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αβ-Hydrolase 6

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Target id: 2919

Nomenclature: αβ-Hydrolase 6

Abbreviated Name: ABHD6

Family: 2-Acylglycerol ester turnover

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 337 3p14.3 ABHD6 abhydrolase domain containing 6, acylglycerol lipase
Mouse 1 336 14 A1 Abhd6 abhydrolase domain containing 6
Rat 1 337 15p14 Abhd6 abhydrolase domain containing 6, acylglycerol lipase
Previous and Unofficial Names Click here for help
2-arachidonoylglycerol hydrolase | abhydrolase domain-containing protein 6 | alpha/beta-Hydrolase domain containing 6 | abhydrolase domain containing 6 | abhydrolase domain containing 6, acylglycerol lipase
Database Links Click here for help
Alphafold Q9BV23 (Hs), Q8R2Y0 (Mm), Q5XI64 (Rn)
BRENDA 3.1.1.23
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL2189127 (Hs), CHEMBL5010 (Mm), CHEMBL3708569 (Rn)
Ensembl Gene ENSG00000163686 (Hs), ENSMUSG00000025277 (Mm), ENSRNOG00000008167 (Rn)
Entrez Gene 57406 (Hs), 66082 (Mm), 305795 (Rn)
Human Protein Atlas ENSG00000163686 (Hs)
KEGG Enzyme 3.1.1.23
KEGG Gene hsa:57406 (Hs), mmu:66082 (Mm), rno:305795 (Rn)
OMIM 616966 (Hs)
Pharos Q9BV23 (Hs)
UniProtKB Q9BV23 (Hs), Q8R2Y0 (Mm), Q5XI64 (Rn)
Wikipedia ABHD6 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.1.1.23
Endogenous substrates
1-arachidonoylglycerol > 2-arachidonoylglycerol > 1-oleoylglycerol > 2-oleoyl glycerol  [6]

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
KT-109 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.8 pIC50 4
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [4]
WWL70 Small molecule or natural product Hs Inhibition 7.2 pIC50 5
⤷ pIC50 7.2 [5]
WWL123 Small molecule or natural product Hs Inhibition 6.4 pIC50 1
⤷ pIC50 6.4 [1]
SA-57 Small molecule or natural product Click here for species-specific activity table Mm Inhibition 6.2 pIC50 7
⤷ pIC50 6.2 (IC50 6.5x10-7 M) [7]
ABD-1970 Small molecule or natural product Click here for species-specific activity table Rn Inhibition 6.1 pIC50 3
⤷ pIC50 6.1 (IC50 8x10-7 M) [3]
ABX-1431 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.6 pIC50 2
⤷ pIC50 5.6 (IC50 2.7x10-6 M) [2]
ABD-1970 Small molecule or natural product Click here for species-specific activity table Mm Inhibition 5.5 pIC50 3
⤷ pIC50 5.5 (IC50 3.2x10-6 M) [3]
View species-specific inhibitor tables

References

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1. Bachovchin DA, Ji T, Li W, Simon GM, Blankman JL, Adibekian A, Hoover H, Niessen S, Cravatt BF. (2010) Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening. Proc Natl Acad Sci USA, 107 (49): 20941-6. [PMID:21084632]

2. Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, Alexander JP, Jones TK, Ezekowitz RAB, O'Neill GP et al.. (2018) Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem, 61 (20): 9062-9084. [PMID:30067909]

3. Clapper JR, Henry CL, Niphakis MJ, Knize AM, Coppola AR, Simon GM, Ngo N, Herbst RA, Herbst DM, Reed AW et al.. (2018) Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators. J Pharmacol Exp Ther, 367 (3): 494-508. [PMID:30305428]

4. Hsu KL, Tsuboi K, Adibekian A, Pugh H, Masuda K, Cravatt BF. (2012) DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat Chem Biol, 8 (12): 999-1007. [PMID:23103940]

5. Li W, Blankman JL, Cravatt BF. (2007) A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases. J Am Chem Soc, 129 (31): 9594-5. [PMID:17629278]

6. Navia-Paldanius D, Savinainen JR, Laitinen JT. (2012) Biochemical and pharmacological characterization of human α/β-hydrolase domain containing 6 (ABHD6) and 12 (ABHD12). J Lipid Res, 53 (11): 2413-24. [PMID:22969151]

7. Niphakis MJ, Johnson DS, Ballard TE, Stiff C, Cravatt BF. (2012) O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci, 3 (5): 418-26. [PMID:22860211]

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