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Literature summary extracted from

  • Tyukhtenko, S.; Karageorgos, I.; Rajarshi, G.; Zvonok, N.; Pavlopoulos, S.; Janero, D.R.; Makriyannis, A.
    Specific inter-residue interactions as determinants of human monoacylglycerol lipase catalytic competency a role for global conformational chanages (2016), J. Biol. Chem., 291, 2556-2565 .
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
3.1.1.23 H103A site-directed mutagenesis, the mutant shows 20fold reduced catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 H269A site-directed mutagenesis, structural comparison to the wild-type enzyme by NMR spectrometry Homo sapiens
3.1.1.23 H272A site-directed mutagenesis, the mutant shows 13fold reduced catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 H272S site-directed mutagenesis, the mutant shows 58fold reduced catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 H272Y site-directed mutagenesis, the muant shows 12fold reduced catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 H49A site-directed mutagenesis, the mutant shows 5fold reduced catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 H54A site-directed mutagenesis, structural comparison to the wild-type enzyme by NMR spectrometry, the mutant shows a dramatic 25000fold loss in hMGL catalytic efficiency compared to wild-type Homo sapiens
3.1.1.23 L169S/L176S site-directed mutagenesis, hMGL function is not significantly compromised by the mutation, structural comparison to the wild-type enzyme by NMR spectrometry Homo sapiens
3.1.1.23 S122C site-directed mutagenesis, structural comparison to the wild-type enzyme by NMR spectrometry Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 additional information structure-based MGL inhibitor design Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.23 additional information
-
 additional information Michaelis-Menten kinetics Homo sapiens
3.1.1.23 0.012
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H54A Homo sapiens
3.1.1.23 0.022
-
 2-arachidonoylglycerol pH 7.4, 22°C, soluble wild-type variant Homo sapiens
3.1.1.23 0.0222
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272A Homo sapiens
3.1.1.23 0.0308
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272S Homo sapiens
3.1.1.23 0.0362
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272Y Homo sapiens
3.1.1.23 0.0366
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H49A Homo sapiens
3.1.1.23 0.122
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H103A Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.23 Homo sapiens Q99685
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-arachidonoylglycerol + H2O
-
 Homo sapiens arachidonoate + glycerol
-
 ?
3.1.1.23 additional information direct NMR detection of a reversible equilibrium between active and inactive states of human MGL (hMGL) that is slow on the NMR time scale and can be modulated in a controlled manner by pH, temperature, and select point mutations Homo sapiens ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.1.1.23 ? x * 34100, SDS-PAGE Homo sapiens
3.1.1.23 More simultaneous NMR detection of both active and inactive hMGL states in solution Homo sapiens

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.1.23 11
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H54A Homo sapiens
3.1.1.23 13000
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272S Homo sapiens
3.1.1.23 14000
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H103A Homo sapiens
3.1.1.23 45000
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272A Homo sapiens
3.1.1.23 70000
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272Y Homo sapiens
3.1.1.23 160000
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H49A Homo sapiens
3.1.1.23 570000
-
 2-arachidonoylglycerol pH 7.4, 22°C, soluble wild-type variant Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.23 7.4
-
 assay at Homo sapiens

General Information

EC Number General Information Comment Organism
3.1.1.23 evolution the enzyme is a member of the serine hydrolase superfamily Homo sapiens
3.1.1.23 additional information a network of aromatic interactions and hydrogen bonds regulates hMGL active-inactive state interconversion. Specific inter-residue interactions within hMGL modulate the enzymes function and implicate transitions between active (open) and inactive (closed) states of the hMGL lid domain in controlling substrate access to the enzymes active site. The residues Ser122, His269, and Asp239 form the catalytic triad, hMGL structure-function correlations, overview Homo sapiens
3.1.1.23 physiological function the serine hydrolase monoacylglycerol lipase (MGL) functions as the main metabolizing enzyme of 2-arachidonoyl glycerol, an endocannabinoid signaling lipid. Monoacylglycerol lipase is largely responsible for the catalytic inactivation of the endocannabinoid signaling lipid, 2-arachidonoylglycerol, and regulates a fatty acid network that promotes tumorigenesis Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.1.1.23 917
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H54A Homo sapiens
3.1.1.23 2027
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272A Homo sapiens
3.1.1.23 4372
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H49A Homo sapiens
3.1.1.23 25909
-
 2-arachidonoylglycerol pH 7.4, 22°C, soluble wild-type variant Homo sapiens
3.1.1.23 114754
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H103A Homo sapiens
3.1.1.23 422078
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272S Homo sapiens
3.1.1.23 1933700
-
 2-arachidonoylglycerol pH 7.4, 22°C, mutant H272Y Homo sapiens