
9.8
-
choline
-
S86A mutant enzyme, pH 10, 37C
12.91
-
choline
-
pH 7.8, 37C, assay with recombinantly expressed enzyme
14
-
choline
P35790, Q9Y259
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication
20.8
-
choline
-
N308A mutant enzyme, pH 10, 37C
21
-
choline
-
E125A mutant enzyme, pH 10, 37C
27.1
-
choline
-
R111A mutant enzyme, pH 10, 37C
29.7
-
choline
-
N87A mutant enzyme, pH 10, 37C
31.4
-
choline
-
E125Q mutant enzyme, pH 10, 37C
35.7
-
choline
-
S85T mutant enzyme, pH 10, 37C
37.5
-
choline
-
N308Q mutant enzyme, pH 10, 37C
38.7
-
choline
-
E303D mutant enzyme, pH 10, 37C
38.9
-
choline
-
R149A mutant enzyme, pH 10, 37C
42.9
-
choline
-
H253A mutant enzyme, pH 10, 37C
47.33
-
choline
P35790, Q9Y259
wild type isoform ChoKalpha2, pH and temperature not specified in the publication
49.5
-
choline
P35790, Q9Y259
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
58.7
-
choline
-
E303Q mutant enzyme, pH 10, 37C
71
-
choline
-
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25C
71.5
-
choline
-
in 100 mM Tris-HCl buffer (pH 7.5) containing 100 mM KCl, 10 mM MgCl2, 0.5 mM phosphoenolpyruvate, 0.25 mM NADH, 4 units pyruvate kinase, and 5 units lactate dehydrogenase
72.3
-
choline
-
wild type enzyme including His-tag, pH 10, 37C
74
-
choline
-
wild type enzyme, pH 10, 37C
76.83
-
choline
P35790, Q9Y259
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
79.9
-
choline
-
E320A mutant enzyme, pH 10, 37C
84.3
-
choline
-
C252S mutant enzyme, pH 10, 37C
84.6
-
choline
-
N308D mutant enzyme, pH 10, 37C
87.9
-
choline
-
R149K mutant enzyme, pH 10, 37C
89.2
-
choline
-
E151A mutant enzyme, pH 10, 37C
97.3
-
choline
-
E134A mutant enzyme, pH 10, 37C
130
-
choline
-
E125D mutant enzyme, pH 10, 37C
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.014
-
choline
-
pH 8.5, 37C
2
-
ethanolamine
-
pH 8.5, 37C
5.5
-
ethanolamine
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37C
0.00021
-
hemicholinium-3
P35790, Q9Y259
wild type isoform ChoKalpha1, pH and temperature not specified in the publication
0.00023
-
hemicholinium-3
P35790, Q9Y259
wild type isoform ChoKalpha2, pH and temperature not specified in the publication
0.00045
-
hemicholinium-3
P35790, Q9Y259
isoform ChoKalpha2 mutant F352A, pH and temperature not specified in the publication
0.005
-
hemicholinium-3
P35790, Q9Y259
isoform ChoKbeta mutant F352L, pH and temperature not specified in the publication
0.008
-
hemicholinium-3
P35790, Q9Y259
isoform ChoKbeta mutant F352A, pH and temperature not specified in the publication
0.016
-
hemicholinium-3
P35790, Q9Y259
isoform ChoKalpha2 mutant F352L, pH and temperature not specified in the publication
0.116
-
hemicholinium-3
P35790, Q9Y259
wild type isoform ChoKbeta, pH and temperature not specified in the publication
3.45
-
phosphocholine
-
in 100 mM Tris/HCl, 6 mM MgCl2, 5 mM ATP, pH 8.8, at 37C
0.9
-
SAR97276
Q8IM71
calculated from Dixon analysis
1.03
-
SAR97276
Q8IM71
calculated from Lineweaver-Burk analysis
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.0528
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0528 mM
0.0842
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0842 mM
0.0084
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0084 mM
0.0072
-
1,1'-(benzene-1,3-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0072 mM
0.0375
-
1,1'-(benzene-1,3-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0375 mM
0.0377
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0377 mM
0.024
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.024 mM
0.0097
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0097 mM
0.0029
-
1,1'-(benzene-1,4-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0029 mM
0.015
-
1,1'-(benzene-1,4-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.015 mM
0.0119
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: 0.0119 mM
0.0206
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0206 mM
0.0012
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0012 mM
0.0005
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0005 mM
0.0019
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0019 mM
0.0058
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0058 mM
0.0026
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0026 mM
0.0015
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0015 mM
0.0021
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0021 mM
0.147
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.147 mM
0.0012
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0012 mM
0.0057
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
0.0044
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0044 mM
0.0013
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0013 mM
0.00043
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.00043 mM
0.0004
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0004 mM
0.0568
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0568 mM
0.0096
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0096 mM
0.0031
-
1,1'-(biphenyl-3,3'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0031 mM
0.2
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-3-methylquinolinium) dibromide
-
IC50: above 0.2 mM
0.0633
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: 0.0633 mM
0.0811
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-aminoquinolinium) dibromide
-
IC50: 0.0811 mM
0.0022
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.0022 mM
0.0088
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.0088 mM
0.0111
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: 0.0111 mM
0.0034
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0034 mM
0.0018
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0018 mM
0.002
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.002 mM
0.0461
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0461 mM
0.0198
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.0198 mM
0.0114
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0114 mM
0.0397
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0397 mM
0.0178
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0178 mM
0.0043
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: 0.0043 mM
0.003
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.003 mM
0.0961
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0961 mM
0.0206
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0206 mM
0.0114
-
1,1'-(biphenyl-4,4'-diyldimethanediyl)bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0114 mM
0.08
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-aminoquinolinium)
-
-
0.0006
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis(4-azepan-1-ylquinolinium)
-
-
0.0102
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(dimethylamino)quinolinium]
-
-
0.0023
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-(phenylamino)quinolinium]
-
-
0.0048
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.0014
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[4-[methyl(phenyl)amino]quinolinium]
-
-
0.0575
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
0.133
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
0.009
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-(dimethylamino)quinolinium]
-
-
0.0057
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.0035
-
1,1'-(ethane-1,2-diyldibenzene-4,1-diyl)bis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
0.01109
-
1,1'-biphenyl-3,3'-diylbis(4-amino-3-methylquinolinium)
-
-
0.0206
-
1,1'-biphenyl-3,3'-diylbis(4-amino-7-chloroquinolinium)
-
-
0.0012
-
1,1'-biphenyl-3,3'-diylbis(4-aminoquinolinium)
-
-
0.0005
-
1,1'-biphenyl-3,3'-diylbis(4-azepan-1-ylquinolinium)
-
-
0.0012
-
1,1'-biphenyl-3,3'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
-
0.0044
-
1,1'-biphenyl-3,3'-diylbis[4-(dimethylamino)quinolinium]
-
-
0.0013
-
1,1'-biphenyl-3,3'-diylbis[4-(phenylamino)quinolinium]
-
-
0.0021
-
1,1'-biphenyl-3,3'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.0004
-
1,1'-biphenyl-3,3'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
-
0.147
-
1,1'-biphenyl-3,3'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
0.0568
-
1,1'-biphenyl-3,3'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
0.0096
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
-
0.0057
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.0031
-
1,1'-biphenyl-3,3'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
0.0633
-
1,1'-biphenyl-4,4'-diylbis(4-amino-7-chloroquinolinium)
-
-
0.0811
-
1,1'-biphenyl-4,4'-diylbis(4-aminoquinolinium)
-
-
0.0022
-
1,1'-biphenyl-4,4'-diylbis(4-azepan-1-ylquinolinium)
-
-
0.0198
-
1,1'-biphenyl-4,4'-diylbis(7-chloro-4-pyrrolidin-1-ylquinolinium)
-
-
0.0397
-
1,1'-biphenyl-4,4'-diylbis[4-(dimethylamino)quinolinium]
-
-
0.0178
-
1,1'-biphenyl-4,4'-diylbis[4-(phenylamino)quinolinium]
-
-
0.002
-
1,1'-biphenyl-4,4'-diylbis[4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.003
-
1,1'-biphenyl-4,4'-diylbis[4-[methyl(phenyl)amino]quinolinium]
-
-
0.0461
-
1,1'-biphenyl-4,4'-diylbis[7-amino-4-[(4-chlorophenyl)(methyl)amino]-8-methylquinolinium]
-
-
0.0961
-
1,1'-biphenyl-4,4'-diylbis[7-amino-8-methyl-4-[methyl(phenyl)amino]quinolinium]
-
-
0.0206
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-(dimethylamino)quinolinium]
-
-
0.0114
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[(4-chlorophenyl)(methyl)amino]quinolinium]
-
-
0.0114
-
1,1'-biphenyl-4,4'-diylbis[7-chloro-4-[methyl(phenyl)amino]quinolinium]
-
-
0.098
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-piperidin-1-ylpyridinium) dibromide
-
IC50: 0.098 mM
0.1
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-pyrrolidin-1-ylpyridinium) dibromide
-
IC50: above 0.1 mM
0.0482
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: 0.0482 mM
0.1
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis(4-[[(3,5-dichlorophenyl)amino]methyl]pyridinium) dibromide
-
IC50: above 0.1 mM
0.1
-
1,1'-[(1S,2S)-cyclopropane-1,2-diyldiethane-2,1-diyl]bis[4-[(phenylamino)methyl]pyridinium] dibromide
-
IC50: above 0.1 mM
0.2
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-amino-7-chloroquinolinium) dibromide
-
IC50: above 0.2 mM
0.08
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-aminoquinolinium) dibromide
-
IC50: 0.08 mM
0.006
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-azepan-1-ylquinolinium) dibromide
-
IC50: 0.006 mM
0.0048
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0048 mM
0.0575
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-amino-4-[[(4-chlorophenyl)amino]methyl]-8-methylquinolinium) dibromide
-
IC50: 0.0575 mM
0.001
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-pyrrolidin-1-ylquinolinium) dibromide
-
IC50: 0.001 mM
0.0057
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis(7-chloro-4-[[(4-chlorophenyl)amino]methyl]quinolinium) dibromide
-
IC50: 0.0057 mM
0.0102
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.0102 mM
0.0023
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-(phenylamino)quinolinium] dibromide
-
IC50: 0.0023 mM
0.0014
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0014 mM
0.133
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-amino-8-methyl-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.133 mM
0.009
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-(dimethylamino)quinolinium] dibromide
-
IC50: 0.009 mM
0.0035
-
1,1'-[ethane-1,2-diylbis(benzene-4,1-diylmethanediyl)]bis[7-chloro-4-[(phenylamino)methyl]quinolinium] dibromide
-
IC50: 0.0035 mM
0.00621
-
1-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]benzyl)-4-(dimethylamino)pyridinium bromide
P35790
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37C
-
0.0389
-
1-[4-(4-[4-[(6-amino-3H-purin-3-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
P35790
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37C
-
0.0107
-
1-[4-(4-[4-[(6-amino-9H-purin-9-yl)methyl]phenyl]butyl)benzyl]-4-(dimethylamino)pyridinium bromide
P35790
in 100 mM Tris (pH 8.5), 10 mM MgCl2, at 37C
-
0.0132
-
12,19-diaza-1,8-diazoniapentacyclo[18.2.2.23,6.28,11.214,17]triaconta-1(22),3,5,8,10,14,16,20,23,25,27,29-dodecaene dibromide
-
IC50: 0.0132 mM
0.0021
-
12,21-diaza-1,8-diazoniapentacyclo[20.2.2.23,6.28,11.014,19]triaconta-1(24),3,5,8,10,14,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0021 mM
0.0003
-
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM
0.0003
-
14,21-diaza-1,10-diazoniapentacyclo[20.2.2.210,13.216,19.03,8]triaconta-1(24),3,5,7,10,12,16,18,22,25,27,29-dodecaene dibromide
-
IC50: 0.0003 mM, most potent inhibitor
3.2
-
2-amino-1-butanol
Q8IM71
endogenous enzyme
0.0014
-
4-chloro-N-methylanilino
-
IC50: 0.0014 mM
0.0248
-
5,10,11,16,17,22-hexahydro-6,9:18,21-diethenodibenzo[g,p][1,5,10,14]tetraazacyclooctadecine-6,21-diium dibromide
-
IC50: 0.0248 mM
0.001
-
7-chloro-1-(4-[2-[4-(7-chloro-5-pyrrolidin-1-ylquinolinium-1-yl)phenyl]ethyl]phenyl)-4-pyrrolidin-1-ylquinolinium
-
-
0.005
-
choline kinase inhibitor Mn58b
-
-
-
0.1075
-
choline kinase inhibitor Mn58b
-
-
-
0.057
-
hemicholinium-3
-
weak inhibitor, IC50: 0.057 mM
0.22
-
hemicholinium-3
Q8IM71
endogenous enzyme
0.58
-
hemicholinium-3
Q8IM71
recombinant enzyme
0.0001
-
MN58b
-
H510 cell, 144 h
-
0.00027
-
MN58b
-
H82 cell, 144 h
-
0.0004
-
MN58b
-
H510 cell, 72 h
-
0.0005
0.072
MN58b
-
specific inhibitor, IC50: 0.0005-0.072 mM depending on cell type
-
0.0008
-
MN58b
-
H82 cell, 72 h
-
0.0009
-
MN58b
-
H1299 cell, 144 h
-
0.0011
-
MN58b
-
H460 cell, 144 h; H510 cell, 48 h
-
0.0019
-
MN58b
-
H82 cell, 48 h
-
0.0026
-
MN58b
-
H460 cell, 72 h
-
0.0027
-
MN58b
-
H1299 cell, 72 h
-
0.0034
-
MN58b
-
primary HMEC cell, 144 h
-
0.0042
-
MN58b
-
primary BEC cell, 144 h
-
0.00703
-
MN58b
-
H460 cell, 48 h
-
0.0103
-
MN58b
-
H1299 cell, 48 h
-
0.0183
-
MN58b
-
primary BEC cell, 72 h
-
0.0209
-
MN58b
-
primary HMEC cell, 72 h
-
0.0405
-
MN58b
-
primary BEC cell, 48 h
-
0.0447
-
MN58b
-
primary HMEC cell, 48 h
-
0.52
-
SAR97276
Q8IM71
endogenous enzyme
1.12
-
SAR97276
Q8IM71
recombinant enzyme
0.00047
-
V-11-023907
-
in 100 mM Tris-HCl pH 7.5, 100 mM KCl, 10 mM MgCl2, at 25C
-
SPECIFIC ACTIVITY [µmol/min/mg]
SPECIFIC ACTIVITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
0.000139
-
-
skeletal muscle, hindlimbs of +/+ CK-alpha mice, supernatant of tissue homogenates are incubated in volume of 0.100 ml of reaction buffer at 37C for 30 min. The reaction product, phosphocholine, is separated using an AG1-X8 column.To determine the activity of each CK isoform, supernatant fractions are treated with an antisera raised against GST (control), GST-CK-alpha or GST-CK-beta fusion proteins combined with protein A-Sepharose overnight at 4C, and the supernatant is used.
0.000484
-
-
in 40 mM Tris/HCl with 10 mM MgCl2, 2 mM ATP and 0.25 mM choline, pH 7.4, at 37C
0.0045
-
-
pH 9.0
2.4
-
-
isozyme CKB-2, pH 10.0, 37C
10.67
-
-
2 microgram of purified protein is incubated with a reaction mixture of 100 mM MOPS (pH 7.8), 6 mM MgCl2 and 5 mM ATP, with either 2 mM ethanolamine and 200 nanoCi of [3H]ethanolamine or 2 mM choline and 200 nanoCi of (3H)choline at 37C for 20 min and quenched by boiling at 100C for 5 min. Substrates and products are separated by high-performance TLC using silica 60 plates with methanol/0.6% NaCl/ammonium hydroxide as solvent. Radiolabelled species are detected by fluorography at -70C.
10.8
-
Q8IM71
recombinant protein
17.9
-
-
-
40.4
-
-
30C, pH 8.0
40.4
-
-
30C
43
-
-
isozyme CKA-2, pH 10.0, 37C
143
-
-
pH 8.5, 37C
additional information
-
-
-
additional information
-
-
-
additional information
-
-
exponentially growing cells: 484.04 pmol/mg/min (activity is determined after homogenizing a cell pellet in Tris/HCl buffer. Homogenisate of exponentially growing and confluent cells is centrifugated. Assay mixture containing 40 mM Tris/HCl with unlabelled carrier of 0.25 mM choline, (methyl-3H)choline (37 kBq/sample), 2 mM ATP and 10 mM MgCl2 were added to homogenate protein. After incubation, reaction is stopped by addition of ice-cold mixture of methanol and chloroform and lipid-metabolite extraction is then carried out. Protein content is set for each sample and total radioactivity is determined. Separation of (methyl-3H)-phosphocholine and (methyl-3H)-choline is carried out using ion exchange chromatography)
additional information
-
-
Genes significantly down-regulated by choline kinase: BCL2-interacting killer (apoptosis-inducing), stabilization of the calcium channel, cyclin G2. Inhibition of cell proliferation, T-cell surface protein tactile, cyclin-dependent kinase inhibitor 1A (p21, Cip1), cyclin-dependent kinase inhibitor 1B (p27, Kip1), dual-specificity-(Y)-tyrosine phosphor regulated kinase, Mad signalling (altered response to quimiotherapy), opioid receptor, mu 1 (negative regulat of cell proliferation), retinoblastoma-like 1 (p107) (Rb associated protein), transforming growth factor, beta receptor I, Toll like receptor (antitumoral immunity), immune escape of human cancer, Visinin like 1
additional information
-
-
The specific activity of choline kinase in wild type zinc-depleted cells is 2.7fold greater when compared with the activity from cells grown with 1.5 microM ZnSO4. Choline kinase activity is measured in a reaction mixture that contains 67 mM glycine-NaOH, 5 mM (methyl-14C)choline, 5 mM ATP, 10mM MgSO4 and 1.3 mM dithiothreitol. The radiolabeled product phosphocholine, is separated from the substrate by precipitation of choline as a reineckate salt.
additional information
-
-
increase in mRNA levels results in an increase in protein expression and ChoK enzymatic activity
additional information
-
Q8IM71
62.2 micromol/min/mg for ethanolamine
pH OPTIMUM
pH MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
6.5
-
-
ADP + O-phosphocholine
7.4
-
-
assay at
7.8
-
-
The pH optimum is assessed by measuring choline kinase activities at various pH values from pH 5.0 to pH 9.0
8
9.5
-
-
8
-
Culex pipiens fatigans
-
2 optima: pH 8.0 and pH 9.0, cytosolic enzyme
8
-
-
assay at
8.7
-
-
-
8.8
-
-
assay at
8.8
-
-
assay at
9
-
Culex pipiens fatigans
-
2 optima: pH 8.0 and pH 9.0, cytosolic enzyme
9.2
-
-
-
9.5
-
-
assay at
10
-
-
ATP + choline
10
-
-
isoform CKA-2
pH RANGE
pH RANGE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
7.5
9
-
pH 7.5: about 30% of maximum activity, pH 9.0: about 45% of maximum activity
8.5
10.5
-
about 80% of maximum activity at pH 8.5 and pH 10.5
10.5
-
-
increase of activity up to
TEMPERATURE OPTIMUM
TEMPERATURE OPTIMUM MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
25
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
37
-
-
assay at
37
-
-
assay at
37
-
-
assay at
37
-
-
assay at
pI VALUE
pI VALUE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
4.1
-
-
isoelectric disc gel electrophoresis, isoenzyme C
4.7
4.8
-
isoelectric focusing, isoform CKII
4.7
4.8
-
isoelectric focusing, acidic isoform
4.8
-
-
isoelectric focusing, isoform CKI
5
-
-
isoelectric disc gel electrophoresis, isoenzyme B
10
-
-
isoelectric focusing, basic isoform
SOURCE TISSUE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
SOURCE
-
IBEC (CC-2541), primary bronchial epithelial cell
Manually annotated by BRENDA team
-
nerve endings from forebrains
Manually annotated by BRENDA team
-
strainn 427 is used for isolation of RNA
Manually annotated by BRENDA team
Culex pipiens fatigans
-
-
Manually annotated by BRENDA team
-
high expression of the beta subtype
Manually annotated by BRENDA team
-
Transfection of human HeK293T is carried out by the calcium phosphate method. The amount of plasmidic DNA is kept constant at 2 microg with the corresponding empty vector. Tumors induced by ChoK alpha over-expression in Hek293T are removed from the mice to generate the ChoK tumoral cell line ADJ. Different slices of the tissue are placed into culture 100mm dishes and treated with trypsin and 1 mg/ml of G418 to avoid murine cells contamination. The resultant cell line ADJ displays constitutive ChoK alpha activation and a fully transformed phenotype
Manually annotated by BRENDA team
-
CC-2551, primary mammary epithelial cell
Manually annotated by BRENDA team
Culex pipiens fatigans
-
-
Manually annotated by BRENDA team
-
high expression of the alpha and beta subtype
Manually annotated by BRENDA team
-
subtype alpha
Manually annotated by BRENDA team
O54804
from male mice C57B16 (12 weeks old); Male C57Bl6 mice (12 weeks old) are injected intraperitoneally with carbon tetrachloride dissolved in olive oil at the dosage of 3 ml/kg. Mice are killed at indicated times and the livers quickly removed.
Manually annotated by BRENDA team
-
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.
Manually annotated by BRENDA team
-
HMEC cell line, a spontaneously immortalized nonmalignant mammary epithelial cell line
Manually annotated by BRENDA team
-
; human breast cancer cell line
Manually annotated by BRENDA team
-
estrogen receptor-positive poorly metastatic breast cancer cell line
Manually annotated by BRENDA team
-
invasive estrogen receptor-negative cell line
Manually annotated by BRENDA team
-
of the intestine
Manually annotated by BRENDA team
-
non-small cell lung cancer epithelial cell line
Manually annotated by BRENDA team
-
non-small cell lung cancer epithelial cell line
Manually annotated by BRENDA team
-
small cell lung cancer cell line
Manually annotated by BRENDA team
-
small cell lung cancer cell line
Manually annotated by BRENDA team
-
prostate cancer cell
Manually annotated by BRENDA team
-
forelimb, hindlimb
Manually annotated by BRENDA team
-
choline kinase beta is the major isoform in hindlimb muscle and contributes more to choline kinase activity, while choline kinase alpha is predominant in forelimb muscle and contributes more to choline kinase activity
Manually annotated by BRENDA team
-
high expression of the alpha subtype
Manually annotated by BRENDA team
Culex pipiens fatigans
-
-
Manually annotated by BRENDA team
-
strains W303-1A,DY1457, ZHY6, ZHY3, SH304, SH303, SH307
Manually annotated by BRENDA team
additional information
-
parasites isolated from infected human erythrocytes
Manually annotated by BRENDA team
MOLECULAR WEIGHT
MOLECULAR WEIGHT MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
48000
-
-
SDS-PAGE
52000
-
-
CHKA
52000
-
-
-
52000
-
-
estimated from amino acid sequence
52070
-
-
calculation from amino acid sequence
52200
-
-
calculated from amino acid sequence
56000
-
-
SDS-PAGE, recombinant protein
67000
-
-
gel filtration
72610
-
-
determined by MALDI-TOF-MS
75000
80000
-
gel filtration
75000
80000
-
-
87600
-
-
sucrose density gradient centrifugation, gel filtration
160000
-
-
gel filtration
SUBUNITS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
?
-
isoform CKB-2: x * 40600, SDS-PAGE, x * 42000, deduced from gene sequence
?
-
x * 44000, SDS-PAGE
?
-
x * 14400, basic isoform
?
-
x * 44000, the parasite has two potential 53000 and 44000 Da isoforms, SDS-PAGE; x * 53000, the parasite has two potential 53000 and 44000 Da isoforms, SDS-PAGE; x * 70000, full-length enzyme, SDS-PAGE
dimer
-
2 * 44000, brain enzyme, SDS-PAGE
dimer
-
2 * 42000, kidney enzyme, SDS-PAGE
dimer
-
isoform CKA-2: x * 48600, SDS-PAGE, x * 49000, deduced from gene sequence
dimer
-
2 * 73000, SDS-PAGE, 2 * 66300, deduced from gene sequence, enzyme exists also as tetramer and octamer whose amounts increase in the presence of ATP
dimer
-
homodimer, crystal structure
dimer
-
2 * 51000, recombinant enzyme including His-tag, SDS-PAGE, native mass by gel filtration
dimer
-
2 * 52000, glioblastoma enzyme, alpha subtype, homo- or heterodimers formed from alpha and beta subtype
dimer
-
2 * 50000-52000, different molecular weights for splicing variants of the alpha subtype, 20% of enzyme activity, 2 * 45000, beta subtype, 20% of enzyme activity, heterodimer of both subtypes, 1 * 50000-52000 + 1 * 45000, 60% of enzyme activity
dimer
-
enzymes from kidney and brain, 2 * 45000, kidney enzyme, beta subtype
dimer
-
60% of the active enzyme exists as homodimer and 20% as heterodimer
dimer
-
x-ray crystallography
dimer
-
Elution from the gel-filtration column shows that TbC/EK2 exhibited a dimeric state in solution.
homodimer
-
2 * 45000, Western Blot analysis; 2 * 50000, Western Blot analysis; 2 * 52000, Western Blot analysis
homotetramer
-
-
homotetramer
-
4 * 13000
homotetramer
-
4 * 12750
monomer
-
1 * 66000
monomer
-
1 * 52000
oligomer
-
mainly dimers and tetramers, x * 50000
oligomer
Q54AG5
subtype alpha, mainly dimers and tetramers, x * 50000-52000; subtype beta, mainly dimers and tetramers, x * 42000
oligomer
-
mainly dimers
oligomer
-
dimers, tetramers and octamers
tetramer
-
4 * 47000, SDS-PAGE
tetramer
-
2 * 73000, SDS-PAGE, 2 * 66300, deduced from gene sequence, enzyme exists also as dimer and octamer, amount of tetramer and octamer increases in the presence of ATP
tetramer
-
enzyme from liver, 4 * 50000-52000, different molecular weights for splicing variants of the alpha subtype
monomer
Q8IM71
1 * 52000, gel filtration
additional information
-
active form of enzyme consists of alpha/beta hetero-oligomers with small parts of activity expressed by alpha/alpha or beta/beta homo-oligomers
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
additional information
-
enzyme activity is regulated via phosphorylation at S30 and/or S85 by protein kinase A
Crystallization/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
in complex with inhibitor V-11-023907, hanging drop vapor diffusion method, using 0.1 M Bis-Tris (pH 6.5), 25% (w/v) polyethylene glycol 3350, and 0.1 M MgCl2
-
isoform ChoKalpha1 in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M HEPES (pH 7.5), 25% (w/v) polyethylene glycol 3350, and 0.2 M lithium sulfate; isoform ChoKbeta in complex with hemicholinium-3 and ADP, sitting drop vapor diffusion method, using 0.1 M sodium cacodylate (pH 6.5), 30% polyethylene glycol 4000, and 0.2 M ammonium sulfate
P35790, Q9Y259
sitting drop vapour diffusion using 25 mM Tris/HCl (pH 7.5), 25 mM KCl, 0.5 mM dithiothreitol, 0.0005 ml of 0.1 M MgCl2 in 12-20% PEG 3350 with 0.2 M NaF
-
pH STABILITY
pH STABILITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
5
-
-
or below, 2-3 h, 90% or more loss of activity, crude enzyme extract
5.5
10
-
inactivation below and above
TEMPERATURE STABILITY
TEMPERATURE STABILITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
30
-
-
40 min, without Mg2+, 80% loss of activity, + 15 mM Mg2+, 9% loss of activity
39
-
-
10 min, 15 mM Mg2+, 50% loss of activity
GENERAL STABILITY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
very stable, even at a low protein concentration, 0.001 mg/ml
-
choline, ATP, bovine serum albumin and changes in ionic strength do not contribute to the stability of choline kinase
-
loss of activity upon freezing and thawing
-
STORAGE STABILITY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
-18C, enzyme kept frozen for 3 h and thawed, 15 min in contact with ice, complete inactivation, cannot be reactivated
-
-20C, stable without any stabilizing additives
-
4C, stable for at least 1 month
-
0C, 10 mM Tris actetate, pH 7.2, 13 mM 2-mercaptoethanol, 1 mM EGTA, 15 mM MgCl2, stable for 1 week
-
Purification/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
isoforms CKA-2, CKB-2
-
recombinant enzymes using His-tag
-
glutathione affinity column chromatography, Ni-NTA column chromatography, and Superdex 200 gel filtration
-
gluthatione-Sepharose column chromatography, Resource Q column chromatography and Superdex-200 gel filtration
-
HisTrap column chromatography and Superdex 200 gel filtration; HisTrap column chromatography and Superdex 200 gel filtration
P35790, Q9Y259
overview
-
recombinant proteins using GST-tag
-
partial
-
Ni-nitrilotriacetic acid agarose affinity and gel filtration; overexpressed PfCK protein is purified to homogeneity using Ni-nitrilotriacetic acid agarose affinity and gel filtration chromatography
-
Ni-NTA agarose resin column chromatography and 300SW gel filtration
-
copurification of choline kinase and ethanolamine kinase
-
isoforms: CK I, CK II
-
multiple forms
-
two isoforms with greatly different pI
-
Con A column chromatography, Affi-Gel Blue gel filtration and Mono Q column chromatography
-
recombinant enzyme, from Sf-9 insect cells
-
Ni-NTA column chromatography
-
cleared lysate is applied to a HisTrap column column pre-loaded with Ni2+. Unbound proteins are removed by washing the column with 50 mM Tris/HCl, pH 8.0, 300 mM NaCl and 10 mM imidazole, whereas TbC/EK1 and TbC/EK2 are eluted with an imidazole gradient in the same buffer. Fractions containing TbC/EK1 or TbC/EK2 are pooled, dialysed against 50 mM Tris/HCl and 300 mM NaCl and purified further through a Superdex 200 16/60 gel-filtration column.
-
Cloned/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
7 different genes, cloned 5
-
native and mutant enzymes expressed as His-tag fusion protein in Sf9 cells
-
expressed in Escherichia coli BL21DE3pLysS
B0URY8, -
enzyme cloned by complementation of the yeast choline kinase mutation cki
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3) cells; expressed in Escherichia coli BL21(DE3) cells
P35790, Q9Y259
expressed in Escherichia coli strain BL21(DE3)
-
expressed in Escherichia coli; expressed in Escherichia coli
-
overview
-
Small interfering RNA-chk (siRNA) is designed and transfected for 48 h using oligofectamine and Opti-MEM based on the observed decrease of Chk message using reverse transcription-PCR analysis within this time. Immunoblot assay results with Chk antibody shows significant reduction of Chk protein expression levels in MCF-12A, MCF-7, and MDA-MB-231 cells after transient siRNA-chk transfection.
-
The genomic sequence of the putative human chk-alpha promoter is obtained by performing a BLAST search in National Center for Biotechnology Information using the known promoter sequence of the rat chk-a gene as query sequence. A 2.3-kb region at the 5'-end of the human chk-a gene on chromosome 11, immediately upstream of the translation start site, is found to contain several putative HRE sites with the core sequence RCGTG. Due to its high GC content, this 2.3-kb region is cloned as four smaller overlapping fragments, and formamide (5%) is added in all PCRs. The four overlapping sequences are PCR amplified from human genomic DNA. The PCR products of paired sense and antisense primer sequences used for the cloning of these fragments (Chk) are subcloned into the pCR 2.1 TA vector. The full 2.3-kb promoter region is obtained by appropriate endonuclease digestions and ligation of these four overlapping fragments. Each of the four fragments alone, as well as several subligations of two or three consecutive fragments, and the full-length 2.3-kb chk-a promoter are cloned into the pGL4-basic Luc reporter vector.
-
Transfection of human HeK293T is carried out by the calcium phosphate method. The amount of plasmidic DNA is kept constant at 0.2 mg with the corresponding empty vector. Tumors induced by ChoK alpha over-expression in Hek293T are removed from the mice to generate the ChoK tumoral cell line ADJ. Different slices of the tissue are placed into culture 100mm dishes and treated with trypsin and G418 to avoid murine cells contamination. The resultant cell line (ADJ) displays constitutive ChoK alpha activation and a fully transformed phenotype
-
A mouse embryonic stem cell line (XH252, strain 129/OlaHsd) with an insertional mutation in choline kinase alpha is created in a gene-trapping prgram. The vector, pGT1Lxf, is designed to create an in-frame fusion between the 5' exons of the trapped gene and a reporter, betageo (a fusion of beta-galactosidase and neomycin phosphotransferase 2). CK-alpha spans 12 exons on mouse chromosome 19. The insertional mutation in XH252 occurred in intron 5. Thus, the gene-trapped locus is predicted to yield a fusion transcript containing exons 1-5 of CK-alpha and betageo. The embryonic stem cells are injected into C57BL/6 blastocysts to create chimeric mice, which are bred with C57BL/6 mice to generate heterozygous (+/-) CK-alpha-deficient mice. All mice had a mixed genetic background. The mice are weaned at 21 days of age, housed in a barrier facility with a 12-h light-dark cycle, and fed chow containing 4.5% fat. Creating of mice lacking CK- alpha with an embryonic stem cell line containing an insertional mutation in the gene for CK-alpha. Embryos homozygous for the mutant CK-alpha allele are recovered at the blastocyst stage, but not at embryonic day 7.5, indicating that CK-alpha is crucial for the early development of mouse embryos.
-
a series of luciferase vectors that contained the CKalpha promoter and ranged from +57 to -3840 bp is constructed. The vectors are cotransfected into hepa-1 cells with the renilla luciferase expression vector as a control; To identify the region of the CK apha promoter that is important to regulate its transcription, a series of luciferase vectors that contained the CK alpha promoter and ranged from +57 to -3840 bp are constructed. The vectors are cotransfected into Hepa-1 cells with the renilla luciferase expression vector as a control
O54804
encoding isozymes alpha, beta
O54804
expressed in COS-7 cells; expression in COS-7 cells
-
parts of the alpha and beta subtype expressed as GST-fusion protein in Escherichia coli, alpha and beta subtype coexpressed in COS-7 cells
-
expressed in Escherichia coli
-
expressed in Escherichia coli; The RT-PCR-amplified PfCK gene is cloned in pRSET-C, an Escherichia coli expression vector. The host strain is optimized
-
His-tag, expressed in Escherichia coli BL21(DE3)-pRIL
Q8IM71
enzyme expressed in Escherichia coli
-
expressed in Sf9 cells
-
plasmid maintenance and amplification are performed in Escherichia coli strain DH5 alpha
-
expressed in Escherichia coli Rosetta cells and in Saccharomyces cerevisiae KS106 cells
-
molecular cloning and recombinant expression in Escherichia coli strains DH5alpha, XL-1 blue and TOP10. BL21-Gold(DE3) is used for protein overexpression, RNA from bloodstream form of Trypanosoma brucei is used for cDNA synthesis.
-
EXPRESSION
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
hypoxia decrease choline kinase activity and isoform ChKalpha mRNA and protein levels
-
expression levels increase with increasing malignancy of the cell lines, i.e., MDA-MB-231 > MCF-7 > MCF-12A
-
choline kinase activity in forelimb and hindlimb muscle decreases with increasing age from 1 to 8 weeks
-
ENGINEERING
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
C252S
-
slightly increased turnover
D255A
-
no activity detectable
D255A
-
omplete loss of activity
D255E
-
activity almost completely abolished
D255E
-
small residual activity
D255N
-
no activity detectable
D255N
-
small residual activity
D301A
-
no activity detectable
D301A
-
complete loss of activity
D301E
-
no activity detectable
D301E
-
complete loss of activity
D301N
-
no activity detectable
D301N
-
complete loss of activity
D313A
-
low expression level
E125A
-
reduced activity
E125A
-
modest reduction of kcat and Km for ATP
E125D
-
increased turnover
E125D
-
no influence
E125Q
-
reduced activity
E125Q
-
modest reduction of kcat and Km for ATP
E134A
-
slightly increased turnover
E151A
-
slightly increased turnover
E303A
-
strongly reduced activity, increased Km for both substrates, strongly increased Km for Mg2+
E303A
-
strong reduction of the catalytic efficiency
E303D
-
reduced activity
E303D
-
small reduction of kcat
E303N
-
small reduction of kcat
E303Q
-
reduced activity
E320A
-
slightly increased turnover
E320A
-
reduction of ATP affinity and time instability
H181A
-
low expression level
H253A
-
reduced activity
H253A
-
similar initial activity like wild type enzyme, but time instability
N254A
-
similar initial activity like wild type enzyme, but time instability
N260A
-
activity almost completely abolished, strongly increased Km for Mg2+
N260A
-
small residual activity
N308 A
-
small reduction of kcat
N308A
-
reduced activity
N308D
-
slightly increased turnover
N308D
-
modest reduction of kcat
N308Q
-
reduced activity
N308Q
-
modest reduction of kcat
N354A
-
strongly reduced activity, only minor effect on Km for both substrates
N87A
-
reduced activity
N87A
-
small reduction of the catalytic efficiency
R111A
-
reduced activity
R111A
-
4-fold increase in Km for ATP
R149A
-
reduced activity
R149A
-
no influence
R149K
-
slightly increased turnover
S85T
-
reduced activity
S86A
-
strongly reduced activity, increased Km for ATP
S86A
-
pronounced reduction of the catalytic efficiency
S86T
-
moderate reduction of the catalytic efficiency
W387A
-
strongly reduced activity, only minor effect on Km for both substrates
W387A
-
strong reduction of kcat (30-fold)
D255A
-
complete loss of activity
D306A
-
inactive
E125A
-
2-25% catalytic efficiency compared to the wild type enzyme; modest change in kcat/Km with a marked decrease in the affinity for Ca2+ and a significant increase in Km for Mg2+
E255A
-
almost complete loss of activity
E303A
-
10fold decrease in activity
E320A
-
26fold higher Km for ATP
F352A
P35790, Q9Y259
the mutant exhibits a higher turnover number compared to the wild type enzyme
F352L
P35790, Q9Y259
the mutant exhibits a higher turnover number compared to the wild type enzyme
L401A
P35790, Q9Y259
the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme
L401F
P35790, Q9Y259
the mutant of isoform ChoKalpha1 exhibts a lower turnover number compared to the wild type enzyme
N255A
-
complete loss of activity
R111A
-
2-25% catalytic efficiency compared to the wild type enzyme
S86A
-
2-25% catalytic efficiency compared to the wild type enzyme
W387A
-
2-25% catalytic efficiency compared to the wild type enzyme
Y197/333F
-
the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enyzme
Y197F
-
the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enyzme
Y333F
-
the mutant shows reduced activity in the presence of epidermal growth factor receptor compared to the wild type enyzme
S25A
-
mutation results in 32% decrease of phosphatidylcholine synthesis compared to the wild type enzyme
S25D
-
mutation results in 14% increase of phosphatidylcholine synthesis compared to the wild type enzyme
S30A
-
specific activity reduced by 44%, phosphorylation reduced by 70%
S30A/S85A
-
specific activity reduced by 60%, phosphorylation reduced by 83%
S85A
-
specific activity reduced by 8%, phosphorylation reduced by 17%
S25A
Saccharomyces cerevisiae KS106
-
mutation results in 32% decrease of phosphatidylcholine synthesis compared to the wild type enzyme
-
S25D
Saccharomyces cerevisiae KS106
-
mutation results in 14% increase of phosphatidylcholine synthesis compared to the wild type enzyme
-
APPLICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
biotechnology
-
enzyme based assay for choline content of feed
diagnostics
-
prognostic factor in human cancer
diagnostics
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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.
drug development
-
choline kinase is elevated in cancer cells and presents a novel target for increasing cell kill. Data support exploring transient Chk silencing as a broad-spectrum chemotherapeutic agent for cancer cells.
drug development
-
choline kinase is gaining importance as a potential target for anticancer therapy
drug development
-
target for therapy since its specific inhibitors display efficient antitumoral activity in vivo
medicine
-
new enzyme inhibitors with in vivo antitumor activity, mechanism
medicine
-
potential target for anti-tumor drugs, potential use of the enzyme level as tumor marker
medicine
-
target in anti-cancer therapy
medicine
P35790, Q9Y259
the enzyme is implicated in tumorigenesis and an attractive target for anticancer chemotherapy; the enzyme is implicated in tumorigenesis and an attractive target for anticancer chemotherapy
medicine
-
in intact lenses, choline and ethanolamine are phosphorylated independently, during galactosemic cataractogenesis choline and ethanolamine become competing substrates of a single enzyme
biotechnology
-
enzyme based assay for choline content of feed