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- | Journal: The role of monoglyceride lipase gene in promoting proliferation, metastasis, and free fatty acid accumulation in uveal melanoma cells. (Pubmed Central) - Oct 9, 2024
Additionally, MGLL modulated free fatty acid (FFA) levels within these cells. Our findings reveal MGLL as a crucial player in uveal melanoma progression and propose it as a novel therapeutic target, potentially leading to improved management and outcomes for patients with this disease.
- | Journal: The Interplay among Glucocorticoid Therapy, Platelet-Activating Factor and Endocannabinoid Release Influences the Inflammatory Response to COVID-19. (Pubmed Central) - Mar 1, 2023
Corroborating this, transcriptome analysis of GC-treated patients blood leukocytes showed differential modulation of monoacylglycerol lipase and phospholipase A2 gene expression. Altogether, these findings offer a breakthrough in our understanding of COVID-19 pathophysiology, indicating that GCs may promote additional protective pharmacological effects by influencing the eCB and PAF pathways involved in the disease course.
- Endocannabinoid signaling from hypothalamic neurons enhances subventricular zone neural stem cell differentiation () - Jun 16, 2022 - Abstract #CANACN2022CAN_ACN_267;
Furthermore, we report similar observations in a germline Mgll knockout model, suggesting that neuronal Mgll dominates Mgll-mediated signaling in the SVZ. Taken together, these findings provide a holistic understanding of how Mgll regulates neurogenesis in vivo.
- || Lu AG06466 / Lundbeck
Clinical, P1 data: Endocannabinoid Modulation Using Monoacylglycerol Lipase Inhibition in Tourette Syndrome: A Phase 1 Randomized, Placebo-Controlled Study. (Pubmed Central) - May 19, 2022
Taken together, these findings provide a holistic understanding of how Mgll regulates neurogenesis in vivo. In this exploratory trial, a single dose of Lu AG06466 showed statistically significant positive effects on key measures of TS symptoms.
- | Journal: Novel Aminocyclobutanes as Monoacylglycerol Lipase Modulators. (Pubmed Central) - Feb 19, 2022
In this exploratory trial, a single dose of Lu AG06466 showed statistically significant positive effects on key measures of TS symptoms. No abstract available
- | Journal: Monoacylglycerol lipase (MAGL) inhibitors based on a diphenylsulfide-benzoylpiperidine scaffold. (Pubmed Central) - Oct 14, 2021
In this context, we developed new diphenylsulfide-benzoylpiperidine derivatives characterized by a high enzymatic MAGL inhibition activity in the low nanomolar range, a reversible mechanism of action and selectivity. The three most active compounds (15-17) induced an appreciable inhibition of cell viability in a panel of nine cancer cell lines, with IC values ranging between 0.32 and 10 μM, thus highlighting their potential as novel anticancer agents.
- [VIRTUAL] Long-range hypothalamic neuronal projections to the subventricular zone neurogenic niche regulates neural stem cell function through endocannabinoid signaling () - Sep 10, 2021 - Abstract #CANACN2021CAN_ACN_392;
Intriguingly, specific removal of Mgll expression in ARC neurons using virally transfected Cre recombinase in Mgll-floxed mice resulted in a decrease of SVZ NPCs in this microdomain and a subsequent reduction of proliferating cells in this microdomain. These findings provide an understanding of how longrange neuronal Mgll activity regulates adult SVZ NPC function in a microdomain-specific Fashion.
- | Journal: A New Ultrasensitive Bioluminescence-Based Method for Assaying Monoacylglycerol Lipase. (Pubmed Central) - Jul 28, 2021
The assay was validated for the identification and characterization of MAGL modulators using the well-known MAGL inhibitor JZL184. The use of PLG2 displaying distinct bioluminescence color and kinetics may offer a highly desirable opportunity to extend the range of applications to cell-based assays.
- | Journal: Set-Up and Validation of a High Throughput Screening Method for Human Monoacylglycerol Lipase (MAGL) Based on a New Red Fluorescent Probe. (Pubmed Central) - Dec 6, 2019
The assay was highly reproducible with an overall average Z' value of 0.86. The fast, sensitive and accurate method described in this study is suitable for low-cost high-throughput screening (HTS) of MAGL modulators and is a powerful new tool for studying MAGL activity.