Results 21 to 30 of about 3,186 (156)

Discovering monoacylglycerol lipase inhibitors by a combination of fluorogenic substrate assay and activity-based protein profiling

Frontiers in Pharmacology, 2022
The endocannabinoid 2-arachidonoylglycerol (2-AG) is predominantly metabolized by monoacylglycerol lipase (MAGL) in the brain. Selective inhibitors of MAGL provide valuable insights into the role of 2-AG in a variety of (patho)physiological processes and
Hui Deng, Hui Deng, Qianwen Zhang, Qian Lei, Qian Lei, Na Yang, Na Yang, Kai Yang, Jianbing Jiang, Zhiyi Yu   +9 more
doaj   +1 more source

Unraveling Endocannabinoid Signaling Pathways in Cisplatin-Induced Ototoxicity. [PDF]

FASEB J
We performed a comprehensive molecular profiling of the endocannabinoid (eCB) system (ECS) in an auditory Hair cell (HC)‐like cell line (1). Afterwards, we developed suitable in vitro and in vivo models of cisplatin‐induced ototoxicity where we identified distinct components of the ECS (CB2R, DAGLβ and ABHD6) as molecular targets of the drug (2 ...
Palaniappan S, Tisi A, Di Meo C, Urbano C, Fenton GE, Della Valle F, Fanti F, Compagnone D, Nazarè M, Versnel H, Aramini A, Allegretti M, Maccarrone M.   +12 more
europepmc   +2 more sources

Monoacylglycerol lipase reprograms hepatocytes and macrophages to promote liver regeneration

JHEP Reports, 2023
Background & Aims: Liver regeneration is a repair process in which metabolic reprogramming of parenchymal and inflammatory cells plays a major role. Monoacylglycerol lipase (MAGL) is an ubiquitous enzyme at the crossroad between lipid metabolism and ...
Manon Allaire, Rola Al Sayegh, Morgane Mabire, Adel Hammoutene, Matthieu Siebert, Charles Caër, Mathilde Cadoux, JingHong Wan, Aida Habib, Maude Le Gall, Pierre de la Grange, Hervé Guillou, Catherine Postic, Valérie Paradis, Sophie Lotersztajn, Hélène Gilgenkrantz   +15 more
doaj   +1 more source

A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence

Nature Communications, 2023
Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is limited by central nervous system (CNS)-mediated side effects ...
Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, Mario van der Stelt   +28 more
doaj   +1 more source

S1P₃ Receptor Mediates the Proinflammatory Effect of the Endocannabinoid 2-Arachidonoylglycerol in Endometriotic Epithelial Cells. [PDF]

FASEB J
The endocannabinoid 2‐arachidonoylglycerol (2‐AG) induced a marked inflammatory response in human endometriotic epithelial cells. A functional cross talk between the signaling pathways of 2‐AG and the bioactive sphingolipid sphingosine 1‐phosphate (S1P) has been identified here in endometriosis.
Raeispour M, Prisinzano M, Seidita I, Romeo L, Nardi E, Castiglione F, Bruni P, Petraglia F, Bernacchioni C, Donati C.   +9 more
europepmc   +2 more sources

Selective inhibition of monoacylglycerol lipase is associated with passive coping behavior and attenuation of stress-induced dopamine release in the medial prefrontal cortex

Neurobiology of Stress, 2021
The endocannabinoid system is involved in the regulation of the stress response, but the relative contribution of N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) and their mechanisms have to be elucidated.
Francisco Javier Pavón, Ilham Y. Polis, David G. Stouffer, Benjamin F. Cravatt, Marisa Roberto, Rémi Martin-Fardon, Fernando Rodríguez de Fonseca, Loren H. Parsons, Antonia Serrano   +8 more
doaj   +1 more source

Gift of the MAGL [PDF]

Science-Business eXchange, 2009
A team at Scripps has developed a compound that should help tease out whether the endocannabinoid-degrading enzyme MAGL is a better pain target than the closely related enzyme FAAH. The answer could enable the design of better cannabinoid receptor agonist–based analgesics.
openaire   +1 more source

Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2017
Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol. A wide number of MAGL inhibitors are reported in literature; however, many of them are characterised ...
Carlotta Granchi, Isabella Caligiuri, Eleonora Bertelli, Giulio Poli, Flavio Rizzolio, Marco Macchia, Adriano Martinelli, Filippo Minutolo, Tiziano Tuccinardi   +8 more
doaj   +1 more source

Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Monoacylglycerol lipase (MAGL) is an attractive therapeutic target for many pathologies, including neurodegenerative diseases, cancer as well as chronic pain and inflammatory pathologies.
Giulio Poli, Margherita Lapillo, Vibhu Jha, Nayla Mouawad, Isabella Caligiuri, Marco Macchia, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi, Carlotta Granchi   +9 more
doaj   +1 more source

Monoacylglycerol Lipase Regulates Fever Response. [PDF]

PLoS ONE, 2015
Cyclooxygenase inhibitors such as ibuprofen have been used for decades to control fever through reducing the levels of the pyrogenic lipid transmitter prostaglandin E2 (PGE2).
Manuel Sanchez-Alavez, William Nguyen, Simone Mori, Gianluca Moroncini, Andreu Viader, Daniel K Nomura, Benjamin F Cravatt, Bruno Conti   +7 more
doaj   +1 more source