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Literature summary for 3.1.1.116 extracted from

  • Bisogno, T.; Howell, F.; Williams, G.; Minassi, A.; Cascio, M.; Ligresti, A.; Matias, I.; Schiano-Moriello, A.; Paul, P.; Williams, E.; Gangadbaran, U.; Hobbs, C.; Di Marzo, V.; Doherty, P.
    Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain (2003), J. Cell Biol., 163, 463-468 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
glutathione
-
Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
gene DAGLA, DNA and amino acid sequence determination and analysis, sequence comparisons of the two isozymes, real-time RT-PCR analysis of DAGLalpha expression, recombinant expression of V5- and His-tagged isozyme DAGLalpha in COS-7 cells Homo sapiens
gene DAGLB, DNA and amino acid sequence determination and analysis, sequence comparisons of the two isozymes, recombinant expression of FLAG-tagged isozyme DAGLbeta in COS-7 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
HgCl2
-
Homo sapiens
additional information no inhibition by PMSF; no inhibition by PMSF Homo sapiens
p-hydroxy-mercuri-benzoate
-
Homo sapiens
RHC80267 blocks 2-AG formation from intact cells; blocks 2-AG formation from intact cells Homo sapiens
tetrahydrolipstatin THL, THL inhibits the neurite outgrowth response stimulated by FGF2, at 100 nM it inhibits 66.7%, 93.5% and 99.2% of AG-2 release in N18-TG2, C6, and RBL-2H3 cells, respectively. IC50 of 0.002 mM for the inhibition by THL of FGF2 response; THL, THL inhibits the neurite outgrowth response stimulated by FGF2, at 100 nM it inhibits 66.7%, 93.5% and 99.2% of AG-2 release in N18-TG2, C6, and RBL-2H3 cells, respectively. IC50 of 0.002 mM for the inhibition by THL of FGF2 response Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.1588
-
sn-1-stearoyl-2-arachidonoyl-glycerol pH 7.0, 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required for activity Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1,2-di-(9Z-octadecenoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction (9Z)-octadecenoate + 2-(9Z-octadecenoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction (9Z)-octadecenoate + 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-(9Z,12Z-octadecadienoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction (9Z)-octadecenoate + 2-(9Z,12Z-octadecadienoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-O-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction (9Z)-octadecenoate + 2-O-(5Z,8Z,11Z,14Z)-eicosatetraenoylglycerol
-
?
1-(9Z-octadecenoyl)-2-octadecanoyl-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction (9Z)-octadecenoate + 2-octadecanoylglycerol
-
?
1-acyl-2-arachidonoyl-sn-glycerol + H2O Homo sapiens
-
2-arachidonoylglycerol + fatty acid
-
?
1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward direction 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + octadecanoate
-
?
1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O Homo sapiens the reaction proceeds in the forward reaction 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + octadecanoate
-
?
sn-1-stearoyl-2-arachidonoyl-glycerol + H2O Homo sapiens
-
2-arachidonoylglycerol + stearate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8NCG7
-
-
Homo sapiens Q9Y4D2
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain two closely related genes are identified and their expression in cells correlates with 2-arachidonoylglycerol (2-AG) biosynthesis and release. The expression of both enzymes changes from axonal tracts in the embryo to dendritic fields in the adult, and this correlates with the developmental change in requirement for 2-AG synthesis from the pre- to the postsynaptic compartment. This switch provides a possible explanation for a fundamental change in endocannabinoid function during brain development Homo sapiens
-
C6 glioma cell
-
Homo sapiens
-
Caco-2 cell
-
Homo sapiens
-
embryo
-
Homo sapiens
-
HEK-293 cell
-
Homo sapiens
-
additional information real-time RT-PCR analysis of DAGLalpha expression in various tissues Homo sapiens
-
N18TG2 cell neuroblastoma cells Homo sapiens
-
neuron
-
Homo sapiens
-
RBL-2H3 cell basophilic leukemia cells Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,2-di-(9Z-octadecenoyl)-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens (9Z)-octadecenoate + 2-(9Z-octadecenoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens (9Z)-octadecenoate + 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-(9Z,12Z-octadecadienoyl)-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens (9Z)-octadecenoate + 2-(9Z,12Z-octadecadienoyl)-glycerol
-
?
1-(9Z-octadecenoyl)-2-O-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens (9Z)-octadecenoate + 2-O-(5Z,8Z,11Z,14Z)-eicosatetraenoylglycerol
-
?
1-(9Z-octadecenoyl)-2-octadecanoyl-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens (9Z)-octadecenoate + 2-octadecanoylglycerol
-
?
1-acyl-2-arachidonoyl-sn-glycerol + H2O
-
Homo sapiens 2-arachidonoylglycerol + fatty acid
-
?
1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O the reaction proceeds in the forward direction Homo sapiens 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + octadecanoate
-
?
1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycerol + H2O the reaction proceeds in the forward reaction Homo sapiens 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + octadecanoate
-
?
sn-1-stearoyl-2-arachidonoyl-glycerol + H2O
-
Homo sapiens 2-arachidonoylglycerol + stearate
-
?

Synonyms

Synonyms Comment Organism
DAGLA
-
Homo sapiens
DAGLalpha
-
Homo sapiens
DAGLB
-
Homo sapiens
DAGLbeta
-
Homo sapiens
neural stem cell-derived dendrite regulator UniProt Homo sapiens
sn1-DAG lipase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
-
Homo sapiens

General Information

General Information Comment Organism
physiological function enzyme sn1-DAG lipase is involved in the spatial and temporal regulation of endocannabinoid signaling in the brain. The diacylglycerol (DAG) lipase activity is required for axonal growth during development and for retrograde synaptic signaling at mature synapses. This enzyme synthesizes the endocannabinoid 2-arachidonoyl-glycerol (2-AG), and the CB1 cannabinoid receptor is also required for the above responses Homo sapiens