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2.7.1.107: diacylglycerol kinase (ATP)

This is an abbreviated version!
For detailed information about diacylglycerol kinase (ATP), go to the full flat file.

Word Map on EC 2.7.1.107

Reaction

ATP
+
1,2-diacyl-sn-glycerol
=
ADP
 +
1,2-diacyl-sn-glycerol 3-phosphate

Synonyms

1,2-diacylglycerol kinase, 1,2-diacylglycerol kinase epsilon, adenosine 5'-triphosphate:1,2-diacylglycerol 3-phosphotransferase, arachidonoyl-specific diacylglycerol kinase, ATP:diacylglycerol phosphotransferase, DAG kinase, DAG-kinase, DAGK, DAGKalpha, DAGKepsilon, DG kinase, DGK, DGK zeta, DGK-1, DGK-3, DGK-3 diacylglycerol kinase, DGK-alpha, DGK-theta, DGK-zeta, DGK1, DGK2, DGK3, DGK4, DGK5, DGK6, DGK7, DGKA, DGKalpha, DgkB, DGKbeta, DGKdelta, DGKE, DGKepsilon, DGKeta, DGKeta1, DGKeta2, DGKeta3, DGKeta4, DGKgamma, DGKiota, DGKkappa, DGKksi, DGKtheta, DGKzeta, diacylglycerol kinase, diacylglycerol kinase (ATP dependent), diacylglycerol kinase 4, diacylglycerol kinase alpha, diacylglycerol kinase beta, diacylglycerol kinase delta, diacylglycerol kinase epsilon, diacylglycerol kinase eta, diacylglycerol kinase theta, diacylglycerol kinase zeta, diacylglycerol kinase-alpha, diacylglycerol kinase-epsilon, diacylglycerol kinase-zeta, diacylglycerol:ATP kinase, diglyceride kinase, epsilonDGK, eye-specific diacylglycerol kinase, kinase (phosphorylating), 1,2-diacylglycerol, kinase, 1,2-diacylglycerol (phosphorylating), OsDAGK1, Rv2252, sn-1,2-diacylglycerol kinase, type V DGK, YegS, YerQ

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.107 diacylglycerol kinase (ATP)

Inhibitors

Inhibitors on EC 2.7.1.107 - diacylglycerol kinase (ATP)

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-diarachidonoyl phosphatidic acid
about 55% relative activity in the presence of 1.5 mol%
1-arachidoyl-2-arachidonoyl phosphatidic acid
about 70% relative activity in the presence of 1.5 mol%
1-palmitoyl-2-arachidonoyl phosphatidic acid
about 50% relative activity in the presence of 1.5 mol%
1-stearoyl-2-arachidonoyl phosphatidic acid
about 48% relative activity in the presence of 1.5 mol%
1-stearoyl-2-oleoyl phosphatidic acid
about 70% relative activity in the presence of 1.5 mol%
2,3-dioleoylglycerol
-
uncompetitive inhibition of isoforms diacylglycerol kinase alpha and zeta, no inhibition of isoform epsilon. Binds to a site on the alpha and zeta isoforms that is exposed as a consequence of the substrate binding to the active site, the chiral specificity of the isoforms thus mimicks the substrate specificity
2-arachidonoyl glycerol
inhibitor for both of the epsilon or the zeta isoforms of diacylglycerol kinase; inhibitor for both of the epsilon or the zeta isoforms of diacylglycerol kinase
2-oleoyl glycerol
inhibits diacylglycerol kinase epsilon less than does 2-arachidonoyl glycerol; shows similar inhibitory potency for diacylglycerol kinase zeta as 2-arachidonoyl glycerol
4-[bis(4-fluorophenyl)methylidene]piperidine
-
-
5-[(2E)-3-(2-furyl)prop-2-enylidene]-3-[(phenylsulfonyl)amino]2-thioxo-1,3-thiazolidin-4-one
-
adenosine
-
0.5 mM, 5% inhibition of DGK I and 28% inhibition of DGK IV
adenosine 5'-tetraphosphoryl-3-O-(1,2-dihexanoyl)-sn-glycerol
-
-
alpha-thrombin
-
apparent binding parameters of diacylglycerol kinase theta increase following alpha-thrombin stimulation
-
AMP
-
0.5 mM, 18% inhibition of DGK I and 14% inhibition of DGK IV
antineutrophil cytoplasmic antibody
-
selective activation of diacylglycerol kinase
-
ATPgammaS
cAMP
-
0.5 mM, 20% inhibition of DGK I and 15% inhibition of DGK IV
ceramide
-
-
deoxycholate
diacylglycerol
-
above 3.4 mol%, substrate inhibition
dioctanoylglycerol
-
above 3.4 mol%
dioleoylglycerol
-
above 3.4 mol%
ethanol
-
0.5%, 20% inhibition
GTPgammaS
-
0.5 mM, 37% inhibition of DGK I and 32% inhibition of DGK IV
LiCl
more than 50% inhibition at above 200 mM
N-[7-[cyclopropyl(hydroxy)methyl]-2,3-dihydro-1,4-benzodioxin-6-yl]cyclopropanecarboxamide
about 10% inhibition of isoform DGKzeta at 0.1 mM; about 10% inhibition of isoform DGKzeta at 0.1 mM; about 20% inhibition of isoform DGKdelta at 0.1 mM; about 30% inhibition of isoform DGKeta at 0.1 mM; about 50% inhibition of isoform DGKbeta at 0.1 mM; about 70% inhibition of isoform DGKiota at 0.1 mM; KU-8, 0.01 mM significantly inhibits isoform DGKkappa activity by 79%, while almost complete inhibition occurs at 0.02 mM
-
NaCl
more than 50% inhibition at above 200 mM
Nonidet
-
0.5%, 45% inhibition
octyl glucoside
-
enzyme form DGK-I, DGK-II and DGK-III
phorbol ester
-
activation of protein kinase C which inhibits diacylglycerol kinase epsilon binding to retinoblastoma protein. Mimicking of protein kinase C phosphorylation of serine residues by S/D mutations but not S/N mutations within the MARCKS phosphorylation site domain also prevents binding to retinoblastoma protein
phorbol myristate acetate
-
induces the interaction of diacylglycerol kinase gamma with beta2-chimaerin. Simultaneous addition of H2O2 and phorbol myristate acetate synergistically enhances the interaction with concomitant translocation of beta2-chimaerin from cytoplasm to the plasma membrane
phosphate
-
-
phosphatidate
-
moderate
phosphatidic acid
competitive inhibition
phosphatidylcholine
-
enzyme form DGK-I, DGK-II and DGK-III
phosphatidylglycerol
-
inhibits phosphatidylcholine-dependent kinase activity
phosphatidylinositol
-
2.5 mol% results in 50% inhibition of the phosphatidylcholine-dependent kinase activity
phosphatidylinositol 4,5-bisphosphate
potent inhibitor
phosphatidylinositol-(4,5)-bisphosphate
potent inhibitor; potent inhibitor
phosphatidylinositol-4,5-bisphosphate
noncompetitive inhibitor with respect to 1-stearoyl-2-arachidonoyl-sn-glycerol but a competitive inhibitor with respect to ATP
quercetin
-
0.1 mM, 41% inhibition of DGK I and 15% inhibition of DGK IV
R59022
R59949
RhoA
-
V14-RhoA, strong binding to the C-terminal catalytic domain, negative regulation
ritanserin
sodium deoxycholate
at 5 mM
sphingosine
-
inhibits the 150000 Da enzyme
thrombin
-
stimulation results in an increase in the apparent KM of DGKtheta at low concentrations of substrate dioleoylglycerol. Increasing the bulk concentration of dioleoylglycerol returns the apparent KM to the basal value
-
Triton N-101
-
Triton X-100
additional information
-