Reference on EC 3.1.1.23 - acylglycerol lipase and Organism(s) Homo sapiens and UniProt Accession Q99685
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Somma-Delpero, C.; Valette, A.; Lepetit-Thevenin, J.; Nobili, O.; Boyer, J.; Verine, A.
Purification and properties of a monoacylglycerol lipase in human erythrocytes
Biochem. J.
312
519-525
1995
Homo sapiens
Dinh, T.P.; Kathuria, S.; Piomelli, D.
RNA interference suggests a primary role for monoacylglycerol lipase in the degradation of the endocannabinoid 2-arachidonoylglycerol
Mol. Pharmacol.
66
1260-1264
2004
Homo sapiens, Rattus norvegicus
Labar, G.; Bauvois, C.; Muccioli, G.G.; Wouters, J.; Lambert, D.M.
Disulfiram is an inhibitor of human purified monoacylglycerol lipase, the enzyme regulating 2-arachidonoylglycerol signaling
Chembiochem
8
1293-1297
2007
Homo sapiens
Chon, S.H.; Zhou, Y.X.; Dixon, J.L.; Storch, J.
Intestinal monoacylglycerol metabolism: developmental and nutritional regulation of monoacylglycerol lipase and monoacylglycerol acyltransferase
J. Biol. Chem.
282
33346-33357
2007
Homo sapiens, Mus musculus, Mus musculus C57BL/6
Saario, S.M.; Poso, A.; Juvonen, R.O.; Jaervinen, T.; Salo-Ahen, O.M.
Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system
J. Med. Chem.
49
4650-4656
2006
Homo sapiens, Rattus norvegicus
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
Chem. Biol.
15
854-862
2008
Homo sapiens
Muccioli, G.G.; Labar, G.; Lambert, D.M.
CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay
ChemBioChem
9
2704-2710
2008
Homo sapiens
Zvonok, N.; Williams, J.; Johnston, M.; Pandarinathan, L.; Janero, D.R.; Li, J.; Krishnan, S.C.; Makriyannis, A.
Full mass spectrometric characterization of human monoacylglycerol lipase generated by large-scale expression and single-step purification
J. Proteome Res.
7
2158-2164
2008
Rattus norvegicus (Q8R431), Homo sapiens (Q99685), Homo sapiens
Holtfrerich, A.; Makharadze, T.; Lehr, M.
High-performance liquid chromatography assay with fluorescence detection for the evaluation of inhibitors against human recombinant monoacylglycerol lipase
Anal. Biochem.
399
218-224
2010
Homo sapiens, Mus musculus, Rattus norvegicus
Wang, Y.; Chanda, P.; Jones, P.G.; Kennedy, J.D.
A fluorescence-based assay for monoacylglycerol lipase compatible with inhibitor screening
Assay Drug Dev. Technol.
6
387-393
2008
Homo sapiens
Labar, G.; Bauvois, C.; Borel, F.; Ferrer, J.L.; Wouters, J.; Lambert, D.M.
Crystal structure of the human monoacylglycerol lipase, a key actor in endocannabinoid signaling
ChemBioChem
11
218-227
2010
Homo sapiens (Q99685), Homo sapiens
Vandevoorde, S.
Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors
Curr. Top. Med. Chem.
8
247-267
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Bowman, A.L.; Makriyannis, A.
Refined homology model of monoacylglycerol lipase: toward a selective inhibitor
J. Comput. Aided Mol. Des.
23
799-806
2009
Homo sapiens (Q99685)
Feledziak, M.; Michaux, C.; Urbach, A.; Labar, G.; Muccioli, G.G.; Lambert, D.M.; Marchand-Brynaert, J.
beta-Lactams derived from a carbapenem chiron are selective inhibitors of human fatty acid amide hydrolase versus human monoacylglycerol lipase
J. Med. Chem.
52
7054-7068
2009
Homo sapiens
Bjoerklund, E.; Noren, E.; Nilsson, J.; Fowler, C.J.
Inhibition of monoacylglycerol lipase by troglitazone, N-arachidonoyl dopamine and the irreversible inhibitor JZL184: comparison of two different assays
Br. J. Pharmacol.
161
1512-1526
2010
Homo sapiens, Rattus norvegicus
Nomura, D.K.; Long, J.Z.; Niessen, S.; Hoover, H.S.; Ng, S.W.; Cravatt, B.F.
Monoacylglycerol lipase regulates a fatty acid network that promotes cancer pathogenesis
Cell
140
49-61
2010
Homo sapiens
Bertrand, T.; Auge, F.; Houtmann, J.; Rak, A.; Vallee, F.; Mikol, V.; Berne, P.; Michot, N.; Cheuret, D.; Hoornaert, C.; Mathieu, M.
Structural basis for human monoglyceride lipase inhibition
J. Mol. Biol.
396
663-673
2010
Homo sapiens
Karageorgos, I.; Tyukhtenko, S.; Zvonok, N.; Janero, D.R.; Sallum, C.; Makriyannis, A.
Identification by nuclear magnetic resonance spectroscopy of an active-site hydrogen-bond network in human monoacylglycerol lipase (hMGL): implications for hMGL dynamics, pharmacological inhibition, and catalytic mechanism
Mol. Biosyst.
6
1381-1388
2010
Homo sapiens
Schalk-Hihi, C.; Schubert, C.; Alexander, R.; Bayoumy, S.; Clemente, J.C.; Deckman, I.; DesJarlais, R.L.; Dzordzorme, K.C.; Flores, C.M.; Grasberger, B.; Kranz, J.K.; Lewandowski, F.; Liu, L.; Ma, H.; Maguire, D.; Macielag, M.J.; McDonnell, M.E.; Mezzasalma Haarlander, T.; Miller, R.; Milligan, C.; R, R.e.
Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 A resolution
Protein Sci.
20
670-683
2011
Homo sapiens (Q99685), Homo sapiens
Karageorgos, I.; Wales, T.E.; Janero, D.R.; Zvonok, N.; Vemuri, V.K.; Engen, J.R.; Makriyannis, A.
Active-site inhibitors modulate the dynamic properties of human monoacylglycerol lipase: a hydrogen exchange mass spectrometry study
Biochemistry
52
5016-5026
2013
Homo sapiens
Afzal, O.; Kumar, S.; Kumar, R.; Firoz, A.; Jaggi, M.; Bawa, S.
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors
Bioorg. Med. Chem. Lett.
24
3986-3996
2014
Homo sapiens (Q99685), Homo sapiens
Li, C.; Vilches-Flores, A.; Zhao, M.; Amiel, S.A.; Jones, P.M.; Persaud, S.J.
Expression and function of monoacylglycerol lipase in mouse beta-cells and human islets of Langerhans
Cell. Physiol. Biochem.
30
347-358
2012
Homo sapiens, Mus musculus
Laitinen, T.; Navia-Paldanius, D.; Rytilahti, R.; Marjamaa, J.J.; Ka?izkova, J.; Parkkari, T.; Pantsar, T.; Poso, A.; Laitinen, J.T.; Savinainen, J.R.
Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency
Mol. Pharmacol.
85
510-519
2014
Homo sapiens
Savinainen, J.R.; Kansanen, E.; Pantsar, T.; Navia-Paldanius, D.; Parkkari, T.; Lehtonen, M.; Laitinen, T.; Nevalainen, T.; Poso, A.; Levonen, A.L.; Laitinen, J.T.
Robust hydrolysis of prostaglandin glycerol esters by human monoacylglycerol lipase (MAGL)
Mol. Pharmacol.
86
522-535
2014
Homo sapiens (Q99685), Homo sapiens
Chen, H.; Tian, R.; Ni, Z.; Zhang, Z.; Chen, H.; Guo, Q.; Saier, M.H.
Conformational transition pathway in the inhibitor binding process of human monoacylglycerol lipase
Protein J.
33
503-511
2014
Homo sapiens
Lauria, S.; Casati, S.; Ciuffreda, P.
Synthesis and characterization of a new fluorogenic substrate for monoacylglycerol lipase and application to inhibition studies
Anal. Bioanal. Chem.
407
8163-8167
2015
Homo sapiens (Q99685), Homo sapiens
Kim, R.; Suh, M.
The GxSxG motif of Arabidopsis monoacylglycerol lipase (MAGL6 and MAGL8) is essential for their enzyme activities
Appl. Biol. Chem.
59
833-840
2016
Arabidopsis thaliana (O49284), Arabidopsis thaliana (O80959), Arabidopsis thaliana (Q8H133), Homo sapiens (Q99685)
-
De Leo, M.; Huallpa, C.G.; Alvarado, B.; Granchi, C.; Poli, G.; De Tommasi, N.; Braca, A.
New diterpenes from Salvia pseudorosmarinus and their activity as inhibitors of monoacylglycerol lipase (MAGL)
Fitoterapia
130
251-258
2018
Homo sapiens (Q99685)
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
J. Biol. Chem.
291
2556-2565
2016
Homo sapiens (Q99685), Homo sapiens
Xiang, W.; Shi, R.; Kang, X.; Zhang, X.; Chen, P.; Zhang, L.; Hou, A.; Wang, R.; Zhao, Y.; Zhao, K.; Liu, Y.; Ma, Y.; Luo, H.; Shang, S.; Zhang, J.; He, F.; Yu, S.; Gan, L.; Shi, C.; Li, Y.; Yang, W.; Liang, H.; Miao, H.
Monoacylglycerol lipase regulates cannabinoid receptor 2-dependent macrophage activation and cancer progression
Nat. Commun.
9
2574
2018
Mus musculus (O35678), Homo sapiens (Q99685), Homo sapiens