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DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses
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The endocannabinoid 2-arachidonoylglycerol (2-AG) is biosynthesized by diacylglycerol lipases DAGLα and DAGLβ. Chemical probes to perturb DAGLs are needed to characterize endocannabinoid function in biological processes. Here we report a series of 1,2,3-triazole urea inhibitors, along with paired negative-control and activity-based probes, for the functional analysis of DAGLβ in living systems. Optimized inhibitors showed high selectivity for DAGLβ over other serine hydrolases, including DAGLα (∼60-fold selectivity), and the limited off-targets, such as ABHD6, were also inhibited by the negative-control probe. Using these agents and Daglb(-/-) mice, we show that DAGLβ inactivation lowers 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages in a manner that is distinct and complementary to disruption of cytosolic phospholipase-A2. We observed a corresponding reduction in lipopolysaccharide-induced tumor necrosis factor-α release. These findings indicate that DAGLβ is a key metabolic hub within a lipid network that regulates proinflammatory responses in macrophages.
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“Importantly, DAGL-β inhibition also blocks the LPS-induced production of proinflammatory mediators (Hsu et al, 2012).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Hsu et al, 2012
In the citing paper
“Specifically, DAGL-β is highly expressed in macrophages, and its blockade leads to reduced levels of 2-AG, arachidonic acid, and a variety of proinflammatory arachidonic acid metabolites and proinflammatory cytokines in these cells (Hsu et al, 2012).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Hsu et al, 2012
In the citing paper
“The observation that selective inhibition of DAGL-β, the biosynthetic enzyme expressed predominantly on macrophages and microglia, reduces pro-inflammatory mediators (Hsu et al, 2012), and reverses nociceptive behavior in a mouse model of CCI (Wilkerson et al, 2016a) appears to be at odds with the antinociceptive effects of MAGL inhibitors in this same model.”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Hsu et al, 2012
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Metadata
- Authors
- Hsu, K.-L., Tsuboi, K., Adibekian, A., Pugh, H., Masuda, K., & Cravatt, B. F.
- Affiliations
- Scripps Research Institute (US)
- Corresponding author
- Cravatt, Benjamin F
- Venue
- Nature Chemical Biology
- Published
- 2012-10-28
- Volume
- 8
- Issue
- 12
- Pages
- 999-1007
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- PMC
- PMC3513945
- OpenAlex
- W2134450626
- Cited by
- 222
- References
- 51
- Citations by year
- 2026: 14 · 2025: 7 · 2024: 11 · 2023: 17 · 2022: 17 · 2021: 22 · 2020: 13 · 2019: 15 · 2018: 17 · 2017: 15 · 2016: 22 · 2015: 18 · 2014: 18 · 2013: 15 · 2012: 1
- FWCI
- 12.45
- Type
- journal article
- Language
- en
- Open access
- green
- europepmc.org
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature Chemical Biology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Mental Health (U54MH084512, MH-084512)
- National Institute on Drug Abuse (DA033760, P01DA009789, R01DA033760, DA 009789)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Eicosanoids and Hypertension Pharmacology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Lipid metabolism and biosynthesis
- Keywords
- diacylglycerol lipase, 2-arachidonoylglycerol, endocannabinoid system, activity-based probes, macrophage inflammation, eicosanoids, arachidonic acid, cytosolic phospholipase A2, lipopolysaccharide, TNF-α, lipid metabolism, ABHD6
- MeSH terms
- Animals, Arachidonic Acids, Cell Line, Glycerides, Inflammation, Lipoprotein Lipase, Neurons, Prostaglandins, Triazoles, Tumor Necrosis Factor-alpha, Signal Transduction, Cytokines, Arachidonic Acid, Macrophages, Peritoneal, Mice, Knockout, Protein Isoforms, Proteome, Quantitative Structure-Activity Relationship, Lipid Metabolism, Mice, Drug Discovery, Endocannabinoids
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