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Literature summary for 3.1.1.23 extracted from

  • Vandevoorde, S.; Saha, B.; Mahadevan, A.; Razdan, R.K.; Pertwee, R.G.; Martin, B.R.; Fowler, C.J.
    Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase (2005), Biochem. Biophys. Res. Commun., 337, 104-109.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-arachidin 11% inhibition of the membraneous enzyme at 0.1 mM, 19% inhibition of the cytosolic enzyme at 0.1 mM Rattus norvegicus
1-arachidonoylglycerol IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible Rattus norvegicus
1-myristin IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible Rattus norvegicus
1-palmitin 44% inhibition of the membraneous enzyme at 0.1 mM, 38% inhibition of the cytosolic enzyme at 0.1 mM Rattus norvegicus
2,3-dihydroxypropyl (11Z)-icos-11-enoate i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79% Rattus norvegicus
2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (5Z)-icos-5-enoate i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65% Rattus norvegicus
2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible Rattus norvegicus
2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible Rattus norvegicus
additional information inhibitory potency of different 1-arachidonic acid analogues, the chain length of the fatty acid is important for affinity and inhibition, while methylations of the fatty acids do not influence the inhibitory potency, overview Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Rattus norvegicus 5829
-
membrane bound Rattus norvegicus 16020
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
Sprague-Dawley rats
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-oleoylglycerol + H2O
-
Rattus norvegicus oleic acid + glycerol
-
?

Synonyms

Synonyms Comment Organism
MAGL
-
Rattus norvegicus
MAGL-cy
-
Rattus norvegicus
MAGL-m
-
Rattus norvegicus
monoacylglycerol lipase
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0051
-
IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate
0.0083
-
i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate
0.0095
-
IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible Rattus norvegicus 1-arachidonoylglycerol
0.011
-
IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate
0.016
-
i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate
0.017
-
i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
0.026
-
i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79% Rattus norvegicus 2,3-dihydroxypropyl (11Z)-icos-11-enoate
0.032
-
IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible Rattus norvegicus 1-myristin
0.056
-
i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65% Rattus norvegicus 2,3-dihydroxypropyl (5Z)-icos-5-enoate
0.071
-
i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate
0.073
-
i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible Rattus norvegicus 2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate