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1-alkyl-sn-glycero-3-phospho-L-serine + H2O
1-alkyl-sn-glycerol 3-phosphate + L-serine
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Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycero-3-phosphate + choline
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Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycero-3-phosphate + ethanolamine
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Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
1-heptadecanoyl-sn-glycero-3-phosphocholine + H2O
1-heptadecanoyl-sn-glycerol 3-phosphate + choline
1-linoleoyl-2-lyso-glycerophoshorylcholine + H2O
1-linoleoyl-sn-glycerol-3-phosphate + choline
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Substrates: -
Products: -
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1-linoleoyl-sn-glycero-3-phosphocholine + H2O
1-linoleoyl-sn-glycerol 3-phosphate + choline
1-myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
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Substrates: -
Products: -
?
1-O-alkyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-2-lyso-sn-glycero-3-phosphate + choline
1-O-alkyl-2-lyso-sn-glycero-3-phosphoethanolamine + H2O
1-O-alkyl-2-lyso-sn-glycero-3-phosphate + ethanolamine
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Substrates: the microsomal enzyme
Products: the microsomal enzyme
?
1-O-alkyl-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-sn-glycerol 3-phosphate + choline
Substrates: i.e. lyso-platelet-activating factor
Products: -
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1-O-hexadecyl-2-lyso-glycerophosphorylcholine + H2O
1-O-hexadecyl-sn-glycerol-3-phosphate + choline
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Substrates: lysoPAF (alkyl-lysophosphatidylcholine), lysoPLD shows higher activity towards lysoPAF
Products: -
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1-O-hexadecyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-hexadecyl-2-lyso-sn-glycero-3-phosphate + choline
1-O-hexadecyl-2-lyso-sn-glycero-3-phosphoethanolamine + H2O
1-O-hexadecyl-2-lyso-sn-glycero-3-phosphate + ethanolamine
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Substrates: -
Products: -
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1-O-octadecyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-octadecyl-2-lyso-sn-glycero-3-phosphate + choline
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Substrates: -
Products: -
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1-palmitoyl-2-lyso-glycerophoshorylcholine + H2O
1-palmitoyl-sn-glycerol-3-phosphate + choline
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Substrates: -
Products: -
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1-palmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycerol 3-phosphate + choline
1-stearoyl-2-lyso-glycerophoshorylcholine + H2O
1-stearoyl-sn-glycerol-3-phosphate + choline
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Substrates: -
Products: -
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4-nitrophenyl thymidine 5'-phosphate + H2O
4-nitrophenol + thymidine 5'-phosphate
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Substrates: -
Products: -
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4-nitrophenyl-TMP + H2O
4-nitrophenol + TMP
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Substrates: -
Products: -
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4-nitrophenyl-TMP + H2O
?
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Substrates: -
Products: -
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5-[[(23R)-33-(4-[[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,33-dioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid + H2O
?
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Substrates: fluorogenic substrate analogue for lysophosphatidylcholine
Products: -
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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
?
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Substrates: -
Products: -
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bis(para-nitrophenyl)phosphate + H2O
?
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Substrates: -
Products: -
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caproyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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capryl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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caprylyl-lysophosphatidylcholine + H2O
1-octanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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coumarin-phosphate-fluorescein + H2O
?
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Substrates: -
Products: -
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decanoyl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
FS-2 + H2O
?
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Substrates: fluorogenic substrate analogue for lysophosphatidylcholine
Products: -
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FS-3 + H2O
2-(6-hydroxy-3-oxo-9a,10a-dihydro-3H-xanthen-9-yl)-5-[(18-hydroxy-15-oxo-3,6,9,12-tetraoxa-16-azaoctadec-1-yl)carbamoyl]benzoic acid + (2R)-2-hydroxy-3-(phosphonooxy)propyl 6-[(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]benzoyl)amino]hexanoate
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Substrates: fluorogenic lysoPLD substrate
Products: -
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hexanoyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
lauroyl-lysophosphatidylcholine + H2O
1-lauroyl-sn-gycerol-3-phosphate + choline
lyso-phosphatidylcholine + H2O
lyso-phosphatidic acid + choline
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Substrates: -
Products: central in some key metabolic deregulations
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lysoDDPB + H2O
?
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Substrates: synthesized by an enzyme-assisted strategy. Lysophosphatidylcholine analogue that contains a fluorescence quencher at each acyl chain terminus and a fluorophore appended to the phospholipid headgroup through a choline-mimetic linker
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
lysophosphatidyl ethanolamine + H2O
lysophosphatidic acid + ethanolamine
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatic acid + choline
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Substrates: LPC, purified enzyme hydrolyzes saturated forms of lysophosphatidylcholine more robustly than unsaturated forms
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
lysophosphatidylcholine 16:0 + H2O
?
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Substrates: -
Products: -
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lysophosphatidylcholine 18:0 + H2O
?
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Substrates: -
Products: -
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lysophosphatidylcholine 18:1 + H2O
?
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Substrates: -
Products: -
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myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
N-arachidonoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-arachidonoyl-ethanolamine
Substrates: -
Products: -
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N-arachidonoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-arachidonoylethanolamine
Substrates: -
Products: -
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N-oleoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-oleoyl-ethanolamine
Substrates: -
Products: -
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N-oleoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-oleoylethanolamine
Substrates: -
Products: -
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N-palmitoyl-lysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoyl-ethanolamine
Substrates: -
Products: -
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N-palmitoyl-lysoplasmenylethanolamine + H2O
lysoplasmenic acid + N-palmitoyl-ethanolamine
Substrates: -
Products: -
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N-palmitoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoylethanolamine
N-palmitoyllysoplasmenylethanolamine + H2O
lysoplasmenic acid + N-palmitoylethanolamine
Substrates: -
Products: -
?
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
Substrates: -
Products: -
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p-nitrophenyl thymidine 5'-monophosphate + H2O
?
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Substrates: -
Products: -
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palmitoyl-lysophosphatidylcholine + H2O
1-palmitoyl-sn-gycerol-3-phosphate + choline
platelet-activating factor + H2O
? + choline
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Substrates: PAF, same extent as palmityl-lysophosphatidylcholine
Products: -
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sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
sphingosylphosphorylcholine + H2O
sphingosine-1-phosphate + choline
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Substrates: -
Products: -
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stearoyl-lysophosphatidylcholine + H2O
1-stearoyl-sn-gycerol-3-phosphate + choline
[(11R)-1-(4-[(Z)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-N-[3-[(5-[5-[(3,5-dimethyl-2H-pyrrol-2-ylidene-kappaN)methyl]-1H-pyrrol-2-yl-kappaN]pentanoyl)amino]propyl]-11,14-dihydroxy-N,N-dimethyl-1,8-dioxo-9,13,15-trioxa-2-aza-14-phosphaheptadecan-17-aminiumato 14-oxide](difluoro)boron(1+) + H2O
?
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Substrates: synthesized by an enzyme-assisted strategy. lysophosphatidylcholine analogue that contains a fluorescence quencher at each acyl chain terminus and a fluorophore append to the phospholipid headgroup through a choline-mimetic linker
Products: -
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[(2R)-26-(4-[(Z)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-2,5-dihydroxy-5-oxido-10,26-dioxo-4,6,13,16,19,22-hexaoxa-9,25-diaza-5-phosphahexacos-1-yl 6-[(5-[5-[(3,5-dimethyl-2H-pyrrol-2-ylidene-kN)methyl]-1H-pyrrol-2-yl-kappaN]pentanoyl)amino]hexanoatato](difluoro)boron + H2O
?
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Substrates: fluorogenic substrate analogue for lysophosphatidylcholine
Products: -
?
[5-[[(23S)-33-(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,26,33-trioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)phenyl]acetic acid + H2O
?
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Substrates: second-generation fluorogenic autotaxin/lysoPLD substrate. The molecule consists of an ethanoamido head group linked to a dabcyl quencher via the amino group. The hydroxyl group of the head group is conjugated to fluorescein via a phosphodiester bond and a polyethylene glycol linker. [5-[[(23S)-33-(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,26,33-trioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)phenyl]acetic acid is therefore a more lipid-like substrate than coumarin-phosphate-fluorescein
Products: -
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additional information
?
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
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Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: 16:0, 18:1 and 18:2-lysophosphatidylcholine are the predominant physiological substrates of the enzyme in rabbit aqueous humor
Products: -
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1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
r
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
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1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
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1-heptadecanoyl-sn-glycero-3-phosphocholine + H2O
1-heptadecanoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
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1-heptadecanoyl-sn-glycero-3-phosphocholine + H2O
1-heptadecanoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-linoleoyl-sn-glycero-3-phosphocholine + H2O
1-linoleoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-linoleoyl-sn-glycero-3-phosphocholine + H2O
1-linoleoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-O-alkyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-2-lyso-sn-glycero-3-phosphate + choline
-
Substrates: -
Products: -
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1-O-alkyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-2-lyso-sn-glycero-3-phosphate + choline
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Substrates: may play a role in the metabolism of platelet-activating factor
Products: -
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1-O-hexadecyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-hexadecyl-2-lyso-sn-glycero-3-phosphate + choline
-
Substrates: -
Products: -
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1-O-hexadecyl-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-hexadecyl-2-lyso-sn-glycero-3-phosphate + choline
-
Substrates: -
Products: -
?
1-palmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-palmitoyl-sn-glycero-3-phosphocholine + H2O
1-palmitoyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
arachidoyl-lysophosphatidylcholine + H2O
1-arachidoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
arachidoyl-lysophosphatidylcholine + H2O
1-arachidoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
behenoyl-lysophosphatidylcholine + H2O
1-behenoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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behenoyl-lysophosphatidylcholine + H2O
1-behenoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
CPF4 + H2O
?
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Substrates: fluorescence resonance energy transfer substrate derived from bis-p-nitrophenyl phosphate
Products: -
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CPF4 + H2O
?
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Substrates: i.e. 5-([4-[(4-[[(6-chloro-7-hydroxy-2-oxo-2H-chromen-4-yl)acetyl]amino]phenoxy)(hydroxy)phosphoryl]phenyl]carbamoyl)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid, fluorescence resonance energy transfer substrate derived from bis-p-nitrophenyl phosphate
Products: -
?
CPF4 + H2O
?
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Substrates: bis-pNPP-derived probe, in which both phenyl moieties are linked to coumarin and fluorescein, respectively
Products: -
?
decanoyl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
decanoyl-lysophosphatidylcholine + H2O
1-decanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
FS-3 + H2O
?
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Substrates: fluorogenic substrate analogue for lysophosphatidylcholine
Products: -
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FS-3 + H2O
?
-
Substrates: -
Products: -
?
hexanoyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
hexanoyl-lysophosphatidylcholine + H2O
1-hexanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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lauroyl-lysophosphatidylcholine + H2O
1-lauroyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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lauroyl-lysophosphatidylcholine + H2O
1-lauroyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: various concentration of lysophosphatidyl choline with or without 2.5 pM of hATX S48 are exposed to HT-1080 cells and motile area is analyzed
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: best substrate, reaction of EC 3.1.4.5
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
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lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: best substrate, reaction of EC 3.1.4.5
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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6, 663457, 664939, 665229, 666223, 666527, 670114, 681769, 696397, 697080, 698987, 700238, 701580, 701638, 702025, 702693, 703104, 705057, 706456, 706577 Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: bioactive phospholipid regulating a wide range of cellular responses
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: albumin-bound lipid
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: present in the plasma
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: radiolabeled substrate
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: lysophospholipase D activity
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: radiolabeled substrate and fluorogenic substrate FS-3
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: -
Products: Hydrolysis of lysophospholipids by the secreted plasma protein autotaxin/lysophospholipase D (lysoPLD) is a major mechanism for generation of lysophosphatidic acid in the blood
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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665507, 678439, 679137, 681910, 695455, 700364, 703366, 704356, 704588, 705323, 705706, 706456, 706564 Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: -
Products: lysophosphatidic acid is a bioactive lysophospholipid present in circulating blood
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: lysophosphatidic acid is a bioactive phospholipid regulating a wide range of cellular responses
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
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Substrates: -
Products: LPA, lysophosphatidic acid is a bioactive lysophospholipid present in circulating blood
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
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lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
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myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
myristoyl-lysophosphatidylcholine + H2O
1-myristoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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N-palmitoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoylethanolamine
Substrates: -
Products: -
?
N-palmitoyllysophosphatidylethanolamine + H2O
lysophosphatidic acid + N-palmitoylethanolamine
Substrates: -
Products: -
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octanoyl-lysophosphatidylcholine + H2O
1-octanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
octanoyl-lysophosphatidylcholine + H2O
1-octanoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
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oleoyl-lysophosphatidylcholine + H2O
1-oleoyl-sn-gycerol 3-phosphate + choline
Substrates: -
Products: -
?
oleoyl-lysophosphatidylcholine + H2O
1-oleoyl-sn-gycerol 3-phosphate + choline
Substrates: -
Products: -
?
palmitoyl-lysophosphatidylcholine + H2O
1-palmitoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
palmitoyl-lysophosphatidylcholine + H2O
1-palmitoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
-
Substrates: -
Products: -
?
sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
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Substrates: Whereas lysoPC is present in the blood at concentrations well in excess of the measured Km of autotaxin/lysoPLD for this substrate, levels of SPC are considerably lower, suggesting that this may not be a relevant substrate in vivo
Products: bioactive lipid with a spectrum of signaling activities broadly similar to those of lysophosphatidic acid
?
sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
-
Substrates: -
Products: bioactive lysophospholipid, in vitro
?
stearoyl-lysophosphatidylcholine + H2O
1-stearoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
stearoyl-lysophosphatidylcholine + H2O
1-stearoyl-sn-gycerol-3-phosphate + choline
Substrates: -
Products: -
?
additional information
?
-
-
Substrates: zATX preferably hydrolyzes LPC and lysophosphatidylethanolamine but does not efficiently hydrolyze lysophosphatidylserine, lysophosphatidylinositol or sphingosylphosphorylcholine
Products: -
?
additional information
?
-
-
Substrates: the enzyme converts lysophospholipids such as lysophosphatidylcholine to lysophosphatidic acid
Products: -
?
additional information
?
-
-
Substrates: zATX preferably hydrolyzes LPC and lysophosphatidylethanolamine but does not efficiently hydrolyze lysophosphatidylserine, lysophosphatidylinositol or sphingosylphosphorylcholine
Products: -
?
additional information
?
-
-
Substrates: the enzyme is active on human macrophages, erythrocytes, Jurkat and HeLa cells, and on chicken embryo chorioallantoic membrane
Products: -
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additional information
?
-
-
Substrates: the enzyme shows slight activity with sphingomyelin, but no activity with phosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: the plasma enzyme hydrolyzes acyl-, alkyl- and alkenyl-lysophophatidylcholines
Products: -
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additional information
?
-
Substrates: Catalytic ability of ATX for p-nitrophenyl thymidine 5'-monophosphate and adenosine triphosphate hydrolysis are low compared with nucleotide pyrophosphatases-1/phosphodiesterases
Products: -
?
additional information
?
-
-
Substrates: Catalytic ability of ATX for p-nitrophenyl thymidine 5'-monophosphate and adenosine triphosphate hydrolysis are low compared with nucleotide pyrophosphatases-1/phosphodiesterases
Products: -
?
additional information
?
-
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
Products: -
?
additional information
?
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: activity implicated in a large variety of biological processes (during normal development and under pathological conditions). Developmental roles include adipogenesis, intestinal cell motility and neurite morphology, a contribution to disease is described for alzheimer's disease, chronic hepatitis C, multiple sclerosis, neuropathic pain, obesity, rheumatoid arthritis
Products: -
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additional information
?
-
-
Substrates: assay development devised to quantify 4-nitrophenol from hydrolysis of chromogenic substrate by serum lysoPLD without tedious lipid extraction procedures
Products: -
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additional information
?
-
-
Substrates: lysophospholipase D generates lysophosphatidic acid from lysophosphatidylcholine
Products: -
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additional information
?
-
-
Substrates: reaction mechanism of NBD-LPC hydrolysis, overview. Artificial substrates FS-3 and pNP-TMP are used for kinetic studies, overview
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
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additional information
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-
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Substrates: the recombinant enzyme promotes MDA-MB-231 breast cancer cell and mouse aortic vascular smooth muscle cell migration in lysophosphatidic acid-dependent and -independent ways. The enzyme also shows nucleotide phosphodiesterase activity with nucleotide derivative 4-nitrophenyl-TMP as a substrate
Products: -
?
additional information
?
-
Substrates: poor substrate: glycerophospho-N-palmitoylethanolamine
Products: -
?
additional information
?
-
-
Substrates: poor substrate: glycerophospho-N-palmitoylethanolamine
Products: -
?
additional information
?
-
Loxosceles sp.
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
additional information
?
-
-
Substrates: no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
Substrates: no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl lysophosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
Products: -
?
additional information
?
-
Substrates: There are no major differences in the respective specificities of the various isoforms, main substrate is lauroyl-lysophosphatidylcholine
Products: -
?
additional information
?
-
-
Substrates: 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
Products: -
?
additional information
?
-
-
Substrates: brain homogenate forms N-palmitoylethanolamine, N-oleoylethanolamine, and anandamide from their corresponding lyso-N-acylphosphatidylethanolamines by a Mg2+-dependent lysophospholipase D, substrate specificity, overview
Products: -
?
additional information
?
-
Substrates: the enzyme converts lysophospholipids such as lysophosphatidylcholine to lysophosphatidic acid
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
additional information
?
-
Substrates: poor substrate: glycerophospho-N-palmitoylethanolamine
Products: -
?
additional information
?
-
-
Substrates: poor substrate: glycerophospho-N-palmitoylethanolamine
Products: -
?
additional information
?
-
-
Substrates: brain homogenate forms N-palmitoylethanolamine, N-oleoylethanolamine, and anandamide from their corresponding lyso-N-acylphosphatidylethanolamines by a Mg2+-dependent lysophospholipase D, substrate specificity, overview
Products: -
?
additional information
?
-
-
Substrates: the enzyme is active on 16:0, 18:1 and 18:2-lysophosphatidylcholine, it also hydrolyzes three lysophosphatidylcholine subclasses in the following order: 16:0-acyl-lysophosphatidylcholine > 16:0-alkyl-lysophosphatidylcholine > 16:0-rich alkenyl-lysophosphatidylcholine, substrate specificity, overview
Products: -
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additional information
?
-
-
Substrates: no hydrolysis of 1-acyl-2-lyso-sn-glycero-3-phosphoethanolamine or 1-acyl-2-lyso-sn-glycero-3-phosphocholine
Products: -
?
additional information
?
-
-
Substrates: the microsomal enzymes prefer alkyl-lysophospholipids, the extracellular enzyme prefer acyl-phospholipids, but can use alkyl-lysophospholipids
Products: -
?
additional information
?
-
-
Substrates: the product lysophosphatidic acid mediates multiple biological functions
Products: -
?
additional information
?
-
Substrates: binding of ATX to activated platelets and lymphocytes in an integrin-dependent manner mediated by the consecutive cysteine-rich somatomedin-B-like, SMB, domains
Products: -
?
additional information
?
-
-
Substrates: heterotrimeric G protein subunits Galphaq and Gbeta1 have lysophospholipase D activity, choline production from lysoPAF by the purified FLAG-tagged Galphaq, overview. K52A, T186A, D205A, G48A and Q209L mutant forms of Galphaq show a significant reduction of lysoPLD activity, whereas G48V does not. The decrease of lysoPLD activity of G48A and Q209L is low
Products: -
?
additional information
?
-
-
Substrates: protein-protein interaction with proteins via the enzyme's SMB1 domain, which binds to the PDE domain. The enzyme binds to activated lymphocytes possibly involving an enzyme lymphocyte- and alpha4beta1-specific 458LDV460 motif. Autotaxin (ATX or ENPP2) is an ectonucleotide pyrophosphatase/phosphodiesterase that functions as a secreted lysophospholipase D to produce the multifunctional lipid mediator lysophosphatidic acid from more complex lysophospholipids
Products: -
?
additional information
?
-
-
Substrates: the enzyme can produce bioactive lysophosphatidic acid from diverse lysophospholipid substrates, particularly lysophosphatidylcholine, the most abundant lysophospholipid in the circulation, but also from lysophosphatidylserine and lysophosphatidylethanolamine. It does not discriminate between phospholipid headgroups
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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-2-lyso-sn-glycero-3-phosphocholine + H2O
1-O-alkyl-2-lyso-sn-glycero-3-phosphate + choline
-
Substrates: may play a role in the metabolism of platelet-activating factor
Products: -
?
lysophosphatidyl choline + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
sphingosylphosphorylcholine + H2O
sphingosine 1-phosphate + choline
-
Substrates: -
Products: -
?
additional information
?
-
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphocholine + H2O
1-alkyl-sn-glycerol 3-phosphate + choline
-
Substrates: 16:0, 18:1 and 18:2-lysophosphatidylcholine are the predominant physiological substrates of the enzyme in rabbit aqueous humor
Products: -
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
?
1-alkyl-sn-glycero-3-phosphoethanolamine + H2O
1-alkyl-sn-glycerol 3-phosphate + ethanolamine
-
Substrates: -
Products: -
r
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: bioactive phospholipid regulating a wide range of cellular responses
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: present in the plasma
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: lysophospholipase D activity
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: lysophosphatidic acid is a bioactive lysophospholipid present in circulating blood
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: lysophosphatidic acid is a bioactive phospholipid regulating a wide range of cellular responses
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
-
Substrates: -
Products: -
?
lysophosphatidylcholine + H2O
lysophosphatidic acid + choline
Substrates: -
Products: -
?
additional information
?
-
-
Substrates: zATX preferably hydrolyzes LPC and lysophosphatidylethanolamine but does not efficiently hydrolyze lysophosphatidylserine, lysophosphatidylinositol or sphingosylphosphorylcholine
Products: -
?
additional information
?
-
-
Substrates: the enzyme converts lysophospholipids such as lysophosphatidylcholine to lysophosphatidic acid
Products: -
?
additional information
?
-
-
Substrates: zATX preferably hydrolyzes LPC and lysophosphatidylethanolamine but does not efficiently hydrolyze lysophosphatidylserine, lysophosphatidylinositol or sphingosylphosphorylcholine
Products: -
?
additional information
?
-
-
Substrates: the enzyme is active on human macrophages, erythrocytes, Jurkat and HeLa cells, and on chicken embryo chorioallantoic membrane
Products: -
?
additional information
?
-
-
Substrates: activity implicated in a large variety of biological processes (during normal development and under pathological conditions). Developmental roles include adipogenesis, intestinal cell motility and neurite morphology, a contribution to disease is described for alzheimer's disease, chronic hepatitis C, multiple sclerosis, neuropathic pain, obesity, rheumatoid arthritis
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
additional information
?
-
Loxosceles sp.
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
additional information
?
-
-
Substrates: brain homogenate forms N-palmitoylethanolamine, N-oleoylethanolamine, and anandamide from their corresponding lyso-N-acylphosphatidylethanolamines by a Mg2+-dependent lysophospholipase D, substrate specificity, overview
Products: -
?
additional information
?
-
Substrates: the enzyme converts lysophospholipids such as lysophosphatidylcholine to lysophosphatidic acid
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
additional information
?
-
-
Substrates: brain homogenate forms N-palmitoylethanolamine, N-oleoylethanolamine, and anandamide from their corresponding lyso-N-acylphosphatidylethanolamines by a Mg2+-dependent lysophospholipase D, substrate specificity, overview
Products: -
?
additional information
?
-
-
Substrates: the product lysophosphatidic acid mediates multiple biological functions
Products: -
?
additional information
?
-
Substrates: binding of ATX to activated platelets and lymphocytes in an integrin-dependent manner mediated by the consecutive cysteine-rich somatomedin-B-like, SMB, domains
Products: -
?
additional information
?
-
-
Substrates: heterotrimeric G protein subunits Galphaq and Gbeta1 have lysophospholipase D activity, choline production from lysoPAF by the purified FLAG-tagged Galphaq, overview. K52A, T186A, D205A, G48A and Q209L mutant forms of Galphaq show a significant reduction of lysoPLD activity, whereas G48V does not. The decrease of lysoPLD activity of G48A and Q209L is low
Products: -
?
additional information
?
-
-
Substrates: protein-protein interaction with proteins via the enzyme's SMB1 domain, which binds to the PDE domain. The enzyme binds to activated lymphocytes possibly involving an enzyme lymphocyte- and alpha4beta1-specific 458LDV460 motif. Autotaxin (ATX or ENPP2) is an ectonucleotide pyrophosphatase/phosphodiesterase that functions as a secreted lysophospholipase D to produce the multifunctional lipid mediator lysophosphatidic acid from more complex lysophospholipids
Products: -
?
additional information
?
-
-
Substrates: the enzyme hydrolyzes extracellular lysophospholipids into the lipid mediator lysophosphatidic acid, a ligand for specific G protein-coupled receptors
Products: -
?
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)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
-
-
(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
(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
(5Z)-5-(3-bromobenzylidene)-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
(5Z)-5-(4-chlorobenzylidene)-2-(4-ethylpiperazin-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
(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-2-(morpholin-4-yl)-1,3-thiazol-4(5H)-one
(5Z)-5-benzylidene-2-(4-ethylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
1,10-phenantroline
-
50% inhibition at 2.5 mM, 70% inhibition
1-acyl glycerol 3-phosphate
-
also fatty alcohol phosphates (structurally 1-acyl glycerol 3-phosphate analogs)
1-arachidonoyl-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-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
-
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-myristoyl-lysophosphatidic acid
1-oleoyl-lysophosphatidic acid
1-palmitoyl-lysophosphatidic acid
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
2,2'-methylenebis(4-chlorophenol)
-
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
56.4% residual activity at 0.001 mM using FS-3 as substrate
2-amino-2-(2-(4-octylphenyl) ethyl)propan-1,3-diol
-
synonyms FTY720, finolimod, competitive inhibition
2-carba cyclic phosphatidic acid
-
-
3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
-
-
3-carba cyclic phosphatidic 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
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
-
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)
-
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
-
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
ATP
-
extracellular enzyme
bis(para-nitrophenyl)phosphate
-
inhibition above a concentration of 1 mM
bovine serum albumin
-
concentration-dependent inhibition on lysoPLD activity in egg white during 24 h incubation
-
brefeldin-A
-
inhibitor of trans-Golgi transport, inhibits secretion of ATX
cyclohexanaminium hydrogen [4-(decanoylamino)benzyl]phosphonate
-
-
cyclohexanaminium hydrogen [4-(heptanoylamino)benzyl]phosphonate
-
-
cyclohexanaminium hydrogen [4-(tetradecanoylamino)benzyl]phosphonate
-
-
cyclohexanaminium hydrogen [4-([3-[2-(2-methoxyethoxy)ethoxy]propanoyl]amino)benzyl]phosphonate
-
-
cyclohexanaminium hydrogen [fluoro[4-(heptanoylamino)phenyl]methyl]phosphonate
-
-
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate
-
-
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate
-
-
cyclohexanaminium hydrogen [[4-(heptanoylamino)phenyl](hydroxy)methyl]phosphonate
-
-
D-histidine
-
15 mM, 75% inhibition
fatty alkyl phosphonate
-
-
fatty alkyl thiophosphate
-
-
FTY720P
-
binds apo-ATX and an ATX with bound FS-3/products complex, noncompetitive/mixed inhibition
G protein
-
G protein exhibits lysoPLD activity, lysoPLD activity is highly associated with heterotrimeric G protein
-
Globomycin
-
Treatment with the signal peptidase inhibitor inhibits ATX secretion by adipocytes treated for 6 h
H2L 5210574
-
mixed-mode inhibition against ATX-mediated FS-3 hydrolysis
H2L 5564949
-
mixed-mode inhibition against ATX-mediated FS-3 hydrolysis
H2L 5761473
-
competitive ATX inhibitor
H2L 7839888
-
mixed-mode inhibition against ATX-mediated FS-3 hydrolysis
H2L 7921385
-
non-competitive inhibitor
histidine methylester
-
15 mM, 65% inhibition
histidineamide
-
15 mM, 20% inhibition
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
-
isorhamnetin-3-O-glucoside
-
-
Ki16425
-
inhibits the migratory response of lysophosphatidic acid1-expressing cells to both lysophosphatidic acid and ATX
L-histidine amide
-
15 mM, 20% inhibition
L-histidine methylester
-
15 mM, 65% inhibition
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
lysozyme
-
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
-
N-(2-chlorophenyl)-2-([(2E)-2-[1-(pyridin-2-yl)ethylidene]hydrazinyl]carbonothioyl)hydrazinecarbothioamide
N-glycosidase
-
treatment with N-glycosidase inhibits lysophospholipase D activity of ATX. N-glycosylation of ATX strongly influences its secretion and its lysoPLD activity
-
N-methyl histidine
-
15 mM, 30% inhibition
N-methyl-L-histidine
-
15 mM, 30% inhibition
oleoyl-LPA
-
inhibition of ATX pNP-TMP hydrolysis activity
palmitoyl-lysophosphatidic acid
-
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
serine esterase inhibitors
-
inhibition of extracellular enzyme
-
sodium cholate
-
16 mM, 77% inhibition
sodium deoxycholate
-
6 mM, 100% inhibition
Triton X-100
-
0.3 mM, 64% inhibition
tunicamycin
-
inhibits secretion of ATX
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid
-
-
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
-
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
-
i.e. VPC8a202
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
-
[(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
-
-
[(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
-
-
[(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
-
[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-(tetradecanoylamino)benzyl]phosphonic acid
[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-(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
1,10-phenanthroline
-
extracellular enzyme
1,10-phenanthroline
-
0.5 mM
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-myristoyl-lysophosphatidic acid
-
-
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-oleoyl-lysophosphatidic acid
-
-
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
1-palmitoyl-lysophosphatidic acid
-
-
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-[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
-
-
5-[4-[(5Z)-5-(3,4-dichlorobenzylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperazin-1-yl]pentanoic acid
-
bithionol
-
-
bithionol
-
inhibitory in vitro and in vivo
bithionol
-
inhibitory in vitro and in vivo
Cu2+
-
-
Cu2+
-
the inhibition of extracellular enzyme can be prevented by 2,6-di-tert-butyl-4-hydroxy-methylphenol
EDTA
-
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
-
extracellular enzyme
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
-
inhibition of extracellular enzyme
EDTA
-
hydrolysis of 1-palmitoyl-glycerophoshorylcholine is inhibited, indicating that a divalent cation is essential for catalytic activity
EGTA
-
48% inhibition
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
-
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
-
potent ATX inhibitor, complete inhibition of FS-3 hydrolysis at 0.01 mM, competitive inhibitor
HA155
-
-
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
hypericin
inhibitor of autotaxin beta; new inhibitor of autotaxin beta; new inhibitor of autotaxin beta
L-histidine
-
15-20 mM, noncompetitive, 75% inhibition, inhibition can be reversed by 20fold lower concentrations of zinc or cobalt salts
lysophosphatic acid
-
inhibits at biologically relevant concentrations
lysophosphatidic acid
reported as an inhibitor of its own production; reported as an inhibitor of its own production
lysophosphatidic acid
-
efficacious inhibitor of ATX activity
lysophosphatidic acid
-
-
lysophosphatidic acid
-
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
-
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
-
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
-
-
p-hydroxymercuribenzoate
-
the inhibition of the microsomal enzyme can be prevented by glutathione and dithiothreitol
PF8380
-
-
PF8380
-
the inhibitor shows adequate oral bioavailability and potency in reducing lysophosphatidic acid levels in plasma and at sites of infl ammation
sphingosine 1-phosphate
-
inhibits at biologically relevant concentrations
sphingosine 1-phosphate
-
-
sphingosine-1-phosphate
-
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
sphingosine-1-phosphate
-
0.001 mM, complexed to albumin
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
-
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
-
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-(tetradecanoylamino)benzyl]phosphonic acid
-
S32826
[4-(tetradecanoylamino)benzyl]phosphonic acid
-
-
[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
[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
-
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
-
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. 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
-
additional information
-
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
-
additional information
-
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
-
additional information
-
inhibitor development and synthesis, anti and syn forms of the molecules show different effects on the inhibitory potency, homology model docking study, overview
-
additional information
-
no inhibition by 4 at 0.01 mM
-
additional information
-
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
-
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
-
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
-
not affected by dioleoylphosphatidic acid, 1-oleoyl-glycerol, sphingosine, glycerol 3-phosphate
-
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0.097
1-alkyl-sn-glycero-3-phosphocholine
-
pH 7.4, 37°C
0.1
1-alkyl-sn-glycero-3-phosphoethanolamine
-
achieved under optimal assay conditions, almost same results in blood plasma
0.0083
1-linoleoyl-2-lyso-glycerophoshorylcholine
-
Vmax is 0.019 micromol/min/mg
0.32
1-O-alkyl-sn-glycero-3-phosphocholine
pH 7.4, temperature not specified in the publication
0.0267
1-O-hexadecyl-2-lyso-glycerophosphorylcholine
-
Vmax is 0.29 micromol/min/mg, lysoPLD activity is more than twice that observed with 1-palmitoyl-glycerophoshorylcholine
0.0207
1-palmitoyl-2-lyso-glycerophoshorylcholine
-
Vmax is 0.059 micromol/min/mg
0.176
1-palmitoyl-glycerophoshorylcholine
-
Vmax is 0.3 micromol/min/mg, best substrate
0.101
1-stearoyl-2-lyso-glycerophoshorylcholine
-
Vmax is 0.035 micromol/min/mg
0.7 - 5.6
4-nitrophenyl-TMP
0.0063
5-[[(23R)-33-(4-[[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,33-dioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid
-
-
0.004
coumarin-phosphate-fluorescein
-
coumarin-phosphate-fluorescein is a fluorescence resonance energy transfer (FRET)-based sensor of phosphodiesterase activity. Very useful substrate for enzymatic analysis of purified autotaxin/lysoPLD and can also be used to detect autotaxin/lysoPLD activity in serum-free conditioned culture medium isolated from cells expressing the enzyme
0.094 - 1
lysophosphatidylcholine
0.066 - 0.126
lysophosphatidylcholine 16:0
0.089 - 0.27
lysophosphatidylcholine 18:0
0.069 - 0.126
lysophosphatidylcholine 18:1
0.004
[5-[[(23S)-33-(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,26,33-trioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)phenyl]acetic acid
-
[5-[[(23S)-33-(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,26,33-trioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)phenyl]acetic acid can be used to detect autotaxin/lysoPLD activity in human and mouse blood
additional information
additional information
-
0.7
4-nitrophenyl-TMP
-
wild type enzyme, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
4.8
4-nitrophenyl-TMP
-
mutant enzyme H226Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
5.6
4-nitrophenyl-TMP
-
-
0.0026
FS-3
-
wild type enzyme, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.019
FS-3
-
mutant enzyme H226Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.094
lysophosphatidylcholine
-
-
0.1
lysophosphatidylcholine
-
kinetic analysis of recombinant autotaxin/lysoPLD using [14C] lysophosphatidylcholine substrate
0.15
lysophosphatidylcholine
-
-
0.47
lysophosphatidylcholine
-
in presence of 0.25 mM Zn2+ plus 10 mM L-histidine
0.49
lysophosphatidylcholine
-
-
0.55
lysophosphatidylcholine
-
in presence of 0.25 mM Zn2+
0.66
lysophosphatidylcholine
-
in presence of 10 mM L-histidine
1
lysophosphatidylcholine
pH 7.4, temperature not specified in the publication
0.066
lysophosphatidylcholine 16:0
-
wild type enzyme, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.094
lysophosphatidylcholine 16:0
-
mutant enzyme H420Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.12
lysophosphatidylcholine 16:0
-
mutant enzyme H434Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.126
lysophosphatidylcholine 16:0
-
mutant enzyme H226Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.089
lysophosphatidylcholine 18:0
-
wild type enzyme, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.115
lysophosphatidylcholine 18:0
-
mutant enzyme H420Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.27
lysophosphatidylcholine 18:0
-
mutant enzyme H226Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.069
lysophosphatidylcholine 18:1
-
mutant enzyme H420Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.073
lysophosphatidylcholine 18:1
-
wild type enzyme, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.105
lysophosphatidylcholine 18:1
-
mutant enzyme H434Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
0.126
lysophosphatidylcholine 18:1
-
mutant enzyme H226Q, in 50 mM Tris pH 7.4, 5 mM CaCl2, 1 mg/ml bovine serum albumin, at 37°C
additional information
additional information
-
suggestion that lysoPLD predominantly utilizes saturated forms of lysophosphatidylcholine
-
additional information
additional information
-
affinity for lysophosphatidylcholine is significantly higher than for nucleotides
-
additional information
additional information
-
capable of hydrolyzing sphingosylphosphorylcholine with a significantly higher km-value, also able to hydrolyze nucleotide triphosphates di-adenosine polyphosphates and artificial phosphodiester substrates such as p-nitrophenyl thymidine phosphate with Km-values close to 1 and optimal activity observed at alkaline pH
-
additional information
additional information
-
steady-state, single-turnover, and transient kinetics, kinetic analysis and modeling, using artificial fluorescent substrate FS-3, overview
-
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0.0001
1-acyl glycerol 3-phosphate
-
CPF4 FRET assay (change of fluorescence intensity), inihibition involves both a reduction in vmax and an increase in km, binding affinity is 1000fold stronger than to 1-alkyl-sn-glycero-3-phosphoethanolamine and analogue substrates
0.00055 - 0.0034
1-arachidonoyl-lysophosphatidic acid
0.01031 - 0.06
1-arachidoyl-lysophosphatidic acid
0.01299 - 0.06
1-hexanoyl-lysophosphatidic acid
0.00021 - 0.0018
1-linoleoyl-lysophosphatidic acid
0.005 - 0.0065
1-myristoyl-lysophosphatidic acid
0.0012 - 0.0096
1-oleoyl-lysophosphatidic acid
0.00141 - 0.0104
1-palmitoyl-lysophosphatidic acid
0.00209 - 0.0258
1-stearoyl-lysophosphatidic acid
0.0034
2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.004
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
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0042
2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0071
2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0026
2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0074
2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0045
2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0007
2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0057
2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0132
2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0132
2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0002
2-amino-2-(2-(4-octylphenyl) ethyl)propan-1,3-diol
-
substrate p-nitrophenyl thymidine 5-monophosphate, pH 8.0, 30 min of incubation at 37°C, measuring absorbance at 405 nm, twofold higher KI compared to inhibitor S1P
0.000018
cyclohexanaminium hydrogen [4-(decanoylamino)benzyl]phosphonate
-
pH and temperature not specified in the publication
0.000512
cyclohexanaminium hydrogen [4-(heptanoylamino)benzyl]phosphonate
-
pH and temperature not specified in the publication
0.000009
cyclohexanaminium hydrogen [4-(tetradecanoylamino)benzyl]phosphonate
-
pH and temperature not specified in the publication
0.000834
cyclohexanaminium hydrogen [fluoro[4-(heptanoylamino)phenyl]methyl]phosphonate
-
pH and temperature not specified in the publication
0.0000061 - 0.000072
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate
0.000024 - 0.0000242
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate
0.001009
cyclohexanaminium hydrogen [[4-(heptanoylamino)phenyl](hydroxy)methyl]phosphonate
-
pH and temperature not specified in the publication
0.0151
H2L 5564949
-
with respect to ATX-mediated FS-3 hydrolysis
0.002
H2L 5761473
-
with respect to ATX-mediated FS-3 hydrolysis
0.0027
H2L 7839888
-
with respect to ATX-mediated FS-3 hydrolysis
0.0019 - 0.0065
H2L 7905958
0.0093
H2L 7921385
-
with respect to ATX-mediated FS-3 hydrolysis
0.00011
lysophosphatidic acid
-
-
0.00001
PF8380
-
pH and temperature not specified in the publication
0.00021 - 0.0018
sphingosine-1-phosphate
0.0225 - 0.027
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid
0.0047 - 0.2175
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid
0.001 - 0.0111
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
0.0088 - 0.0265
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid
0.083
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxypyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0016 - 0.0035
[(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.0039 - 0.0116
[(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.0889 - 0.399
[(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.0015 - 1.059
[(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.0043 - 0.0062
[(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.0044
[(2R,3S)-4-[4-[(3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.011 - 0.5841
[(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
0.00055
1-arachidonoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay
0.0034
1-arachidonoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, spectrophotometric assay
0.01031
1-arachidoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, fluorometric assay
0.06
1-arachidoyl-lysophosphatidic acid
-
> 60 microM, inhibition of lysoPLD activity, spectrophotometric assay
0.01299
1-hexanoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, fluorometric assay
0.06
1-hexanoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, > 60 microM, size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay
0.00021
1-linoleoyl-lysophosphatidic acid
-
most potent in the inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay
0.0018
1-linoleoyl-lysophosphatidic acid
-
competitive inhibition, spectrophotometric assay
0.005
1-myristoyl-lysophosphatidic acid
-
most potent in inhibiting lysoPLD activity, spectrophotometric assay
0.0065
1-myristoyl-lysophosphatidic acid
-
most potent in inhibiting lysoPLD activity, fluorometric assay
0.0012
1-oleoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, based on fluoresecent assay, same order of inhibitory potency among lysophosphatidic acid analogs with different acyl chains in the spectrophotometric assay
0.0096
1-oleoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity, spectrophotometric assay
0.00141
1-palmitoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, fluorometric assay
0.0104
1-palmitoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay
0.00209
1-stearoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, fluorometric assay
0.0258
1-stearoyl-lysophosphatidic acid
-
inhibition of lysoPLD activity,size of acyl chain is crucial for the maximal inhibitory action, spectrophotometric assay
0.0000061
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate
-
pH and temperature not specified in the publication
0.000072
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](fluoro)methyl]phosphonate
-
pH and temperature not specified in the publication
0.000024
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate
-
pH and temperature not specified in the publication
0.0000242
cyclohexanaminium hydrogen [[4-(decanoylamino)phenyl](hydroxy)methyl]phosphonate
-
pH and temperature not specified in the publication
0.0019
H2L 7905958
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0019
H2L 7905958
-
with respect to ATX-mediated FS-3 hydrolysis
0.0065
H2L 7905958
-
with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis
0.00021
sphingosine-1-phosphate
-
SIP, inhibition of lysoPLD activity, fluorometric assay
0.0018
sphingosine-1-phosphate
-
SIP, inhibition of lysoPLD activity, spectrophotometric assay
0.0225
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.027
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-(pyridin-2-ylmethoxy)phenyl]butyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0047
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.2175
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.001
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0111
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0088
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0265
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3-methylbenzyl)oxy]phenyl]butyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0016
[(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0035
[(2R,3S)-4-(4-[[3,5-dimethyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methoxy]phenyl)-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0039
[(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0116
[(2R,3S)-4-[4-(benzyloxy)phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0889
[(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.399
[(2R,3S)-4-[4-[(2,4-dichlorobenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0015
[(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
1.059
[(2R,3S)-4-[4-[(3,5-dimethyl-4-propoxypyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.0043
[(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
0.0062
[(2R,3S)-4-[4-[(3,5-dimethylbenzyl)oxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.011
[(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
anti configuration, pH and temperature not specified in the publication
0.5841
[(2R,3S)-4-[4-[(4-ethoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]-3-(hexadecanoylamino)-2-hydroxybutyl]phosphonic acid
-
syn configuration, pH and temperature not specified in the publication
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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
0.00017
(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
0.0013
2-(4-[[(2,5-dichlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0341
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
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0304
2-(4-[[(3,5-dimethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0286
2-(4-[[(3-benzothiadiazolphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0097
2-(4-[[(3-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0161
2-(4-[[(3-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0016
2-(4-[[(3-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0177
2-(4-[[(3-methoxyphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0135
2-(4-[[(3-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0009
2-(4-[[(3-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0107
2-(4-[[(4-chlorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0177
2-(4-[[(4-fluorophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0015
2-(4-[[(4-iodophenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0161
2-(4-[[(4-methylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0327
2-(4-[[(4-trifluoromethylphenyl)amino]carbonothioyl]-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
Homo sapiens
-
1 mM each CaCl2 and MgCl2, 5 mM KCl, and 140 mM NaCl, in 50 mM Tris, pH 8.0, at 37°C
0.0003
2-amino-2-(2-(4-octylphenyl) ethyl)propan-1,3-diol
Homo sapiens
-
to 0.0004, substrate p-nitrophenyl thymidine 5-monophosphate, pH 8.0, 30 min of incubation at 37°C, measuring absorbance at 405 nm, compared to inhibitor S1P 0.0001 mM
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
0.00023
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
0.0128
H2L 5564949
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0128
H2L 5761473
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0015 - 0.0017
H2L 7839888
0.0012 - 0.0016
H2L 7905958
0.0016
H2L 7921385
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0753 - 0.1035
Human serum albumin
-
0.0016 - 0.0029
hypericin
0.000016 - 0.000038
lysophosphatidic acid
0.187 - 0.317
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
0.000028
[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
0.000022
[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
0.0068
H2L 5210574
Homo sapiens
-
with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis
0.0068
H2L 5210574
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0015
H2L 7839888
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0017
H2L 7839888
Homo sapiens
-
with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis
0.0012
H2L 7905958
Homo sapiens
-
with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis
0.0016
H2L 7905958
Homo sapiens
-
-
0.0016
H2L 7905958
Homo sapiens
-
with respect to ATX-mediated FS-3 hydrolysis
0.0753
Human serum albumin
Homo sapiens
incubating human autotaxin beta with human serum albumin
-
0.1035
Human serum albumin
Homo sapiens
incubating human autotaxin gamma with human serum albumin
-
0.0016
hypericin
Mus musculus
tested on murine autotaxin alpha
0.0025
hypericin
Homo sapiens
tested on human autotaxin gamma
0.0026
hypericin
Mus musculus
tested on murine autotaxin gamma
0.0028
hypericin
Mus musculus
tested on murine autotaxin beta
0.0029
hypericin
Homo sapiens
tested on human autotaxin beta
0.000016
lysophosphatidic acid
Homo sapiens
reported as an inhibitor of its own production, incubating human autotaxin gamma with lysophosphatidic acid
0.000017
lysophosphatidic acid
Homo sapiens
reported as an inhibitor of its own production, incubating human autotaxin beta with lysophosphatidic acid
0.000018
lysophosphatidic acid
Mus musculus
reported as an inhibitor of its own production, incubating murine autotaxin beta with lysophosphatidic acid
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
Homo sapiens
reported as an inhibitor of its own production, incubating human autotaxin alpha 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
-
0.317
murine serum albumin
Mus musculus
incubating murine autotaxin beta with murine serum albumin
-
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0.000005 - 0.000076
-
depending on presence of divalent cations
0.0051
Murine autotaxin gamma, p-nitrophenyl phenylphosphonate as a substrate, Vmax 1.8 nmol p-nitrophenyl/min
0.00847
human autotaxin alpha, p-nitrophenyl phenylphosphonate as a substrate, Vmax 0.67 nmol p-nitrophenyl/min
0.0163
Murine autotaxin alpha, p-nitrophenyl phenylphosphonate as a substrate, Vmax 0.35 nanomol p-nitrophenyl/min
0.036
-
using isotopic assay
0.048
-
colorimetric assay, 6 h incubation, 37°C
0.0919
Murine autotaxin beta, para-nitrophenyl phenylphosphonate as a substrate, Vmax 1.9 nmol para-nitrophenyl/min
0.0997
Human autotaxin gamma, p-nitrophenyl phenylphosphonate as a substrate, Vmax 1.6 nmol p-nitrophenyl/min
0.135
Human autotaxin beta, p-nitrophenyl phenylphosphonate as a substrate, Vmax 1.9 nmol p-nitrophenyl/min
0.14
-
purified enzyme, HiTrap DEAE FF
additional information
-
Spectrophotometric assay of LysoPLD activity. Determination of lysoPLD activity by measuring the amount of choline released from exogenously added LPC. Fluorometric assay for LysoPLD activity. Determination of LysoPLD activity using a fluorogenic substrate, [5-[[(23S)-33-(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]phenyl)-20,23-dihydroxy-20-oxido-15,26,33-trioxo-3,6,9,12,19,21,25-heptaoxa-16,32-diaza-20-phosphatritriacont-1-yl]carbamoyl]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)phenyl]acetic acid (FS-3)
additional information
-
lysoPLD activity of diluted or undiluted egg white measured based on enzyme-linked fluorometric measurement of choline produced together with lysophosphatidic acid from exogenous lysophosphatidylcholine. LysoPLD activity measured by determining lysophosphatidic acid and choline by MALDI-TOF-MS, mass spectrometric and enzyme-linked fluorometric analysis. Quantitative analysis of lysophosphatidic acid by MALDI-TOF-MS using a phosphate-capture molecule. Production of lysophosphatidic acid during incubation of hen egg white, changes in the levels of fatty acyl groups
additional information
-
autotaxin/lysoPLD activity is determined at the indicated substrate concentrations using conditioned medium from V5-autotaxin expressing cells as the source of enzyme and radiolabeled lysophosphatidylcholine as substrate
additional information
biochemical and cell biological activity of hATX S48 protein measured
additional information
-
biochemical and cell biological activity of hATX S48 protein measured
additional information
-
lysoPLD activity is assessed, based on the amount of choline released with lysophosphatidylcholine as the substrate, absorption spectrometry. Amounts of the substrate lysophosphatidylcholine and the product lysophosphatidic acid are also checked simultaneously. Changes in the lysoPLD activity and lysophosphatidylcholine and lysophosphatidic acid concentrations in incubated serum. Concentrations of lysophosphatidylcholine and lysophosphatidic acid increase upon incubation, the levels increase significantly as compared with those in the controls (no incubation) after 60-min incubations. Dramatic increase in the lysophosphatidic acid concentration is observed, and the lysophosphatidic acid level after 180-min incubation is about 15times higher than in the control
additional information
-
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl phenylphosphonate substrate
additional information
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl phenylphosphonate substrate
additional information
-
approx. 0 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 0 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 0 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 10 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 100 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 1000 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 104 micromol/ml/min, serum from a patient with severe pre-eclampsia, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 1100 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 118 micromol/ml/min, serum from a patient with preterm labor (30.1 +/- 0.8 gestational weeks; n is 21), diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 139 micromol/ml/min, serum from a patient with preterm labor (30.1 +/- 0.8 gestational weeks; n is 21), diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 18:2-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 146 micromol/ml/min, serum from a patient with severe pre-eclampsia, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 18:2-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 15 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 15 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 150 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 153 micromol/ml/min, serum from a woman with normal pregnancy (35.8 +/- 0.7 gestational weeks; n is 25), diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 18:2-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 180 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 200 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 300 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 350 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 400 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 450 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 450 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 450 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 49 micromol/ml/min, serum from a patient with moderate pre-eclampsia, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 18:2-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 5 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 500 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 500 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 60 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 65 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 65 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 65 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 1fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 700 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 100fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 8 mmol/ml/min, serum from a patient with preterm labor, detection of dilution dependency of choline-producing activity of sera, diluted 30fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 8 mmol/ml/min, serum from a woman with normal pregnancy, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
approx. 80 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 3.3fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 90 micromol/ml/min, serum from a woman with normal pregnancy (35.8 +/- 0.7 gestational weeks; n is 25), diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx. 92 micromol/ml/min, serum from a patient with moderate pre-eclampsia, diluted 3.3fold (serum + saline), presence of 0.15 mM exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate, 37°C
additional information
-
approx.50 mmol/ml/min, serum from a patient with severe pre-eclampsia, detection of dilution dependency of choline-producing activity of sera, diluted 10fold (serum + saline), absence of exogenous 16:0-lysophosphatidylcholine, radiolabeled substrate , 37°C
additional information
-
overview of methods for determination of autotaxin/lysoPLD activity. Using radiolabeled substrates and fluorogenic substrates for measuring autotaxin/lysoPLD activity
additional information
-
lysophospholipase D activity is measured by conversion of radiolabeled lysophosphatidylcholine into radiolabeled lysophosphatidic acid
additional information
-
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl phenylphosphonate substrate
additional information
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl phenylphosphonate substrate
additional information
-
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl-phenylphosphonate substrate
additional information
phosphodiesterase activity of recombinant autotaxin is measured by using p-nitrophenyl-phenylphosphonate substrate
additional information
-
phosphodiesterase activity of recombinant autotaxin is measured by using para-nitrophenyl phenylphosphonate substrate
additional information
phosphodiesterase activity of recombinant autotaxin is measured by using para-nitrophenyl phenylphosphonate substrate
additional information
-
To deplete ATX from mouse serum, mouse serum is incubated with the 5E5-Sepharose 4B for 2 h at 4°C, and the resulting supernatant is used for measuring lysoPLD activity and lysophosphatidic acid production. Lysophospholipase D activity of plasma and amniotic fluids isolated from atx+/+ and atx+/-adult mice or atx+/+ and atx+/-embryos at different stages of development measured with immunohistochemistry. LysoPLD activity is determined by liberation of choline from lysophosphatidylcholine using myristyl-lysophosphatidylcholine as a substrate
additional information
-
approx. 400 micromol/min/ml, mice are treated with control rat IgG, plasma samples (10 microl) incubate with 4 mmol/l lysophosphatidylcholine, activity determined by enzymatic photometric method using choline oxidase at 560 nm, 37°C
additional information
-
approx. 42 micromol/min/ml, mice are treated with anti-ATX mAb, plasma samples (10 microl) incubate with 4 mmol/l lysophosphatidylcholine, activity determined by enzymatic photometric method using choline oxidase at 560 nm, 37°C
additional information
-
nuclear fraction has relatively high levels of lysoPLD activity. Both lysoPLD activity and highest band density found in microsomal fraction
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