Results 21 to 30 of about 125,969 (167)

A Highly Selective and Versatile Probe Platform for Visualization of Monoacylglycerol Lipase. [PDF]

Angew Chem Int Ed Engl
Hentsch A, Guberman M, Radetzki S, Kaushik S, Huizenga M, Paul J, Schippers M, Benz J, Kuhn B, Heer D, Topp A, Esteves Gloria L, Walter A, Hochstrasser R, Wittwer MB, von Kries JP, Collin L, Blaising J, van der Stelt M, Lipstein N, Grether U, Nazaré M.   +21 more
europepmc   +2 more sources

Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors.

European journal of medicinal chemistry, 2023
The degradation of the endocannabinoid 2-arachidonoylglycerol is mediated by the enzyme monoacylglycerol lipase (MAGL), thus generating arachidonic acid, the precursor of prostaglandins and other pro-inflammatory mediators.
Miriana Di Stefano, Samuele Masoni, Giulia Bononi, G. Poli, Salvatore Galati, F. Gado, Simone Manzi, C. Vagaggini, A. Brai, I. Caligiuri, Kanwal Asif, F. Rizzolio, M. Macchia, A. Chicca, Andrea Sodi, V. Di Bussolo, F. Minutolo, Philip Meier, J. Gertsch, C. Granchi, E. Dreassi, T. Tuccinardi   +21 more
semanticscholar   +1 more source

Monoacylglycerol Lipase Inhibition in Tourette Syndrome: A 12‐Week, Randomized, Controlled Study

Movement Disorders, 2021
Modulation of the endocannabinoid system via monoacylglycerol lipase inhibition with Lu AG06466 (formerly known as ABX‐1431) has previously been shown to reduce tics in patients with Tourette syndrome.
K. Müller-Vahl, C. Fremer, Chan Beals, J. Ivković, H. Loft, Christoph Schindler   +5 more
semanticscholar   +1 more source

The NADPH oxidase NOX4 regulates redox and metabolic homeostasis preventing HCC progression

Hepatology, EarlyView., 2022
Loss of NOX4 in HCC tumor cells induces metabolic reprogramming in a Nrf2/MYC‐dependent manner to promote HCC progression. Abstract Background and Aims The NADPH oxidase NOX4 plays a tumor‐suppressor function in HCC. Silencing NOX4 confers higher proliferative and migratory capacity to HCC cells and increases their in vivo tumorigenic potential in ...
Irene Peñuelas‐Haro, Rut Espinosa‐Sotelo, Eva Crosas‐Molist, Macarena Herranz‐Itúrbide, Daniel Caballero‐Díaz, Ania Alay, Xavier Solé, Emilio Ramos, Teresa Serrano, María L. Martínez‐Chantar, Ulla G. Knaus, José M. Cuezva, Antonio Zorzano, Esther Bertran, Isabel Fabregat   +14 more
wiley   +1 more source

Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold. [PDF]

J Med Chem, 2021
Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system.
Rong J, Mori W, Xia X, Schafroth MA, Zhao C, Van RS, Yamasaki T, Chen J, Xiao Z, Haider A, Ogasawara D, Hiraishi A, Shao T, Zhang Y, Chen Z, Pang F, Hu K, Hu K, Xie L, Fujinaga M, Kumata K, Gou Y, Fang Y, Gu S, Wei H, Bao L, Xu H, Collier TL, Shao Y, Carson RE, Cravatt BF, Wang L, Zhang MR, Liang SH.   +33 more
europepmc   +2 more sources

Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety.

Journal of Medicinal Chemistry, 2021
The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability of reversible-type inhibitor is still limited to clarify the pharmacological ...
Shuhei Ikeda, H. Sugiyama, Hidekazu Tokuhara, M. Murakami, Minoru Nakamura, Yuya Oguro, Jumpei Aida, N. Morishita, S. Sogabe, D. Dougan, S. Gay, L. Qin, N. Arimura, Yasuko Takahashi, Masako Sasaki, Y. Kamada, Kazunobu Aoyama, Kouya Kimoto, M. Kamata   +18 more
semanticscholar   +1 more source

The Monoacylglycerol Lipase Inhibitor JZL184 Inhibits Lung Cancer Cell Invasion and Metastasis via the CB1 Cannabinoid Receptor

Molecular Cancer Therapeutics, 2021
A targeted modulation of the endocannabinoid system is currently discussed as a promising strategy for cancer treatment. An important enzyme for the endocannabinoid metabolism is the monoacylglycerol lipase (MAGL), which catalyzes the degradation of 2 ...
J. Prüser, R. Ramer, Felix Wittig, I. Ivanov, J. Merkord, B. Hinz   +5 more
semanticscholar   +1 more source

Potential of Fatty Acid Amide Hydrolase (FAAH), Monoacylglycerol Lipase (MAGL), and Diacylglycerol Lipase (DAGL) Enzymes as Targets for Obesity Treatment: A Narrative Review

Pharmaceuticals, 2021
The endocannabinoid system (ECS) plays an integral role in maintaining metabolic homeostasis and may affect hunger, caloric intake, and nutrient absorption.
Justin Matheson, Xinxin Zhou, Zoe Bourgault, B. Le Foll   +3 more
semanticscholar   +1 more source

Endocannabinoid Modulation Using Monoacylglycerol Lipase Inhibition in Tourette Syndrome: A Phase 1 Randomized, Placebo-Controlled Study

Pharmacopsychiatry, 2021
Introduction Tourette syndrome (TS) is a complex neurodevelopmental disorder characterized by chronic motor and vocal tics. While consistently effective treatment is lacking, evidence indicates that the modulation of endocannabinoid system is potentially
K. Müller-Vahl, C. Fremer, Chan Beals, J. Ivković, H. Loft, Christoph Schindler   +5 more
semanticscholar   +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.
F. Pavón, I. Polis, D. Stouffer, B. Cravatt, M. Roberto, R. Martin‐Fardon, F. Rodríguez de Fonseca, L. Parsons, A. Serrano   +8 more
semanticscholar   +1 more source