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Literature summary extracted from

  • Zvonok, N.; Pandarinathan, L.; Williams, J.; Johnston, M.; Karageorgos, I.; Janero, D.R.; Krishnan, S.C.; Makriyannis, A.
    Covalent inhibitors of human monoacylglycerol lipase: ligand-assisted characterization of the catalytic site by mass spectrometry and mutational analysis (2008), Chem. Biol., 15, 854-862.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.23 mutant enzymes are expressed in Escherichia coli BL21 (DE3) cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.1.1.23 C215A the mutation does not affect MGL hydrolytic activity and displays heightened N-arachidonylmaleimide sensitivity Homo sapiens
3.1.1.23 C215A/C249A the mutation does not affect MGL hydrolytic activity Homo sapiens
3.1.1.23 C249A the mutation does not affect MGL hydrolytic activity and displays reduced N-arachidonylmaleimide sensitivity Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 AM6701 5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide Homo sapiens
3.1.1.23 AM6702
-
 Homo sapiens
3.1.1.23 N-arachidonylmaleimide
-
 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.1.1.23 34120
-
 calculated from amino acid sequence Homo sapiens
3.1.1.23 35000
-
 SDS-PAGE Homo sapiens

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.23 Talon metal affinity resin chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-arachidonoylglycerol + H2O
-
 Homo sapiens arachidonic acid + glycerol
-
 ?
3.1.1.23 arachidonoyl-7-hydroxy-6-methoxy-4-methylcoumarin ester + H2O
-
 Homo sapiens arachidonic acid + 7-hydroxy-6-methoxy-4-methylcoumarin
-
 ?

Subunits

EC Number Subunits Comment Organism
3.1.1.23 monomer 1 * 35000, SDS-PAGE Homo sapiens

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 0.0000009
-
 native enzyme, in 50 mM Tris-HCl (pH 7.4) containing 8% DMSO, at room temperature Homo sapiens AM6701
3.1.1.23 0.0000017
-
 recombinant enzyme, in 50 mM Tris-HCl (pH 7.4) containing 8% DMSO, at room temperature Homo sapiens AM6701
3.1.1.23 0.0000091
-
 native enzyme, in 50 mM Tris-HCl (pH 7.4) containing 8% DMSO, at room temperature Homo sapiens N-arachidonylmaleimide
3.1.1.23 0.0001
-
 native enzyme, in 50 mM Tris-HCl (pH 7.4) containing 8% DMSO, at room temperature Homo sapiens AM6702
3.1.1.23 0.0028
-
 native enzyme, in 50 mM Tris-HCl (pH 7.4) containing 8% DMSO, at room temperature Homo sapiens AM6702