Diacylglycerol lipase β | 2-Acylglycerol ester turnover | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

Diacylglycerol lipase β

Target not currently curated in GtoImmuPdb

Target id: 1397

Nomenclature: Diacylglycerol lipase β

Abbreviated Name: DAGLβ

Family: 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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 672 7p22.1 DAGLB diacylglycerol lipase beta
Mouse 4 669 5 G2 Daglb diacylglycerol lipase, beta
Rat 4 668 2p11 Daglb diacylglycerol lipase, beta
Previous and Unofficial Names
KCCR13L | NSDDR | neural stem cell-derived dendrite regulator | DGL-alpha | diacylglycerol lipase, alpha | sn1-specific diacylglycerol lipase alpha | diacylglycerol lipase, beta | diacylglycerol lipase
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.1.-
Endogenous substrates
diacylglycerol

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
DH376 Hs Inhibition 8.6 pIC50 4
pIC50 8.6 [4]
DO34 Hs Inhibition 8.1 pIC50 4
pIC50 8.1 [4]
LEI105 Hs Inhibition 8.1 pIC50 1
pIC50 8.1 [1]
Description: Inhibition of recombinant human DAGβ in a biochemical assay with para-nitrophenylbutyrate as a surrogate substrate.
KT-109 Hs Inhibition 7.1 – 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
Description: Determined by competitive ABPP using the HT-01 probe for inhibition of recombinant human DAGL-β
pIC50 7.1 (IC50 8.2x10-8 M) [3]
Description: As measured by LC-MS substrate assay.
orlistat Hs Inhibition 7.0 pIC50 2
pIC50 7.0 (IC50 1x10-7 M) [2]
RHC80267 Hs Inhibition - -

References

Show »

1. Baggelaar MP, Chameau PJ, Kantae V, Hummel J, Hsu KL, Janssen F, van der Wel T, Soethoudt M, Deng H, den Dulk H et al.. (2015) Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons. J. Am. Chem. Soc., 137 (27): 8851-7. [PMID:26083464]

2. Bisogno T, Howell F, Williams G, Minassi A, Cascio MG, Ligresti A, Matias I, Schiano-Moriello A, Paul P, Williams EJ et al.. (2003) Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain. J. Cell Biol., 163 (3): 463-8. [PMID:14610053]

3. Hsu KL, Tsuboi K, Adibekian A, Pugh H, Masuda K, Cravatt BF. (2012) DAGLĪ² inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat. Chem. Biol., 8 (12): 999-1007. [PMID:23103940]

4. Ogasawara D, Deng H, Viader A, Baggelaar MP, Breman A, den Dulk H, van den Nieuwendijk AM, van den Nieuwendijk AM, Soethoudt M, van der Wel T et al.. (2016) Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition. Proc. Natl. Acad. Sci. U.S.A., 113 (1): 26-33. [PMID:26668358]

Contributors

Show »

How to cite this page

Select citation format: