EC Number | Application | Comment | Organism |
---|---|---|---|
3.1.4.39 | drug development | to inhibit lysophosphatidic acid production in the blood. Inhibition of autotaxin/lysoPLD activity by small molecules could be an effective new therapeutic approach for cancer and possibly cardiovascular disease | Mammalia |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
3.1.4.39 | 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 | Mammalia |
EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|---|
3.1.4.39 | 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 | Mammalia | |
3.1.4.39 | 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 | Mammalia | |
3.1.4.39 | 0.1 | - |
lysophosphatidylcholine | kinetic analysis of recombinant autotaxin/lysoPLD using [14C] lysophosphatidylcholine substrate | Homo sapiens |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
3.1.4.39 | extracellular | expression of V5-tagged autotaxin/lysoPLD in HEK293 cells, Western blotting experiments reveal that most of the recombinant autotaxin/lysoPLDaccumulates extracellularly | Homo sapiens | - |
- |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
3.1.4.39 | lysophosphatidylcholine + H2O | Mammalia | - |
lysophosphatidic acid + choline | - |
? | |
3.1.4.39 | lysophosphatidylcholine + H2O | Homo sapiens | - |
lysophosphatidic acid + choline | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
3.1.4.39 | Homo sapiens | - |
- |
- |
3.1.4.39 | Mammalia | - |
- |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
3.1.4.39 | HEK-293 cell | LysoPLD activity is determined in culture medium from control cells or cells expressing V5-autotaxin (ATX) | Homo sapiens | - |
EC Number | Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|---|
3.1.4.39 | 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 | Homo sapiens |
3.1.4.39 | additional information | - |
overview of methods for determination of autotaxin/lysoPLD activity. Using radiolabeled substrates and fluorogenic substrates for measuring autotaxin/lysoPLD activity | Mammalia |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
3.1.4.39 | coumarin-phosphate-fluorescein + H2O | - |
Mammalia | ? | - |
? | |
3.1.4.39 | lysophosphatidylcholine + H2O | - |
Mammalia | lysophosphatidic acid + choline | - |
? | |
3.1.4.39 | lysophosphatidylcholine + H2O | - |
Homo sapiens | lysophosphatidic acid + choline | - |
? | |
3.1.4.39 | lysophosphatidylcholine + H2O | - |
Mammalia | lysophosphatidic acid + choline | Hydrolysis of lysophospholipids by the secreted plasma protein autotaxin/lysophospholipase D (lysoPLD) is a major mechanism for generation of lysophosphatidic acid in the blood | ? | |
3.1.4.39 | sphingosylphosphorylcholine + H2O | 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 | Mammalia | sphingosine 1-phosphate + choline | bioactive lipid with a spectrum of signaling activities broadly similar to those of lysophosphatidic acid | ? | |
3.1.4.39 | [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 | 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 | Mammalia | ? | - |
? |
EC Number | Subunits | Comment | Organism |
---|---|---|---|
3.1.4.39 | More | single polypeptide with an N-terminal putative transmembrane domain, which may also function as a signal sequence specifying secretion of the protein | Mammalia |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
3.1.4.39 | autotaxin | - |
Mammalia |
3.1.4.39 | autotaxin | - |
Homo sapiens |
3.1.4.39 | autotaxin/lysoPLD | belongs to a family of six NPP enzymes, only autotaxin/lysoPLD has activity against phospho- and sphingolipid substrates | Mammalia |
3.1.4.39 | autotaxin/lysoPLD | belongs to a family of six NPP enzymes, only autotaxin/lysoPLD has activity against phospho- and sphingolipid substrates | Homo sapiens |
3.1.4.39 | lysophospholipase D | - |
Mammalia |
3.1.4.39 | lysophospholipase D | - |
Homo sapiens |
3.1.4.39 | lysoPLD | - |
Mammalia |
3.1.4.39 | lysoPLD | - |
Homo sapiens |