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Literature summary for 3.1.1.23 extracted from
- Disulfiram is an inhibitor of human purified monoacylglycerol lipase, the enzyme regulating 2-arachidonoylglycerol signaling (2007), Chembiochem, 8, 1293-1297.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | the enzyme is a target for design of potent and selective inhibitors | Homo sapiens |
| pharmacology | the enzyme is a therapeutic target | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| functional overexpression of His6-tagged and streptavidin-tagged enzyme in Escherichia coli as soluble protein in the supernatant | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-arachidonoylglycerol | - |
Homo sapiens |  |
| 4-chloromercuribenzoic acid | - |
Homo sapiens | |
| 6-methyl-2-p-tolylamino-benzo[d] [1,3]oxazin-4-one | i.e. URB754 | Homo sapiens | |
| arachidonoyltrifluoromethyl ketone | i.e. ATFMK | Homo sapiens | |
| biphenyl-3-yl-carbamic acid cyclohexyl ester | i.e. URB602 | Homo sapiens | |
| 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 | |
| Mercury chloride | - |
Homo sapiens | |
| methyl arachidonyl fluorophosphonate | i.e. MAFP | Homo sapiens | |
| additional information | no inhibition by URB754 | Homo sapiens | |
| N-arachidonoylmaleimide | irreversible inhibition | Homo sapiens | |
| N-ethylmaleimide | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| 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
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2-oleoylglycerol + H2O | - |
Homo sapiens | glycerol + oleic acid | - |
? | |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| MAGL | - |
Homo sapiens |
| monoacylglycerol lipase | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
- |
Homo sapiens | additional information |
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Release 2023.1 (January 2023)
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