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Literature summary extracted from

  • Labar, G.; Bauvois, C.; Muccioli, G.G.; Wouters, J.; Lambert, D.M.
    Disulfiram is an inhibitor of human purified monoacylglycerol lipase, the enzyme regulating 2-arachidonoylglycerol signaling (2007), Chembiochem, 8, 1293-1297.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.1.1.23 drug development the enzyme is a target for design of potent and selective inhibitors Homo sapiens
3.1.1.23 pharmacology the enzyme is a therapeutic target Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.23 functional overexpression of His6-tagged and streptavidin-tagged enzyme in Escherichia coli as soluble protein in the supernatant Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 2-arachidonoylglycerol
-
Homo sapiens
3.1.1.23 4-chloromercuribenzoic acid
-
Homo sapiens
3.1.1.23 6-methyl-2-p-tolylamino-benzo[d] [1,3]oxazin-4-one i.e. URB754 Homo sapiens
3.1.1.23 arachidonoyltrifluoromethyl ketone i.e. ATFMK Homo sapiens
3.1.1.23 biphenyl-3-yl-carbamic acid cyclohexyl ester i.e. URB602 Homo sapiens
3.1.1.23 Disulfiram i.e. tetraethylthiuram disulfide, a compound used to treat alcoholism, inhibition likely through an interaction with cysteine residues Cys208 and/or Cys242, the inhibition is reversible by DTT Homo sapiens
3.1.1.23 Mercury chloride
-
Homo sapiens
3.1.1.23 methyl arachidonyl fluorophosphonate i.e. MAFP Homo sapiens
3.1.1.23 additional information no inhibition by URB754 Homo sapiens
3.1.1.23 N-arachidonoylmaleimide irreversible inhibition Homo sapiens
3.1.1.23 N-ethylmaleimide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.1.23 additional information Homo sapiens key enzyme responsible for the termination of endocannabinoid signaling with a crucial role in 2-arachidonoylglycerol metabolism, MAGL is unable to mediate anandamide degradation, overview ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.23 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.23 recombinant His6-tagged and streptavidin-tagged enzyme from Escherichia coli to homogeneity by Strep-tag targeting afffinity chromatography and nickel affinity chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.23 brain
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-oleoylglycerol + H2O
-
Homo sapiens glycerol + oleic acid
-
?
3.1.1.23 additional information key enzyme responsible for the termination of endocannabinoid signaling with a crucial role in 2-arachidonoylglycerol metabolism, MAGL is unable to mediate anandamide degradation, overview Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.23 MAGL
-
Homo sapiens
3.1.1.23 monoacylglycerol lipase
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.23 37
-
assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.23 8
-
assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 additional information
-
-
Homo sapiens additional information