Monoacylglycerol lipase

Target id: 1399

Nomenclature: Monoacylglycerol lipase

Abbreviated Name: MAGL

Family: S33: Prolyl aminopeptidase, Hydrolases, 2-Acylglycerol ester turnover

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Monoacylglycerol lipase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 303 p13-q13.33 MGLL monoglyceride lipase
Mouse - 319 6 D1 Mgll monoglyceride lipase
Rat - 303 4q34 Mgll monoglyceride lipase
Previous and Unofficial Names
HU-K5 | MGL | MAGL | monoacylglycerol lipase
Database Links
Specialist databases
MEROPS S33.980 (Hs)
Other databases
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.1.23
Endogenous substrates (Human)
2-oleoyl glycerol = 2-arachidonoylglycerol >> anandamide  [3]

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
JJKK 048 Hs Inhibition 9.3 pIC50 1
pIC50 9.3 [1]
KML29 Hs Inhibition 8.5 pIC50 2
pIC50 8.5 [2]
JZL184 Hs Irreversible inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 3.9x10-9 M) [2]
JZL195 Hs Inhibition 8.4 pIC50 4
pIC50 8.4 (IC50 4x10-9 M) [4]
Description: in vitro assay

References

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1. Aaltonen N, Savinainen JR, Ribas CR, Rönkkö J, Kuusisto A, Korhonen J, Navia-Paldanius D, Häyrinen J, Takabe P, Käsnänen H et al.. (2013) Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem. Biol.20 (3): 379-90. [PMID:23521796]

2. Chang JW, Niphakis MJ, Lum KM, Cognetta 3rd AB, Wang C, Matthews ML, Niessen S, Buczynski MW, Parsons LH, Cravatt BF. (2012) Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem. Biol.19 (5): 579-88. [PMID:22542104]

3. Ghafouri N, Tiger G, Razdan RK, Mahadevan A, Pertwee RG, Martin BR, Fowler CJ. (2004) Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol. Br. J. Pharmacol.143 (6): 774-84. [PMID:15492019]

4. Long JZ, Nomura DK, Vann RE, Walentiny DM, Booker L, Jin X, Burston JJ, Sim-Selley LJ, Lichtman AH, Wiley JL et al.. (2009) Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc. Natl. Acad. Sci. U.S.A.106 (48): 20270-5. [PMID:19918051]

How to cite this page

S33: Prolyl aminopeptidase: Monoacylglycerol lipase. Last modified on 07/03/2017. Accessed on 15/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1399.