Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
arachidoyl-lysophosphatidylcholine + H2O
1-arachidoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
behenoyl-lysophosphatidylcholine + H2O
1-behenoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
decanoyl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
hexanoyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
lauroyl-lysophosphatidylcholine + H2O
1-lauroyl-sn-gycerol-3-phosphate + choline
-
-
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
lysophosphatidic acid is a bioactive phospholipid regulating a wide range of cellular responses
-
?
myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
octanoyl-lysophosphatidylcholine + H2O
1-octanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
oleoyl-lysophosphatidylcholine + H2O
1-oleoyl-sn-gycerol 3-phosphate + choline
-
-
-
?
p-nitrophenyl phenylphosphate + H2O
p-nitrophenol + phenylphosphate
-
-
-
?
palmitoyl-lysophosphatidylcholine + H2O
1-palmitoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
stearoyl-lysophosphatidylcholine + H2O
1-stearoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
-
-
-
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
1-O-alkyl-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-sn-glycerol 3-phosphate + choline
i.e. lyso-platelet-activating factor
-
-
?
arachidoyl-lysophosphatidylcholine + H2O
1-arachidoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
behenoyl-lysophosphatidylcholine + H2O
1-behenoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
bis(4-nitrophenyl)phosphate + H2O
?
-
-
-
-
?
caproyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
capryl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
caprylyl-lysophosphatidylcholine + H2O
1-octanoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
lauroyl-lysophosphatidylcholine + H2O
1-lauroyl-sn-gycerol-3-phosphate + choline
-
-
-
?
lyso-phosphatidylcholine + H2O
lyso-phosphatidic acid + choline
-
-
central in some key metabolic deregulations
-
?
lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
lysophosphatidyl ethanolamine + H2O
lysophosphatidic acid + ethanolamine
-
-
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
N-arachidonoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-arachidonoyl-ethanolamine
-
-
-
?
N-oleoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-oleoyl-ethanolamine
-
-
-
?
N-palmitoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoyl-ethanolamine
-
-
-
?
N-palmitoyl-lysoplasmenylethanolamine + H2O
lysoplasmenic acid + N-palmitoyl-ethanolamine
-
-
-
?
N-palmitoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoylethanolamine
-
-
-
?
oleoyl-lysophosphatidylcholine + H2O
1-oleoyl-sn-gycerol 3-phosphate + choline
-
-
-
?
palmitoyl-lysophosphatidylcholine + H2O
1-palmitoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
-
-
bioactive lysophospholipid, in vitro
-
?
stearoyl-lysophosphatidylcholine + H2O
1-stearoyl-sn-gycerol-3-phosphate + choline
-
-
-
?
additional information
?
-
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
-
-
-
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
-
-
-
r
lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
-
-
-
?
lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
best substrate, reaction of EC 3.1.4.5
-
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
-
665507, 678439, 679137, 681910, 695455, 700364, 703366, 704356, 704588, 705323, 705706, 706456, 706564 -
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
-
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
-
lysophosphatidic acid is a bioactive lysophospholipid present in circulating blood
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
lysophosphatidic acid is a bioactive phospholipid regulating a wide range of cellular responses
-
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
-
LPA, lysophosphatidic acid is a bioactive lysophospholipid present in circulating blood
-
?
additional information
?
-
-
There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
-
-
?
additional information
?
-
There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
-
-
?
additional information
?
-
-
There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
-
-
?
additional information
?
-
There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
-
-
?
additional information
?
-
the enzyme converts lysophospholipids such as lysophosphatidylcholine to lysophosphatidic acid
-
-
?
additional information
?
-
-
no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
-
-
?
additional information
?
-
no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
-
-
?
additional information
?
-
-
when recombinant ATX is incubated with ysophosphatidylcholine in the presence of methanol, both lysophosphatidylmethanol and lysophosphatidic acid are produced with a ratio of 1:10, showing that ATX has transphosphatidylation activity in addition to its lysophospholipase D activity
-
-
?
additional information
?
-
-
brain homogenate forms N-palmitoylethanolamine, N-oleoylethanolamine, and anandamide from their corresponding lyso-N-acylphosphatidylethanolamines by a Mg2+-dependent lysophospholipase D, substrate specificity, overview
-
-
?
additional information
?
-
-
the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
-
-
?
additional information
?
-
poor substrate: glycerophospho-N-palmitoylethanolamine
-
-
?
additional information
?
-
-
poor substrate: glycerophospho-N-palmitoylethanolamine
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(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)-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-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-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
90.7% 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
92.2% 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
97.7% inhibition at 0.01 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-chloro-N-methyl-N-{2-[2-(methylsulfonyl)hydrazinyl]-2-oxoethyl}benzenesulfonamide
70.7% 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
-
5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
-
lysophosphatidic acid
reported as an inhibitor of its own production
Mg2+
concentrations ranging from 0.1 to 1000 mM
murine serum albumin
could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears
-
N-(2-chlorophenyl)-2-([(2E)-2-[1-(pyridin-2-yl)ethylidene]hydrazinyl]carbonothioyl)hydrazinecarbothioamide
71.5% inhibition at 0.01 mM
Zn2+
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
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
binding structure, overview
(5Z)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
-
-
1-acyl glycerol 3-phosphate
-
also fatty alcohol phosphates (structurally 1-acyl glycerol 3-phosphate analogs)
1-bromo-3(s)-hydroxy-4-(palmitoyloxy) butylphosphonate
-
inhibitory in vitro and in vivo
3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
-
-
3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-3-methoxyphenoxy)methyl]benzoic acid
-
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
-
competitive inhibition, 7% residual ATX activity at 0.005 mM
bithionol
-
inhibitory in vitro and in vivo
brefeldin-A
-
inhibitor of trans-Golgi transport, inhibits secretion of ATX
EGTA
All isoforms strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent
Globomycin
-
Treatment with the signal peptidase inhibitor inhibits ATX secretion by adipocytes treated for 6 h
hypericin
new inhibitor of autotaxin beta
Ki16425
-
inhibits the migratory response of lysophosphatidic acid1-expressing cells to both lysophosphatidic acid and ATX
lactacystin
-
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
lysophosphatidic acid
reported as an inhibitor of its own production
Mg2+
manganese inhibits the catalytic activities, concentrations ranging from 0.1 to 1000 mM
murine serum albumin
could be a regulator of the circulating autotaxin. When the albumin is a fatty acid-free preparation, this slight inhibition disappears
-
N-glycosidase
-
treatment with N-glycosidase inhibits lysophospholipase D activity of ATX. N-glycosylation of ATX strongly influences its secretion and its lysoPLD activity
-
tunicamycin
-
inhibits secretion of ATX
Zn2+
zinc inhibits the catalytic activities, concentrations ranging from 0.1 to 1000 mM
[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
EDTA
All isoforms being strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent
EDTA
strongly inhibited by increasing concentrations of EDTA, 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
EGTA
strongly inhibited by increasing concentrations of EGTA, 100% inhibition for 100 mM of the chelating agent
hypericin
inhibitor of autotaxin beta
hypericin
new inhibitor of autotaxin beta
EDTA
-
-
EDTA
All isoforms strongly inhibited by increasing concentrations of EDTA, 100% inhibition for 100 mM of the chelating agent
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
-
additional information
-
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.00017
(5Z)-5-(3,4-dichlorobenzylidene)-2-(piperazin-1-yl)-1,3-thiazol-4(5H)-one
Mus musculus
pH 9.0, 37°C
0.000025
(5Z)-5-(3,4-dichlorobenzylidene)-2-[4-[4-(dihydroxymethyl)benzyl]piperazin-1-yl]-1,3-thiazol-4(5H)-one
Mus musculus
pH 9.0, 37°C
0.00023
4-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]butane-1-sulfonic acid
Mus musculus
pH 9.0, 37°C
0.00039
5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
Mus musculus
pH 9.0, 37°C
0.0016 - 0.0026
hypericin
0.00002 - 0.000038
lysophosphatidic acid
0.187 - 0.251
murine serum albumin
-
0.00058
[2-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
Mus musculus
pH 9.0, 37°C
0.000013
[3-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
Mus musculus
pH 9.0, 37°C
0.000022
[4-([4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]methyl)phenyl]boronic acid
Mus musculus
pH 9.0, 37°C
0.00011
(5Z)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
Mus musculus
-
in Tris-HCl buffer (pH 7.4) at 37°C
0.000161
3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
Mus musculus
-
in Tris-HCl buffer (pH 7.4) at 37°C
0.0025
3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-3-methoxyphenoxy)methyl]benzoic acid
Mus musculus
-
in Tris-HCl buffer (pH 7.4) at 37°C
0.0017
3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
Mus musculus
-
in Tris-HCl buffer (pH 7.4) at 37°C
0.0028
hypericin
Mus musculus
tested on murine autotaxin beta
0.000018
lysophosphatidic acid
Mus musculus
reported as an inhibitor of its own production, incubating murine autotaxin beta with lysophosphatidic acid
0.317
murine serum albumin
Mus musculus
incubating murine autotaxin beta with murine serum albumin
-
0.000028
[3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]phenyl]boronic acid
Mus musculus
-
in Tris-HCl buffer (pH 7.4) at 37°C
0.0016
hypericin
Mus musculus
tested on murine autotaxin alpha
0.0026
hypericin
Mus musculus
tested on murine autotaxin gamma
0.00002
lysophosphatidic acid
Mus musculus
reported as an inhibitor of its own production, incubating murine autotaxin gamma with lysophosphatidic acid
0.000038
lysophosphatidic acid
Mus musculus
reported as an inhibitor of its own production, incubating murine autotaxin alpha with lysophosphatidic acid
0.187
murine serum albumin
Mus musculus
incubating murine autotaxin alpha with murine serum albumin
-
0.251
murine serum albumin
Mus musculus
incubating murine autotaxin gamma with murine serum albumin
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
evolution
mouse and human enzymes show high structural homology
physiological function
the enzyme is the predominant contributor to lysophosphatidic acid production in the human body, especially in the blood, and therefore has important roles in various physiological functions, including development of vasculature and lymphocyte trafficking
malfunction
-
down-regulation of endogenous autotaxin expression in 4T1 cells inhibits osteolytic bone metastasis formation independently of primary tumor growth in vivo
malfunction
-
E9.5 ATX null mutants exhibit a failure of neural tube closure, most likely independent of the circulatory failure, which correlates with decreased cell proliferation and increased cell death, obligatory deletion results to embryonic lethality most likely due to aberrant vascular branching morphogenesis and chorio-allantoic fusion
malfunction
-
in Enpp2 knockout mouse embryos, lysosomes in the visceral endoderm cells are fragmented
malfunction
-
adipocyte-specific knockout FATX-KO mice or mice treated with the lysophosphatidic acid receptor antagonist Ki16425 gain more weight and accumulate more adipose tissue than wild-type or control mice fed a high fat diet
malfunction
-
ATX inhibitor bithionol remarkably decreases lymphocyte migration to the intestine and ameliorates both dextran sodium sulfate-induced colitis and CD4-induced ileocolitis, administration of bithionol or 1-bromo-3(s)-hydroxy-4-(palmitoyloxy) butylphosphonate significantly decreases transmigration of splenocytes through high-endothelial-like vessels induced by TNF-alpha
physiological function
-
ATX expression and lysophosphatidic acid signalling are vital for the development of the nervous system, ATX and lysophosphatidic acid are necessary for embryonic HIF-1a expression
physiological function
-
constitutive activationof the Rho-ROCK-LIM kinase pathway by extracellular production of lysophosphatidic acid by the action of autotaxin is required to maintain the large size of lysosomes in visceral endoderm cells
physiological function
-
expression of autotaxin by cancer cells controls osteolytic bone metastasis formation
physiological function
-
autotaxin is a secreted lysophospholipase D that hydrolyzes lysophosphatidylcholine to generate lysophosphatidic acid, a lipid mediator that activates G protein-coupled receptors to evoke various cellular responses. The produced LPAs are delivered from the active site to cognate G protein-coupled receptors through a hydrophobic channel
physiological function
-
GDE1 has a weak activity to generate N-palmitoylethanolamine from its corresponding 1-alkenyl-2-hydroxy-glycero-3-phospho(N-acyl)ethanolamines, suggesting that this enzyme is at least in part responsible for the lysophospholipase D activity in mouse brain
physiological function
-
in a dextran sodium sulfate mouse model, the enzyme expression level is considerably higher in colonic mucosa of chronically developed colitis than in colonic mucosa of acute colitis. The enzyme is required for lymphocyte transmigration, but not for surface expression of b7-integrin and CD11beta on splenocytes that migrated through epithelial cells. The role of the ATX-LPA axis in leukocyte transendothelial migration through induced high endothelial venule-like vessels has no tropism for surface expression of adhesion molecules on leukocytes
physiological function
-
the enzyme is involved in synthesis of lysophosphatidic acid, a phospholipid growth factor acting via lysophosphatidic acid-specific receptors (LPA1R to LPA6R) and involved in several pathologies including obesity. Enzyme expression is up-regulated in obese patients and mice in relationship with insulin resistance and impaired glucose tolerance. Lysophosphatidic acid-specific receptor LPA1R is the most abundant receptor subtype in adipose tissue. Its expression is higher in non-adipocyte cells than in adipocytes and is not altered in obesity. The enzyme increases and receptor LPA1R decreases while preadipocytes differentiate into adipocytes (adipogenesis). Lysophosphatidic acid inhibits adipogenesis through down-regulation of the pro-adipogenic transcription factor PPARgamma2. ATX/LPA signaling impairs glucose homeostasis, regulation of obesity involves the enzyme, overview
physiological function
-
the enzyme is the primary lysophosphatidic acid-producing phospholipase. Enzyme-lysophosphatidic acid, ATX-LPA, signaling is essential for development and has been implicated in a great diversity of (patho)physiological processes, ranging from lymphocyte homing to tumor progression. Isozyme ATX alpha but not ATX beta binds abundantly to cultured mammalian cells in a manner strictly dependent on heparan sulfate. By mediating bindings to heparan sulfate proteoglycans, the isozyme ATXalpha insertion loop likely serves to target LPA production close to the lysophosphatidic acid receptors
physiological function
GDE4 functions as an N-acylethanolamine-generating lysophospholipase D in living cells. The expression of GDE4 increases the levels of most species of lysophosphatidic acid in the cell
additional information
-
a loop region in the catalytic domain is a major determinant for the substrate specificity of the Enpp family enzymes, Asn230 is critical for the recognition of the common phosphate moieties, structure of the ATX active site in the free-form and with bound Zn2+, overview
additional information
-
the catalytic domain shows shallow groove and a deep hydrophobic pocket, and an open tunnel, which forms a sort of T-junction with the shallow groove, substrate binding structure, overview. The enzyme contains a SMB domain that mediates the binding to cell surface integrins
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
DELTA323-375
murine autotaxin gamma isoform, 889 amino acids total
DELTA592-617
ATXalpha isoform, 915 amino acids total
DELTA202-363
-
COS cells transfected with mutated ATX express catalytically inactive phosphodiesterase and lysophospholipase D. Lethality of the ATX-/-embryos. ATX-dependent LPA production is due to the catalytic activity of the enzyme
DELTA323-375
murine autotaxin beta isoform, 863 amino acids total
DELTAA30-G41
-
deletion mutants are generated from plasmid pcDNA-mATX, encompasses furin site
DELTAA30-I33
-
deletion mutants are generated from plasmid pcDNA-mATX, between signal peptidase and furin site
DELTAA36-E40
-
deletion mutants are generated from plasmid pcDNA-mATX
DELTAC25
-
deletion mutants are generated from plasmid pcDNA-mATX, amino acid -3 referring to the potential signal peptidase cleavage site
DELTAE40-P43
-
deletion mutants are generated from plasmid pcDNA-mATX
DELTAG27
-
deletion mutants are generated from plasmid pcDNA-mATX, amino acid -1 referring to the potential signal peptidase cleavage site
DELTAG27-A30
-
deletion mutants are generated from plasmid pcDNA-mATX, contain potential signal peptidase clevage site
DELTAG27-R35
-
deletion mutants are generated from plasmid pcDNA-mATX, encompasses both furin and signal peptidase cleavage sites
DELTAL46-S49
-
deletion mutants are generated from plasmid pcDNA-mATX
DELTAN23
-
deletion mutants are generated from plasmid pcDNA-mATX, amino acid -5 referring to the potential signal peptidase cleavage site
DELTAN23-G27
-
deletion mutants are generated from plasmid pcDNA-mATX, encompasses -1 and -3 amino acids referring to the potential signal peptidase clevage site
DELTAN410
-
deletion mutants are generated from plasmid pcDNA-mATX, contains a N-glycosylation site, point deletion of the amino-acid N410 inhibits lysophospholipase D activity of ATX, does not modify the ATX secretion and strongly inhibits ATX activity
DELTAN53
-
deletion mutants are generated from plasmid pcDNA-mATX, contains a N-glycosylation site, does not modify the ATX secretion and slightly reduces (25%) ATX activity
DELTAN53/DELTAN410
-
deletion mutants are generated from plasmid pcDNA-mATX, two N-glycosylation sites, double point deletion of the amino-acids N53 and N410 inhibits secretion of ATX, without altering the ATX amount in cell homogenate
DELTAP43-L46
-
deletion mutants are generated from plasmid pcDNA-mATX
DELTAR32-R35
-
deletion mutants are generated from plasmid pcDNA-mATX, furine site
DELTAS49-N53
-
deletion mutants are generated from plasmid pcDNA-mATX, contains N-glycosylation site
DELTAV12-G27
-
deletion mutants are generated from plasmid pcDNA-mATX, hydrophobic domain of signal peptide and signal peptide cleavage site, ATX secretion is suppressed
DELTAV12-V22
-
deletion mutants are generated from plasmid pcDNA-mATX, hydrophobic domain of signal peptide, ATX secretion is suppressed
F249A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
F274A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
L213A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
L243A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
M512A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
N230A
-
almost inactive mutant
T209A
-
catalytically inactive
W254A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
Y306A
-
the mutant shows decreased lysoPLD activity and differences in the fatty acid preferences compared to the wild-type enzyme
T210A
-
catalytically inactive
T210A
-
inactive enzyme, generation of a mouse line displaying an inactivated ATX gene product. Lethality of the ATX-/-embryos. ATX-dependent LPA production is due to the catalytic activity of the enzyme. Clone identified, by both PCR and Southern blot as targeted at the Atx locus
additional information
-
deletions of the amino acids N53 and N410 lead to a reduction of the molecular weight of ATX
additional information
-
experiment with ATX-deficient mice. ATX deficiency is lethal at the embryonic stage
additional information
-
generation of adipocyte-specific knockout FATX-KO mice
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Hama, K.; Aoki, J.; Fukaya, M.; Kishi, Y.; Sakai, T.; Suzuki, R.; Ohta, H.; Yamori, T.; Watanabe, M.; Chun, J.; Arai, H.
Lysophosphatidic acid and autotaxin stimulate cell motility of neoplastic and non-neoplastic cells through LPA1
J. Biol. Chem.
279
17634-17639
2004
Mus musculus
brenda
Pradere, J.P.; Tarnus, E.; Gres, S.; Valet, P.; Saulnier-Blache, J.S.
Secretion and lysophospholipase D activity of autotaxin by adipocytes are controlled by N-glycosylation and signal peptidase
Biochim. Biophys. Acta
1771
93-102
2007
Mus musculus
brenda
Savaskan, N.E.; Rocha, L.; Kotter, M.R.; Baer, A.; Lubec, G.; van Meeteren, L.A.; Kishi, Y.; Aoki, J.; Moolenaar, W.H.; Nitsch, R.; Braeuer, A.U.
Autotaxin (NPP-2) in the brain: cell type-specific expression and regulation during development and after neurotrauma
Cell. Mol. Life Sci.
64
230-243
2007
Mus musculus, Rattus norvegicus
brenda
Ferry, G.; Giganti, A.; Coge, F.; Bertaux, F.; Thiam, K.; Boutin, J.A.
Functional invalidation of the autotaxin gene by a single amino acid mutation in mouse is lethal
FEBS Lett.
581
3572-3578
2007
Mus musculus
brenda
Tanaka, M.; Okudaira, S.; Kishi, Y.; Ohkawa, R.; Iseki, S.; Ota, M.; Noji, S.; Yatomi, Y.; Aoki, J.; Arai, H.
Autotaxin stabilizes blood vessels and is required for embryonic vasculature by producing lysophosphatidic acid
J. Biol. Chem.
281
25822-25830
2006
Mus musculus
brenda
Giganti, A.; Rodriguez, M.; Fould, B.; Moulharat, N.; Coge, F.; Chomarat, P.; Galizzi, J.P.; Valet, P.; Saulnier-Blache, J.S.; Boutin, J.A.; Ferry, G.
Murine and human autotaxin alpha, beta, gamma isoforms: Gene organization, tissue distribution and biochemical characterization
J. Biol. Chem.
283
7776-7789
2008
Homo sapiens, Homo sapiens (Q13822), Mus musculus, Mus musculus (Q9R1E6)
brenda
van Meeteren, L.A.; Ruurs, P.; Stortelers, C.; Bouwman, P.; van Rooijen, M.A.; Pradere, J.P.; Pettit, T.R.; Wakelam, M.J.; Saulnier-Blache, J.S.; Mummery, C.L.; Moolenaar, W.H.; Jonkers, J.
Autotaxin, a secreted lysophospholipase D, is essential for blood vessel formation during development
Mol. Cell. Biol.
26
5015-5022
2006
Mus musculus
brenda
Nakasaki, T.; Tanaka, T.; Okudaira, S.; Hirosawa, M.; Umemoto, E.; Otani, K.; Jin, S.; Bai, Z.; Hayasaka, H.; Fukui, Y.; Aozasa, K.; Fujita, N.; Tsuruo, T.; Ozono, K.; Aoki, J.; Miyasaka, M.
Involvement of the lysophosphatidic acid-generating enzyme autotaxin in lymphocyte-endothelial cell interactions
Am. J. Pathol.
173
1566-1576
2008
Mus musculus
brenda
Federico, L.; Pamuklar, Z.; Smyth, S.S.; Morris, A.J.
Therapeutic potential of autotaxin/lysophospholipase d inhibitors
Curr. Drug Targets
9
698-708
2008
Mus musculus
brenda
Kanda, H.; Newton, R.; Klein, R.; Morita, Y.; Gunn, M.D.; Rosen, S.D.
Autotaxin, an ectoenzyme that produces lysophosphatidic acid, promotes the entry of lymphocytes into secondary lymphoid organs
Nat. Immunol.
9
415-423
2008
Mus musculus
brenda
Fotopoulou, S.; Oikonomou, N.; Grigorieva, E.; Nikitopoulou, I.; Paparountas, T.; Thanassopoulou, A.; Zhao, Z.; Xu, Y.; Kontoyiannis, D.L.; Remboutsika, E.; Aidinis, V.
ATX expression and LPA signalling are vital for the development of the nervous system
Dev. Biol.
339
451-464
2010
Mus musculus
brenda
Endo, T.; Kano, K.; Motoki, R.; Hama, K.; Okudaira, S.; Ishida, M.; Ogiso, H.; Tanaka, M.; Matsuki, N.; Taguchi, R.; Kanai, M.; Shibasaki, M.; Arai, H.; Aoki, J.
Lysophosphatidylmethanol is a pan lysophosphatidic acid receptor agonist and is produced by autotaxin in blood
J. Biochem.
146
283-293
2009
Mus musculus
brenda
Koike, S.; Keino-Masu, K.; Ohto, T.; Sugiyama, F.; Takahashi, S.; Masu, M.
Autotaxin/lysophospholipase D-mediated lysophosphatidic acid signaling is required to form distinctive large lysosomes in the visceral endoderm cells of the mouse yolk sac
J. Biol. Chem.
284
33561-33570
2009
Mus musculus
brenda
Ma, L.; Uchida, H.; Nagai, J.; Inoue, M.; Aoki, J.; Ueda, H.
Evidence for de novo synthesis of lysophosphatidic acid in the spinal cord through phospholipase A2 and autotaxin in nerve injury-induced neuropathic pain
J. Pharmacol. Exp. Ther.
333
540-546
2010
Mus musculus
brenda
Im, E.; Motiejunaite, R.; Aranda, J.; Park, E.Y.; Federico, L.; Kim, T.I.; Clair, T.; Stracke, M.L.; Smyth, S.; Kazlauskas, A.
PLCgamma activation drives increased production of autotaxin in endothelial cells and LPA-dependent regression
Mol. Cell. Biol.
30
2401-2410
2010
Mus musculus
brenda
David, M.; Wannecq, E.; Descotes, F.; Jansen, S.; Deux, B.; Ribeiro, J.; Serre, C.M.; Gres, S.; Bendriss-Vermare, N.; Bollen, M.; Saez, S.; Aoki, J.; Saulnier-Blache, J.S.; Clezardin, P.; Peyruchaud, O.
Cancer cell expression of autotaxin controls bone metastasis formation in mouse through lysophosphatidic acid-dependent activation of osteoclasts
PLoS ONE
5
e9741
2010
Homo sapiens, Mus musculus
brenda
Albers, H.M.; Dong, A.; van Meeteren, L.A.; Egan, D.A.; Sunkara, M.; van Tilburg, E.W.; Schuurman, K.; van Tellingen, O.; Morris, A.J.; Smyth, S.S.; Moolenaar, W.H.; Ovaa, H.
Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation
Proc. Natl. Acad. Sci. USA
107
7257-7262
2010
Mus musculus
brenda
Tsuboi, K.; Okamoto, Y.; Ikematsu, N.; Inoue, M.; Shimizu, Y.; Uyama, T.; Wang, J.; Deutsch, D.G.; Burns, M.P.; Ulloa, N.M.; Tokumura, A.; Ueda, N.
Enzymatic formation of N-acylethanolamines from N-acylethanolamine plasmalogen through N-acylphosphatidylethanolamine-hydrolyzing phospholipase D-dependent and -independent pathways
Biochim. Biophys. Acta
1811
565-577
2011
Mus musculus
brenda
Nishimasu, H.; Okudaira, S.; Hama, K.; Mihara, E.; Dohmae, N.; Inoue, A.; Ishitani, R.; Takagi, J.; Aoki, J.; Nureki, O.
Crystal structure of autotaxin and insight into GPCR activation by lipid mediators
Nat. Struct. Mol. Biol.
18
205-212
2011
Mus musculus
brenda
Kawaguchi, M.; Okabe, T.; Okudaira, S.; Nishimasu, H.; Ishitani, R.; Kojima, H.; Nureki, O.; Aoki, J.; Nagano, T.
Screening and X-ray crystal structure-based optimization of autotaxin (ENPP2) inhibitors, using a newly developed fluorescence probe
ACS Chem. Biol.
8
1713-1721
2013
Danio rerio, Mus musculus (Q9R1E6)
brenda
Rancoule, C.; Dusaulcy, R.; Treguer, K.; Gres, S.; Attane, C.; Saulnier-Blache, J.S.
Involvement of autotaxin/lysophosphatidic acid signaling in obesity and impaired glucose homeostasis
Biochimie
96
140-143
2014
Homo sapiens, Mus musculus
brenda
Perrakis, A.; Moolenaar, W.H.
Autotaxin: structure-function and signaling
J. Lipid Res.
55
1010-1018
2014
Homo sapiens, Mus musculus, Streptomyces chromofuscus, Loxosceles sp.
brenda
Hozumi, H.; Hokari, R.; Kurihara, C.; Narimatsu, K.; Sato, H.; Sato, S.; Ueda, T.; Higashiyama, M.; Okada, Y.; Watanabe, C.; Komoto, S.; Tomita, K.; Kawaguchi, A.; Nagao, S.; Miura, S.
Involvement of autotaxin/lysophospholipase D expression in intestinal vessels in aggravation of intestinal damage through lymphocyte migration
Lab. Invest.
93
508-519
2013
Homo sapiens, Mus musculus, Mus musculus BALB/c
brenda
Tsuboi, K.; Okamoto, Y.; Rahman, I.A.; Uyama, T.; Inoue, T.; Tokumura, A.; Ueda, N.
Glycerophosphodiesterase GDE4 as a novel lysophospholipase D a possible involvement in bioactive N-acylethanolamine biosynthesis
Biochim. Biophys. Acta
1851
537-548
2015
Mus musculus (Q9CRY7), Mus musculus
brenda
Rahman, I.A.; Tsuboi, K.; Hussain, Z.; Yamashita, R.; Okamoto, Y.; Uyama, T.; Yamazaki, N.; Tanaka, T.; Tokumura, A.; Ueda, N.
Calcium-dependent generation of N-acylethanolamines and lysophosphatidic acids by glycerophosphodiesterase GDE7
Biochim. Biophys. Acta
1861
1881-1892
2016
Homo sapiens (Q7L5L3), Homo sapiens, Mus musculus (Q99LY2), Mus musculus
brenda
Ohshima, N.; Kudo, T.; Yamashita, Y.; Mariggio, S.; Araki, M.; Honda, A.; Nagano, T.; Isaji, C.; Kato, N.; Corda, D.; Izumi, T.; Yanaka, N.
New members of the mammalian glycerophosphodiester phosphodiesterase family GDE4 and GDE7 produce lysophosphatidic acid by lysophospholipase D activity
J. Biol. Chem.
290
4260-4271
2015
Mus musculus (Q9CRY7)
brenda