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Literature summary for 3.1.1.23 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
Search for more literature for 3.1.1.23

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

Synonyms Comment Organism
MGL
-
 Homo sapiens
monoacylglycerol lipase
-
 Homo sapiens

IC50 Value

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