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Target id: 1396
Nomenclature: diacylglycerol lipase α
Abbreviated Name: DAGLα
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 4 | 1042 | 11q12.2 | DAGLA | diacylglycerol lipase alpha | |
Mouse | 4 | 1044 | 19 A | Dagla | diacylglycerol lipase, alpha | |
Rat | 4 | 1044 | 1q43 | Dagla | diacylglycerol lipase, alpha |
Previous and Unofficial Names |
diacylglycerol lipase | diacylglycerol lipase, alpha | FMP30 | Neural stem cell-derived dendrite regulator |
Database Links | |
Alphafold | Q9Y4D2 (Hs), Q6WQJ1 (Mm), Q5YLM1 (Rn) |
BRENDA | 3.1.1.- |
CATH/Gene3D | 3.40.50.1820 |
ChEMBL Target | CHEMBL5545 (Hs), CHEMBL5180 (Mm), CHEMBL4523331 (Rn) |
Ensembl Gene | ENSG00000134780 (Hs), ENSMUSG00000035735 (Mm), ENSRNOG00000027264 (Rn) |
Entrez Gene | 747 (Hs), 269060 (Mm), 309207 (Rn) |
Human Protein Atlas | ENSG00000134780 (Hs) |
KEGG Enzyme | 3.1.1.- |
KEGG Gene | hsa:747 (Hs), mmu:269060 (Mm), rno:309207 (Rn) |
OMIM | 614015 (Hs) |
Pharos | Q9Y4D2 (Hs) |
RefSeq Nucleotide | NM_006133 (Hs), NM_198114 (Mm), NM_001005886 (Rn) |
RefSeq Protein | NP_006124 (Hs), NP_932782 (Mm), NP_001005886 (Rn) |
UniProtKB | Q9Y4D2 (Hs), Q6WQJ1 (Mm), Q5YLM1 (Rn) |
Wikipedia | DAGLA (Hs) |
Enzyme Reaction | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||
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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. Deng H, Kooijman S, van den Nieuwendijk AM, Ogasawara D, van der Wel T, van Dalen F, Baggelaar MP, Janssen FJ, van den Berg RJ, den Dulk H et al.. (2017) Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. J Med Chem, 60 (1): 428-440. [PMID:27992221]
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. Johnston M, Bhatt SR, Sikka S, Mercier RW, West JM, Makriyannis A, Gatley SJ, Duclos Jr RI. (2012) Assay and inhibition of diacylglycerol lipase activity. Bioorg Med Chem Lett, 22 (14): 4585-92. [PMID:22738638]
6. Knight MA, Hernandez D, Diede SJ, Dauwerse HG, Rafferty I, van de Leemput J, Forrest SM, Gardner RJ, Storey E, van Ommen GJ et al.. (2008) A duplication at chromosome 11q12.2-11q12.3 is associated with spinocerebellar ataxia type 20. Hum Mol Genet, 17 (24): 3847-53. [PMID:18801880]
7. 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]