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Literature summary for 3.1.1.23 extracted from
- Synthesis and characterization of a new fluorogenic substrate for monoacylglycerol lipase and application to inhibition studies (2015), Anal. Bioanal. Chem., 407, 8163-8167 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| JZL184 | - |
Homo sapiens |  |
| methyl arachidonyl fluorophosphonate | - |
Homo sapiens | |
| URB602 | - |
Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q99685 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 7-hydroxycoumarinyl arachidonate + H2O | fluorescence detection using a fluorogenic probe 1,3-dihydroxypropan-2-yl-4-pyren-1-ylbutanoate | Homo sapiens | 7-hydroxycoumarin + arachidonate | - |
? | |
| 7-hydroxyresorufinyl arachidonate + H2O | a red fluorogenic substrate, 7-HRA, that is stable in 10% DMSO for at least 36 h at room temperature and for at least 6 months at 4°C, synthesis, overview | Homo sapiens | 7-hydroxyresorufin + arachidonate | - |
? | |
| additional information | human monoacylglycerol lipase (MAGL) displays catalytic activity on monoacyl glycerols with medium to long-chain lipophylic moieties such as stearoyl, palmitoyl, oleoyl, and especially arachidonoyl groups. MAGL also demonstrates preference for the hydrolysis of 2-acyl glycerols over their 1(3)-regioisomers. Measurement of MAGL-catalyzed hydrolysis of p-nitrophenyl alkyl esters by monitoring the liberation of p-nitrophenol. Fluorogenic enzyme assay method evaluation, 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 |
|---|---|---|---|
| 22 | - |
assay at room temperature | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000054 | - |
pH 7.4, 22°C | Homo sapiens | methyl arachidonyl fluorophosphonate | |
| 0.0002177 | - |
pH 7.4, 22°C | Homo sapiens | JZL184 | |
| 0.0091 | - |
pH 7.4, 22°C | Homo sapiens | URB602 | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| evolution | human monoacylglycerol lipase (MAGL) is a soluble serine hydrolase that belongs to the alpha/beta hydrolase fold superfamily | Homo sapiens |
| additional information | the enzyme is a serine hydrolase | Homo sapiens |
| physiological function | human monoacylglycerol lipase (MAGL) regulates 2-arachidonoyl glycerol level in the endocannabinoid system, which is implicated in a number of severe diseases. It is the main enzyme responsible for inactivating endocannabinoid agonist 2-arachidonoylglycerol (2-AG) for central CB1 and peripheral CB2 receptors and consequently for reducing its (patho)physiological effects. MAGL modulates endocannabinoid signaling in vivo by hydrolysis of 2-AG to arachidonic acid and glycerol | Homo sapiens |
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Release 2023.1 (January 2023)
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