Results 11 to 20 of about 4,187 (189)

Discovery of Monoacylglycerol Lipase (MAGL) Inhibitors Based on a Pharmacophore-Guided Virtual Screening Study [PDF]

Molecules, 2020
Monoacylglycerol lipase (MAGL) is an important enzyme of the endocannabinoid system that catalyzes the degradation of the major endocannabinoid 2-arachidonoylglycerol (2-AG).
Vibhu Jha, Marzia Biagi, Valeria Spinelli, Miriana Di Stefano, Marco Macchia, Filippo Minutolo, Carlotta Granchi, Giulio Poli, Tiziano Tuccinardi   +8 more
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A New Age for MAGL

Chemistry & Biology, 2010
Monoacylglycerol lipase (MAGL) has been known for its participation in triacylglycerol breakdown and endocannabinoid deactivation. Now Nomura et al. show that cancer cells can hijack MAGL to produce oncogenic lipid messengers. This exciting finding raises important pathophysiological questions.
Guzmán, Manuel
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Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors [PDF]

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

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
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Pharmacological inhibition of MAGL attenuates experimental colon carcinogenesis [PDF]

Pharmacological Research, 2017
Colorectal cancer (CRC) is a major health problem in Western countries. The endocannabinoid 2-arachidonoyl-glycerol (2-AG) exerts antiproliferative actions in a number of tumoral cell lines, including CRC cells. Monoacylglycerol lipase (MAGL), a serine hydrolase that inactivates 2-AG, is highly expressed in aggressive human cancer cells.
PAGANO, ESTER, BORRELLI, FRANCESCA, Orlando, Pierangelo, ROMANO, BARBARA, Monti, Martina, Morbidelli, Lucia, Aviello, Gabriella, Imperatore, Roberta, CAPASSO, RAFFAELE, Piscitelli, Fabiana, Buono, Lorena, Di Marzo, Vincenzo, IZZO, ANGELO ANTONIO   +12 more
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Monoacylglycerol lipase (MAGL) inhibitors based on a diphenylsulfide-benzoylpiperidine scaffold

European Journal of Medicinal Chemistry, 2021
Monoacylglycerol lipase (MAGL) is an enzyme belonging to the endocannabinoid system that mainly metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG). Numerous studies have shown the involvement of this enzyme in various pathological conditions such as pain, cancer progression, Parkinson's and Alzheimer's disease, thus encouraging the ...
Bononi G., Tonarini G., Poli G., Barravecchia I., Caligiuri I., Macchia M., Rizzolio F., Demontis G. C. A. G., Minutolo F., Granchi C., Tuccinardi T.   +10 more
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Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors [PDF]

European Journal of Medicinal Chemistry, 2018
Monoacylglycerol lipase (MAGL) is the enzyme hydrolyzing the endocannabinoid 2-arachidonoylglycerol (2-AG) to free arachidonic acid and glycerol. Therefore, MAGL is implicated in many physiological processes involving the regulation of the endocannabinoid system and eicosanoid network.
Bononi, Giulia, Granchi, Carlotta, Lapillo, Margherita, Giannotti, Massimiliano, Nieri, Daniela, Fortunato, Serena, Boustani, Maguie El, Caligiuri, Isabella, Poli, Giulio, Carlson, Kathryn E., Kim, Sung Hoon, Macchia, Marco, Martinelli, Adriano, Rizzolio, Flavio, Chicca, Andrea, Katzenellenbogen, John A., Minutolo, Filippo, Tuccinardi, Tiziano   +17 more
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Intrinsic up-regulation of 2-AG favors an area specific neuronal survival in different in vitro models of neuronal damage. [PDF]

PLoS ONE, 2012
The endocannabinoid 2-arachidonoyl glycerol (2-AG) acts as a retrograde messenger and modulates synaptic signaling e. g. in the hippocampus. 2-AG also exerts neuroprotective effects under pathological situations. To better understand the mechanism beyond
Sonja Kallendrusch, Constance Hobusch, Angela Ehrlich, Marcin Nowicki, Simone Ziebell, Ingo Bechmann, Gerd Geisslinger, Marco Koch, Faramarz Dehghani   +8 more
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Hexafluoroisopropyl Carbamates as Selective MAGL and Dual MAGL/FAAH Inhibitors: Biochemical and Physicochemical Properties [PDF]

ChemMedChem, 2022
AbstractA series of hexafluoroisopropyl carbamates with indolylalkyl‐ and azaindolylalkyl‐substituents at the carbamate nitrogen was synthesized and evaluated for inhibition of the endocannabinoid degrading enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
Maximilian Barth, Stefan Rudolph, Jan Kampschulze, Imke Meyer zu Vilsendorf, Walburga Hanekamp, Dennis Mulac, Klaus Langer, Matthias Lehr   +7 more
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[18F]MAGL-4-11 positron emission tomography molecular imaging of monoacylglycerol lipase changes in preclinical liver fibrosis models

Acta Pharmaceutica Sinica B, 2022
Monoacylglycerol lipase (MAGL) is a pivotal enzyme in the endocannabinoid system, which metabolizes 2-arachidonoylglycerol (2-AG) into the proinflammatory eicosanoid precursor arachidonic acid (AA).
Tuo Shao, Zhen Chen, Jian Rong, Vasily Belov, Jiahui Chen, Andre Jeyarajan, Xiaoyun Deng, Hualong Fu, Qingzhen Yu, Steve H. Rwema, Wenyu Lin, Mikhail Papisov, Lee Josephson, Raymond T. Chung, Steven H. Liang   +14 more
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