Results 31 to 40 of about 4,187 (189)

Monoacylglycerol lipase promotes progression of hepatocellular carcinoma via NF-κB-mediated epithelial-mesenchymal transition

Journal of Hematology & Oncology, 2016
Background Monoacylglycerol lipase (MAGL), a critical lipolytic enzyme, has emerged as a key regulator of tumor progression, yet its biological function and clinical significance in hepatocellular carcinoma (HCC) is still unknown.
Weiping Zhu, Yiming Zhao, Jiamin Zhou, Xin Wang, Qi Pan, Ning Zhang, Longrong Wang, Miao Wang, Dihua Zhan, Zeyang Liu, Xigan He, Dening Ma, Shuang Liu, Lu Wang   +13 more
doaj   +1 more source

Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor [PDF]

, 2019
Monoacylglycerol lipase (MAGL) is the enzyme degrading the endocannabinoid 2-arachidonoylglycerol, and it is involved in several physiological and pathological processes.
Carlotta Granchi (1375599), Granchi, Carlotta, El Boustani, Maguie, Cristina Licari (6319949), Margherita Lapillo (2931531), Tiziano Tuccinardi (409135), Minutolo, Filippo, Gertsch, Jürg, Giulio Poli (809754), Poli, Giulio, Sandra Glasmacher (6319943), Andrea Chicca (710770), Macchia, Marco, Glasmacher, Sandra, Chicca, Andrea, Lapillo, Margherita, Isabella Caligiuri (285374), Bononi, Giulia, Giulia Bononi (6319946), Marco Macchia (409137), Filippo Minutolo (1343184), Jürg Gertsch (1589107), Flavio Rizzolio (74629), Tuccinardi, Tiziano, Rizzolio, Flavio, Caligiuri, Isabella, Maguie el Boustani (6319952), Licari, Cristina   +27 more
core   +1 more source

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

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

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 potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature

PLOS ONE, 2022
ABSTRACT Chronic inflammation and blood–brain barrier dysfunction are key pathological hallmarks of neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease. Major drivers of these pathologies include pro-inflammatory stimuli such as prostaglandins, which are produced in the ...
Alicia M. Kemble, Benoit Hornsperger, Iris Ruf, Hans Richter, Jörg Benz, Bernd Kuhn, Dominik Heer, Matthias Wittwer, Britta Engelhardt, Uwe Grether, Ludovic Collin   +10 more
openaire   +3 more sources

Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors [PDF]

, 2018
Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays an important role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol, which is implicated in many physiological processes.
De Stefano L., Manera, Clementina, Rizzolio F., Margherita Lapillo, Gertsch, Jürg, Tuccinardi T., Baraldi, Stefania, Martinelli, Adriano, Filippo Minutolo, Macchia, Marco, De Stefano, Lucia, Lorenzo Di Cesare Mannelli, Carlotta Granchi, Stefania Baraldi, Martinelli A., Flavio Rizzolio, Carla Ghelardini, Di Cesare Mannelli, Lorenzo, Di Cesare Mannelli L., Ruggiero, Emanuela, Rizzolio, Flavio, Andrea Chicca, Gertsch J., Macchia M., Mojgan Aghazadeh Tabrizi, Lapillo M., Baraldi S., Granchi, Carlotta, Marco Macchia, Baraldi, Pier Giovanni, Minutolo, Filippo, Clementina Manera, Granchi C., Ghelardini, C, Baraldi P. G., Jürg Gertsch, Aghazadeh Tabrizi M., Lucia De Stefano, Aghazadeh Tabrizi, Mojgan, Di Cesare Mannelli, L, Emanuela Ruggiero, Adriano Martinelli, Chicca, Andrea, Pier Giovanni Baraldi, Lapillo, Margherita, Manera C., Chicca A., Ghelardini C., Tuccinardi, Tiziano, Ghelardini, Carla, Ruggiero E., Tiziano Tuccinardi, Minutolo F.   +52 more
core   +1 more source

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

Of Mice and MAGL (Monoacylglycerol Lipase)

The FASEB Journal, 2011
About 18.8 million American adults suffer depressive disorders that may occur with anxiety and substance abuse. Tetrahydrocannabinol (THC), a compound in marijuana, is a cannabinoid chemical that binds to and activates cannabinoid receptors (CB1) in the pre‐synaptic cell membrane as part of neuron‐to‐neuron transmission in the ...
S. Bach, T. Bombinski, M. Daniels, D. Gross, T. Hogg, T. Martin, D. McMurray, E. Naber, N. Perez, A. Schulman, S. Tucker, S. Andera‐Cato, A. Arnold, A. Blumberg, M. Bord, A. Feiertag, M. Greaves, A. Her, E. Kennedy, C. Orozco, C. Rice, A. Rodgers, A. Sauer, J. Schubert, C. Tubbs, T. Wray, G. Vogt, L. Shrestha, C. Hillard   +28 more
openaire   +1 more source

MAGLi 432 blocks MAGL in human and mouse brain lysates in a selective and potent manner.

, 2022
(A) Chemical structure of MAGLi 432 with an IC50 = 4.2 nM in human MAGL as determined by enzymatic assays. (B) X-ray co-crystal structure of MAGLi 432 (cyan) with human MAGL (blue).
Dominik Heer (2169148), Matthias Wittwer (19991), Iris Ruf (13767197), Jörg Benz (13767200), Ludovic Collin (3437399), Benoit Hornsperger (1503058), Bernd Kuhn (260084), Alicia M. Kemble (8555517), Hans Richter (2364346), Britta Engelhardt (307404), Uwe Grether (1594096)   +10 more
core   +1 more source