αβ-Hydrolase 6 | 2-Acylglycerol ester turnover | IUPHAR/BPS Guide to PHARMACOLOGY

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αβ-Hydrolase 6

Target not currently curated in GtoImmuPdb

Target id: 2919

Nomenclature: αβ-Hydrolase 6

Abbreviated Name: ABHD6

Family: 2-Acylglycerol ester turnover

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ABHD6 abhydrolase domain containing 6, acylglycerol lipase
Mouse - - Abhd6 abhydrolase domain containing 6
Rat - - Abhd6 abhydrolase domain containing 6
Previous and Unofficial Names
2-arachidonoylglycerol hydrolase | abhydrolase domain-containing protein 6 | alpha/beta-Hydrolase domain containing 6 | abhydrolase domain containing 6
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.1.23
Endogenous substrates
1-arachidonoylglycerol > 2-arachidonoylglycerol > 1-oleoylglycerol > 2-oleoyl glycerol  [5]

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 Value Parameter Reference
KT-109 Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.6x10-8 M) [3]
WWL70 Hs Inhibition 7.2 pIC50 4
pIC50 7.2 [4]
WWL123 Hs Inhibition 6.4 pIC50 1
pIC50 6.4 [1]
ABX-1431 Hs Inhibition 5.6 pIC50 2
pIC50 5.6 (IC50 2.7x10-6 M) [2]

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. U.S.A., 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. 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]

4. 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]

5. 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]

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