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diacylglycerol lipase β

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Target id: 1397

Nomenclature: diacylglycerol lipase β

Abbreviated Name: DAGLβ

Family: Hydrolases & Lipases, 2-Acylglycerol ester turnover

Contents:

Gene and Protein Information Click here for help
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 12p11 Daglb diacylglycerol lipase, beta
Previous and Unofficial Names Click here for help
diacylglycerol lipase | diacylglycerol lipase, beta | KCCR13L | neural stem cell-derived dendrite regulator | NSDDR
Database Links Click here for help
Alphafold Q8NCG7 (Hs), Q91WC9 (Mm), P0C1S9 (Rn)
BRENDA 3.1.1.-
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL5521 (Hs), CHEMBL5656 (Mm)
Ensembl Gene ENSG00000164535 (Hs), ENSMUSG00000039206 (Mm), ENSRNOG00000001079 (Rn)
Entrez Gene 221955 (Hs), 231871 (Mm), 304289 (Rn)
Human Protein Atlas ENSG00000164535 (Hs)
KEGG Enzyme 3.1.1.-
KEGG Gene hsa:221955 (Hs), mmu:231871 (Mm), rno:304289 (Rn)
OMIM 614016 (Hs)
Pharos Q8NCG7 (Hs)
RefSeq Nucleotide NM_001142936 (Hs), NM_144915 (Mm), NM_001107120 (Rn)
RefSeq Protein NP_001136408 (Hs), NP_659164 (Mm), NP_001100590 (Rn)
UniProtKB Q8NCG7 (Hs), Q91WC9 (Mm), P0C1S9 (Rn)
Wikipedia DAGLB (Hs)
Enzyme Reaction Click here for help
EC Number: 3.1.1.-
Endogenous substrates
diacylglycerol

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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
DH376 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 4
⤷ pIC50 8.6 [4]
DO34 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 4
⤷ pIC50 8.1 [4]
LEI105 Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand 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 Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.0 pIC50 2
⤷ pIC50 7.0 (IC50 1x10-7 M) [2]
RHC80267 Small molecule or natural product Click here for species-specific activity table Hs Inhibition - -
⤷

References

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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) DAGLβ 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 USA, 113 (1): 26-33. [PMID:26668358]

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