3.1.4.39: alkylglycerophosphoethanolamine phosphodiesterase
This is an abbreviated version!
For detailed information about alkylglycerophosphoethanolamine phosphodiesterase, go to the full flat file.
Word Map on EC 3.1.4.39
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3.1.4.39
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lysophosphatidic
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lysophosphatidylcholine
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phospholipid
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fibrosis
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lysophospholipids
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atx-lpa
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metastasis
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choline
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protein-coupled
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melanoma
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autocrine
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motility-stimulating
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ectoenzyme
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lpa-producing
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sphingosine
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analysis
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pruritus
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drug development
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ectonucleoside
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lpars
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e-npps
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motogenic
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lpa-induced
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medicine
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molecular biology
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lysophosphatidylserine
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ntpdases
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diagnostics
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diphosphohydrolase
- 3.1.4.39
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lysophosphatidic
- lysophosphatidylcholine
- phospholipid
- fibrosis
- lysophospholipids
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atx-lpa
- metastasis
- choline
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protein-coupled
- melanoma
-
autocrine
-
motility-stimulating
-
ectoenzyme
-
lpa-producing
- sphingosine
- analysis
- pruritus
- drug development
-
ectonucleoside
-
lpars
- e-npps
-
motogenic
-
lpa-induced
- medicine
- molecular biology
- lysophosphatidylserine
- ntpdases
- diagnostics
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diphosphohydrolase
Reaction
Synonyms
(ecto)nucleotide pyrophosphatase/phosphodiesterase 2 [(E)NPP2], ATX, ATX/lysoPLD, ATX/NPP2, AtxB, ATXgamma, autocrine motility factor, autotaxin, autotaxin (ATX), autotaxin beta, autotaxin gamma, autotaxin/lysoPLD, ecto-nucleotide pyrophosphatase/phosphodiesterase-2, ectonucleotide pyrophosphatase phosphodiesterase-2, ectonucleotide pyrophosphatase/phosphodiesterase, ectonucleotide pyrophosphatase/phosphodiesterase 2, ENPP, ENPP2, GDE1, GDE4, GDE7, GDPD1, GDPD3, glycerophosphodiesterase, hATX, Heminecrolysin, human autotaxin, human autotaxin alpha, human autotaxin beta, LPLD, lyso-PLD, lysophospholipase D, lysophospholipase-D, lysoPLD, lysoPLD autotaxin, lysoPLD/NPP2, mATX, mATXgamma, More, NPP-2, NPP2, NPP2alpha, NPP2gamma, nucleotide phosphodiesterase/pyrophosphatase (NPP), nucleotide pyrophosphatase-phosphodiesterase, nucleotide pyrophosphatase/phosphodiesterase 2, PD-Ialpha, PD-Ialpha/ATX, phosphodiesterase Ialpha, phosphodiesterase Ialpha/autotoxin, phosphodiesterase, alkylglycerophosphorylethanolamine, PLD, rhATX S48, zATX
ECTree
3.1.4.39 alkylglycerophosphoethanolamine phosphodiesteraseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.1.4.39 - alkylglycerophosphoethanolamine phosphodiesterase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(5Z)-2-(4-ethylpiperazin-1-yl)-5-(4-fluorobenzylidene)-1,3-thiazol-4(5H)-one
93.8% inhibition at 0.01 mM
(5Z)-2-(azepan-1-yl)-5-(4-propoxybenzylidene)-1,3-thiazol-4(5H)-one
96.6% inhibition at 0.01 mM
(5Z)-2-(morpholin-4-yl)-5-[4-(pentyloxy)benzylidene]-1,3-thiazol-4(5H)-one
93.3% inhibition at 0.01 mM
(5Z)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
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-
(5Z)-5-(2-chlorobenzylidene)-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
96.1% inhibition at 0.01 mM
(5Z)-5-(3,4-dichlorobenzylidene)-2-[4-[4-(dihydroxymethyl)benzyl]piperazin-1-yl]-1,3-thiazol-4(5H)-one
(5Z)-5-(3,4-dimethoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
(5Z)-5-(4-ethoxy-3-methoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
1-acyl glycerol 3-phosphate
-
also fatty alcohol phosphates (structurally 1-acyl glycerol 3-phosphate analogs)
1-arachidonoyl-lysophosphatidic acid
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Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-arachidoyl-lysophosphatidic acid
-
Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-bromo-3(s)-hydroxy-4-(palmitoyloxy) butylphosphonate
-
inhibitory in vitro and in vivo
1-hexanoyl-lysophosphatidic acid
-
Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-linoleoyl-lysophosphatidic acid
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Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-stearoyl-lysophosphatidic acid
-
Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
2-(4-[[(2,3-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
72.3% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2,4,6-mesitylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
53.5% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
mixed inhibition, 5.4% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
63.2% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
83.5% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
77.3% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
68.4% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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97.6% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(2-methylesterphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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51.2% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3,5-bis(trifluoromethyl)phenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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competitive inhibition, 34.1% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
competitive inhibition, 30.4% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
competitive inhibition, 28.6% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
mixed inhibition, 9.7% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
40.5% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
mixed inhibition, 8.6% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
40.9% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
competitive inhibition, 41.9% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
competitive inhibition, 0.3% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-carboxylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
72.7% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
competitive inhibition, 42.4% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-dimethylaminonaphthylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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59.9% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
48.9% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
mixed inhibition, 32.7% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
79.7% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
49.9% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-morpholinosulfonylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
64.1% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-pyrazolephenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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68.6% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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noncompetitive inhibition, 36.2% residual activity at 0.001 mM using FS-3 as substrate
2-(4-[[(phenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid phenyl
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56.4% residual activity at 0.001 mM using FS-3 as substrate
2-amino-2-(2-(4-octylphenyl) ethyl)propan-1,3-diol
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synonyms FTY720, finolimod, competitive inhibition
3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
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3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-3-methoxyphenoxy)methyl]benzoic acid
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competitive inhibition, 35% residual ATX activity at 0.005 mM
3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
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competitive inhibition, 7% residual ATX activity at 0.005 mM
4-(5-[(4,6-dioxo-2-thioxotetrahydropyrimidin-5(2H)-ylidene)methyl]furan-2-yl)benzenesulfonamide
90.1% inhibition at 0.01 mM
4-amino-6-(2-[4'-[(E)-(8-amino-1-hydroxy-5,7-disulfonaphthalen-2-yl)diazenyl]-3,3'-dimethoxybiphenyl-4-yl]hydrazinyl)-5-hydroxynaphthalene-1,3-disulfonic acid
99.0% inhibition at 0.01 mM
4-amino-6-(2-{4'-[(E)-(8-amino-1-hydroxy-5,7-disulfonaphthalen-2-yl)diazenyl]-3,3'-dimethoxybiphenyl-4-yl}hydrazinyl)-5-hydroxynaphthalene-1,3-disulfonic acid
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26.2% inhibition at 0.01 mM
4-chloro-N-methyl-N-{2-[2-(methylsulfonyl)hydrazinyl]-2-oxoethyl}benzenesulfonamide
70.7% inhibition at 0.01 mM
4-chloro-N-methyl-N-{2-[2-(methylsulfonyl)hydrazinyl]-2-oxoethyl}benzenesulfonamide (non-preferred name)
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99.9% inhibition at 0.01 mM
4-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]butane-1-sulfonic acid
4-{5-[(4,6-dioxo-2-thioxotetrahydropyrimidin-5(2H)-ylidene)methyl]furan-2-yl}benzenesulfonamide
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47.1% inhibition at 0.01 mM
5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
bis(para-nitrophenyl)phosphate
-
inhibition above a concentration of 1 mM
bovine serum albumin
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concentration-dependent inhibition on lysoPLD activity in egg white during 24 h incubation
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cyclohexanaminium hydrogen [4-([3-[2-(2-methoxyethoxy)ethoxy]propanoyl]amino)benzyl]phosphonate
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cyclohexanaminium hydrogen [fluoro[4-(heptanoylamino)phenyl]methyl]phosphonate
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cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate
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cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate
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cyclohexanaminium hydrogen [[4-(heptanoylamino)phenyl](hydroxy)methyl]phosphonate
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FTY720P
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binds apo-ATX and an ATX with bound FS-3/products complex, noncompetitive/mixed inhibition
G protein
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G protein exhibits lysoPLD activity, lysoPLD activity is highly associated with heterotrimeric G protein
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Globomycin
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Treatment with the signal peptidase inhibitor inhibits ATX secretion by adipocytes treated for 6 h
Human serum albumin
could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears; could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears
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Ki16425
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inhibits the migratory response of lysophosphatidic acid1-expressing cells to both lysophosphatidic acid and ATX
lactacystin
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proteasome inhibitor, restores the detection of ATX in cell homogenate of the mutants DELTAV12-V22 and DELTAV12-G27, Synthesis and secretion of ATX are highly dependent on the hydrophobic core of the signal peptide, but not on the amino acid composition the putative signal peptidase cleavage site
lysozyme
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concentration-dependent inhibition on lysoPLD activity in egg white during 24 h incubation
-
murine serum albumin
could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears; could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears
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N-(2-chlorophenyl)-2-([(2E)-2-[1-(pyridin-2-yl)ethylidene]hydrazinyl]carbonothioyl)hydrazinecarbothioamide
N-glycosidase
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treatment with N-glycosidase inhibits lysophospholipase D activity of ATX. N-glycosylation of ATX strongly influences its secretion and its lysoPLD activity
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palmitoyl-lysophosphatidic acid
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concentration-dependent inhibition of lysoPLD activity in egg white during 24 h incubation. More than 100 microM of lysophosphatidic acid needed to inhibit significantly lysoPLD activity of hen egg white
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid
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[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid
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[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
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i.e. VPC8a202
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid
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[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxypyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
-
-
[(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
-
[(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
-
[(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
-
[(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
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-
[(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
-
[(2R,3S)-4-[4-[(3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
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-
[(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
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[2-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
[3-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
[3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]phenyl]boronic acid
-
mixed-type inhibition, complete inhibition at 0.005 mM
[4-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
(5Z)-5-(3,4-dichlorobenzylidene)-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
-
10.5% inhibition at 0.01 mM
(5Z)-5-(3,4-dichlorobenzylidene)-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
94.9% inhibition at 0.01 mM
(5Z)-5-(3,4-dichlorobenzylidene)-2-(piperazin-1-yl)-1,3-thiazol-4(5H)-one
-
(5Z)-5-(3,4-dichlorobenzylidene)-2-[4-[4-(dihydroxymethyl)benzyl]piperazin-1-yl]-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(3,4-dichlorobenzylidene)-2-[4-[4-(dihydroxymethyl)benzyl]piperazin-1-yl]-1,3-thiazol-4(5H)-one
-
(5Z)-5-(3,4-dimethoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
-
18.1% inhibition at 0.01 mM
(5Z)-5-(3,4-dimethoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
95.3% inhibition at 0.01 mM
(5Z)-5-(3-bromobenzylidene)-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
-
70.9% inhibition at 0.01 mM
(5Z)-5-(3-bromobenzylidene)-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
90.7% inhibition at 0.01 mM
(5Z)-5-(4-chlorobenzylidene)-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
-
6.2% inhibition at 0.01 mM
(5Z)-5-(4-chlorobenzylidene)-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
91.5% inhibition at 0.01 mM
(5Z)-5-(4-ethoxy-3-methoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
-
15.7% inhibition at 0.01 mM
(5Z)-5-(4-ethoxy-3-methoxybenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-1,3-thiazol-4(5H)-one
92.2% inhibition at 0.01 mM
(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-2-(morpholin-4-yl)-1,3-thiazol-4(5H)-one
-
23.7% inhibition at 0.01 mM
(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-2-(morpholin-4-yl)-1,3-thiazol-4(5H)-one
93.2% inhibition at 0.01 mM
(5Z)-5-benzylidene-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
-
69.4% inhibition at 0.01 mM
(5Z)-5-benzylidene-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
97.7% inhibition at 0.01 mM
1,10-phenanthroline
-
inhibitory effects of 1,10-phenanthroline at different concentrations on lysoPLD activity against palmitoyl-lysophosphatidylcholine
1-myristoyl-lysophosphatidic acid
-
competitive inhibition of lysoPLD. Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-oleoyl-lysophosphatidic acid
-
Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
1-palmitoyl-lysophosphatidic acid
-
Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity
4-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]butane-1-sulfonic acid
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4-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]butane-1-sulfonic acid
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5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
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5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
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Cu2+
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the inhibition of extracellular enzyme can be prevented by 2,6-di-tert-butyl-4-hydroxy-methylphenol
EDTA
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inhibitory effects of EDTA at different concentrations on lysoPLD activity against palmitoyl-lysophosphatidylcholine. Inhibitory effect disappears when Mn2+ or Co2+ are added with EDTA to the egg white. Co-addition of Zn2+, Ni2+, or Cu2+ with EDTA results in 2-3times higher lysoPLD activity
EDTA
All isoforms being strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent; All isoforms strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent
EDTA
All isoforms being strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent; All isoforms strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent; strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent
EDTA
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hydrolysis of 1-palmitoyl-glycerophoshorylcholine is inhibited, indicating that a divalent cation is essential for catalytic activity
EGTA
All isoforms being strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent; All isoforms strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent
EGTA
All isoforms being strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent; All isoforms strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent; strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent
H2L 7905958
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competitive inhibition with respect to ATX-mediated FS-3 hydrolysis and non-competitive inhibition with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis
H2L 7905958
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potent ATX inhibitor, complete inhibition of FS-3 hydrolysis at 0.01 mM, competitive inhibitor
HA155
the boron atom on one end of the inhibitor forms a reversible covalent bond with the nucleophile hydroxyl group of Thr209. One of the two boron hydroxyl groups is further stabilized between the two zinc ions, binding structure, overview
hypericin
inhibitor of autotaxin beta; new inhibitor of autotaxin beta; new inhibitor of autotaxin beta
L-histidine
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15-20 mM, noncompetitive, 75% inhibition, inhibition can be reversed by 20fold lower concentrations of zinc or cobalt salts
lysophosphatidic acid
reported as an inhibitor of its own production; reported as an inhibitor of its own production
lysophosphatidic acid
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product inhibition of autotaxin/lysoPLD by lysophosphatidic acid, which is a potent mixed (both competitive and noncompetitive) inhibitor of the hydrolysis of lysoPC by autotaxin/lysoPLD in vitro. Possibility that lysophosphatidic acid regulates its own biosynthesis through feedback inhibition of autotaxin/lysoPLD
lysophosphatidic acid
reported as an inhibitor of its own production; reported as an inhibitor of its own production
lysophosphatidic acid
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0.001 mM, complexed to albumin, competitive and noncompetitive components
Mg2+
concentrations ranging from 0.1 to 1000 mM; concentrations ranging from 0.1 to 1000 mM
Mg2+
concentrations ranging from 0.1 to 1000 mM; manganese inhibits the catalytic activities, concentrations ranging from 0.1 to 1000 mM
N-(2-chlorophenyl)-2-([(2E)-2-[1-(pyridin-2-yl)ethylidene]hydrazinyl]carbonothioyl)hydrazinecarbothioamide
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58.3% inhibition at 0.01 mM
N-(2-chlorophenyl)-2-([(2E)-2-[1-(pyridin-2-yl)ethylidene]hydrazinyl]carbonothioyl)hydrazinecarbothioamide
71.5% inhibition at 0.01 mM
p-hydroxymercuribenzoate
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the inhibition of the microsomal enzyme can be prevented by glutathione and dithiothreitol
PF8380
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the inhibitor shows adequate oral bioavailability and potency in reducing lysophosphatidic acid levels in plasma and at sites of infl ammation
sphingosine-1-phosphate
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Clarification of the structural importance of acyl chain for the inhibitory effect of lysophosphatidic acid on lysoPLD activity. Lysophosphatidic acids with polyunsaturated acyl chains are more potent than those with saturated acyl chains in the inhibition of serum lysoPLD activity; competitive inhibition of lysoPLD
Zn2+
concentrations ranging from 0.1 to 1000 mM; concentrations ranging from 0.1 to 1000 mM
Zn2+
concentrations ranging from 0.1 to 1000 mM; zinc inhibits the catalytic activities, concentrations ranging from 0.1 to 1000 mM
[2-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
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binding structure, overview
[2-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
binding structure, overview
[3-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
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binding structure, overview
[3-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
binding structure, overview
[4-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
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binding structure, overview
[4-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
binding structure, overview
additional information
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several extracts from edible plant seeds (sesame, sunflower, soybean) tested for the inhibition of lysoPLD activity, show a inhibition (>80%) of lysoPLD, fluorometric assay is favored over the spectrophotometric assay, ESI-MS/MS spectrum and MRM spectrum of major lysophosphatidic acids from seed lipid
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additional information
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inhibitor screening of thiazolone derivatives, overview. Screening for specific enzyme inhibitors using TG-mTMP, a highly sensitive fluorescence probe for the enzyme, that consists of enzyme recognition moiety, linker moiety, and fluorophore. It is almost nonfluorescent before the enzymatic reaction, and the enzyme generates strongly fluorescent 6-hydroxy-9-(4-methoxy-2-methylphenyl)-3H-xanthen-3-one with elimination of thymidine monophosphate and formaldehyde. In vitro and In vivo studies and evaluation of optimized inhibitors. No or poor inhibition by (5Z)-2-(azepan-1-yl)-5-(4-propoxybenzylidene)-1,3-thiazol-4(5H)-one, (5Z)-2-(morpholin-4-yl)-5-[4-(pentyloxy)benzylidene]-1,3-thiazol-4(5H)-one, (5Z)-2-(4-ethylpiperazin-1-yl)-5-(4-fluorobenzylidene)-1,3-thiazol-4(5H)-one, and (5Z)-5-(2-chlorobenzylidene)-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
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additional information
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Hypothesis that a protein in hen egg white masks the lysoPLD activity in undiluted egg white, and that dilution at more than 10times results in a high decline of the inhibitory activity
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additional information
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not inhibited by 2-(4-[[(2-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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additional information
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inhibitor development and synthesis, anti and syn forms of the molecules show different effects on the inhibitory potency, homology model docking study, overview
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additional information
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the low hydrophobicity of an inhibitor is a critical factor in its preference for the binding to a noncatalytic binding site over a catalytic binding site in ATX. Structure-activity relationship of inhibition on lysoPLD activity by polyphenols, overview. Resveratrol, caffeine, L-amino acids, tyrosine, phenylalanine, and 3-(3,4-dihydroxyphenyl)alanine, and phenolic antioxidants (propyl gallate, BHT, BHA), methyl (R)-(þ)-2-(4-hydroxyphenoxy)propionate, 3-(4-hydroxyphenyl)-1-propanol, and 4-(4-hydroxyphenyl)-2-butanone are inactive. Also inactive are flavonols kaempferol, tamarixetin, flavones luteolin, apigenin, chrysin, flavanols (+)-catechin, (-)-epicatechin, isoflavones daidzein, genistein; the low hydrophobicity of an inhibitor is a critical factor in its preference for the binding to a noncatalytic binding site over a catalytic binding site in ATX. Structure-activity relationship of inhibition on lysoPLD activity by polyphenols, overview. Resveratrol, caffeine, L-amino acids, tyrosine, phenylalanine, and 3-(3,4-dihydroxyphenyl)alanine, and phenolic antioxidants (propyl gallate, BHT, BHA), methyl (R)-(+)-2-(4-hydroxyphenoxy)propionate, 3-(4-hydroxyphenyl)-1-propanol, and 4-(4-hydroxyphenyl)-2-butanone are inactive. Also inactive are flavonols kaempferol, tamarixetin, flavones luteolin, apigenin, chrysin, flavanols (+)-catechin, (-)-epicatechin, isoflavones daidzein, genistein
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additional information
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possible involement of furin in secretion of ATX by adipocytes tested, furin inhibitor decanoyl-ArgValLysArgchloromethylketone does not modify secretion or lysophospholipase D activity of ATX
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additional information
inhibitor screening of thiazolone derivatives, overview. Screening for specific enzyme inhibitors using TG-mTMP, a highly sensitive fluorescence probe for the enzyme, that consists of enzyme recognition moiety, linker moiety, and fluorophore. It is almost nonfluorescent before the enzymatic reaction, and the enzyme generates strongly fluorescent 6-hydroxy-9-(4-methoxy-2-methylphenyl)-3H-xanthen-3-one with elimination of thymidine monophosphate and formaldehyde. In vitro and In vivo studies and evaluation of optimized inhibitors, inhibitory potencies of monosubstituted and disubstituted aryl-methyl derivatives, overview
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additional information
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not affected by dioleoylphosphatidic acid, 1-oleoyl-glycerol, sphingosine, glycerol 3-phosphate
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