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Literature summary extracted from

  • Morris, A.J.; Smyth, S.S.
    Measurement of autotaxin/lysophospholipase D activity (2007), Methods Enzymol., 434, 89-104.
    View publication on PubMed

Application

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

Inhibitors

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

KM Value [mM]

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

Localization

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
-
-

Natural Substrates/ Products (Substrates)

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
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.39 Homo sapiens
-
-
-
3.1.4.39 Mammalia
-
-
-

Source Tissue

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
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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 ?
-
?

Subunits

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

Synonyms

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