Cloned (Comment) | Organism |
---|---|
full-length cDNA subcloned into the pEF15b vector containing an N-terminal histidine tag and transformed in Escherichia coli DH5alpha. Positive clones expressed in Escherichia coli Rosetta 2(De3)pLysS cells. Expression of wild-type and mutants in HeLa cells | Rattus norvegicus |
Protein Variants | Comment | Organism |
---|---|---|
C201G | causes significant decreases in enzyme activity, albeit smaller than that produced by mutant C242G. Inhibitory potency of N-arachidonylmaleimide is selectively decreased | Rattus norvegicus |
C208G | causes significant decreases in enzyme activity, albeit smaller than that produced by mutant C242G. Inhibitory potency of octhilinone is selectively decreased. Has no effect on the inhibitory potency of N-arachidonylmaleimide | Rattus norvegicus |
C242G | produces a striking reduction in MGL activity, due to a decrease in maximal reaction velocity rather than a change in Michaelis constant. Inhibitory potency of N-arachidonylmaleimide is selectively decreased | Rattus norvegicus |
C301G | has no effect on MGL activity | Rattus norvegicus |
C32G | has no effect on MGL activity | Rattus norvegicus |
C55G | has no effect on MGL activity | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(5E)-5-(3-methylbutylidene)-2-thioxo-1,3-thiazolidin-4-one | weak inhibitory effect | Rattus norvegicus | |
2-methyl-4-isothiazolin-3-one | - |
Rattus norvegicus | |
2-octyl-4-isothiazolin-3-one | octhilinone, inhibits purified recombinant MGL through a partially reversible mechanism that involves a specific interaction with cysteine 208 | Rattus norvegicus | |
2-octyl-benzo[d]isothiazol-3-one | - |
Rattus norvegicus | |
2-oleoyl-4-isothiazolin-3-one | - |
Rattus norvegicus | |
3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine | weak inhibitory effect | Rattus norvegicus | |
additional information | 3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine and 3-propoxy-2-benzofuran-1(3H)-one do not inhibit | Rattus norvegicus | |
N-arachidonylmaleimide | inhibitory effect is attributed to the ability of this compound to react with C242 and form a Michael addition product | Rattus norvegicus | |
N-ethylmaleimide | - |
Rattus norvegicus |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.098 | - |
2-oleoylglycerol | mutant C242G | Rattus norvegicus | |
0.115 | - |
2-oleoylglycerol | wild-type | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
by gel filtration | Rattus norvegicus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
2-oleoylglycerol + H2O | Cys208 plays an important role in MGL function | Rattus norvegicus | oleic acid + glycerol | - |
? |
Synonyms | Comment | Organism |
---|---|---|
MGL | - |
Rattus norvegicus |
monoacylglycerol lipase | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00003 | - |
wild-type, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | N-arachidonylmaleimide | |
0.000043 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 2-oleoyl-4-isothiazolin-3-one | |
0.000046 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/mlL bovine serum albumin, fatty acid-free | Rattus norvegicus | N-arachidonylmaleimide | |
0.000059 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 2-octyl-benzo[d]isothiazol-3-one | |
0.000107 | - |
mutant C242G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | N-arachidonylmaleimide | |
0.000151 | - |
wild-type, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 2-octyl-4-isothiazolin-3-one | |
0.000239 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 2-methyl-4-isothiazolin-3-one | |
0.000442 | - |
mutant C201G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | N-arachidonylmaleimide | |
0.000722 | - |
mutant C208G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 2-octyl-4-isothiazolin-3-one | |
0.0027 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | N-ethylmaleimide | |
0.02 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | (5E)-5-(3-methylbutylidene)-2-thioxo-1,3-thiazolidin-4-one | |
0.028 | - |
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free | Rattus norvegicus | 3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine |