Any feedback?
Literature summary for 3.1.4.39 extracted from
- Measurement of autotaxin/lysophospholipase D activity (2007), Methods Enzymol., 434, 89-104.
Application
| Application | Comment | Organism |
|---|---|---|
| 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 |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 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 |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 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 | |
| 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 | |
| 0.1 | - |
lysophosphatidylcholine | kinetic analysis of recombinant autotaxin/lysoPLD using [14C] lysophosphatidylcholine substrate | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | expression of V5-tagged autotaxin/lysoPLD in HEK293 cells, Western blotting experiments reveal that most of the recombinant autotaxin/lysoPLDaccumulates extracellularly | Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| lysophosphatidylcholine + H2O | Mammalia | - |
lysophosphatidic acid + choline | - |
? | |
| lysophosphatidylcholine + H2O | Homo sapiens | - |
lysophosphatidic acid + choline | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mammalia | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HEK-293 cell | LysoPLD activity is determined in culture medium from control cells or cells expressing V5-autotaxin (ATX) | Homo sapiens | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 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 |
| additional information | - |
overview of methods for determination of autotaxin/lysoPLD activity. Using radiolabeled substrates and fluorogenic substrates for measuring autotaxin/lysoPLD activity | Mammalia |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| coumarin-phosphate-fluorescein + H2O | - |
Mammalia | ? | - |
? | |
| lysophosphatidylcholine + H2O | - |
Mammalia | lysophosphatidic acid + choline | - |
? | |
| lysophosphatidylcholine + H2O | - |
Homo sapiens | lysophosphatidic acid + choline | - |
? | |
| 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 | ? | |
| 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 | ? | |
| [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 | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | single polypeptide with an N-terminal putative transmembrane domain, which may also function as a signal sequence specifying secretion of the protein | Mammalia |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| autotaxin | - |
Mammalia |
| autotaxin | - |
Homo sapiens |
| autotaxin/lysoPLD | belongs to a family of six NPP enzymes, only autotaxin/lysoPLD has activity against phospho- and sphingolipid substrates | Mammalia |
| autotaxin/lysoPLD | belongs to a family of six NPP enzymes, only autotaxin/lysoPLD has activity against phospho- and sphingolipid substrates | Homo sapiens |
| lysophospholipase D | - |
Mammalia |
| lysophospholipase D | - |
Homo sapiens |
| lysoPLD | - |
Mammalia |
| lysoPLD | - |
Homo sapiens |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
