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Literature summary for 3.1.1.23 extracted from

  • King, A.R.; Dotsey, E.Y.; Lodola, A.; Jung, K.M.; Ghomian, A.; Qiu, Y.; Fu, J.; Mor, M.; Piomelli, D.
    Discovery of potent and reversible monoacylglycerol lipase inhibitors (2009), Chem. Biol., 16, 1045-1052.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.23

Cloned(Commentary)

Cloned (Comment) Organism
HeLa cells transiently transfected with pEF6 vector containing full-length ABHD6 or ABHD12 Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
celastrol inhibits MGL activity, albeit less potently than pristimerin Rattus norvegicus
dihydrocelastrol inhibits MGL activity, albeit less potently than pristimerin Rattus norvegicus
dihydrocelastryl diacetate inhibits MGL activity, albeit less potently than pristimerin Rattus norvegicus
euphol inhibits MGL activity with high potency. Blocks MGL activity through a reversible and noncompetitive mechanism, which is apparently identical to that of pristimerin Rattus norvegicus
pristimerin inhibits MGL activity with high potency. Addition to purified MGL produces an almost immediate blockade of MGL activity. Inhibits MGL through a mechanism that is rapid, reversible, and noncompetitive Rattus norvegicus
pristimerol inhibits MGL activity, albeit less potently than pristimerin Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000014
-
 2-oleoylglycerol in the presence of 0.0005 mM pristimerin, at pH 7.5, 37°C Rattus norvegicus
0.000024
-
 2-oleoylglycerol in the presence of 0.0003 mM pristimerin, at pH 7.5, 37°C Rattus norvegicus
0.000027
-
 2-oleoylglycerol in the presence of 0.0001 mM pristimerin, at pH 7.5, 37°C Rattus norvegicus
0.000028
-
 2-oleoylglycerol in the presence of vehicle (0.1% DMSO), at pH 7.5, 37°C Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
 Wistar rats
-

Purification (Commentary)

Purification (Comment) Organism
-
 Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
brain MGL is localized to axon terminals throughout the brain Rattus norvegicus
-
embryo day 18-20 Rattus norvegicus
-
neuron
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
MGL
-
 Rattus norvegicus
monoacylglycerol lipase
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000093
-
 purified MGL, at pH 7.5, 37°C Rattus norvegicus pristimerin
0.000315
-
 purified MG, at pH 7.5, 37°CL Rattus norvegicus euphol
0.000398
-
 nonpurified MGL, at pH 7.5, 37°C Rattus norvegicus pristimerin
0.000882
-
 nonpurified MGL, at pH 7.5, 37°C Rattus norvegicus euphol
0.0016
-
 purified MGL, at pH 7.5, 37°C Rattus norvegicus celastrol
0.004
-
 purified MGL, at pH 7.5, 37°C Rattus norvegicus pristimerol
0.015
-
 purified MGL, at pH 7.5, 37°C Rattus norvegicus dihydrocelastrol
0.015
-
 purified MGL, at pH 7.5, 37°C Rattus norvegicus dihydrocelastryl diacetate