Results 41 to 50 of about 4,187 (189)

Rational Development of MAGL Inhibitors

, 2018
Hit identification and hit-to-lead optimization are key steps of the early drug discovery program. Starting from the X-ray crystal structure of the human monoacylglycerol lipase (hMAGL), we herein describe the computational and experimental procedures that we applied for identifying and optimizing a new active inhibitor of this target enzyme.
Granchi, Carlotta, Rizzolio, Flavio, Caligiuri, Isabella, Macchia, Marco, Martinelli, Adriano, Minutolo, Filippo, Tuccinardi, Tiziano   +6 more
openaire   +3 more sources

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

Brain structural changes in cannabis dependence: association with MAGL [PDF]

Molecular Psychiatry, 2019
AbstractCannabis use is rising, yet there is poor understanding of biological processes that might link chronic cannabis use to brain structural abnormalities. To lend insight into this topic, we examined white matter microstructural integrity and gray matter cortical thickness/density differences between 89 individuals with cannabis dependence (CD ...
Manza, Peter, Yuan, Kai, Shokri-Kojori, Ehsan, Tomasi, Dardo, Volkow, Nora D.   +4 more
openaire   +2 more sources

Set-Up and Validation of a High Throughput Screening Method for Human Monoacylglycerol Lipase (MAGL) Based on a New Red Fluorescent Probe

Molecules, 2019
Monoacylglycerol lipase (MAGL) is a serine hydrolase that has a key regulatory role in controlling the levels of 2-arachidonoylglycerol (2-AG), the main signaling molecule in the endocannabinoid system.
Matteo Miceli, Silvana Casati, Roberta Ottria, Simone Di Leo, Ivano Eberini, Luca Palazzolo, Chiara Parravicini, Pierangela Ciuffreda   +7 more
doaj   +1 more source

Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. [PDF]

, 2021
An interesting enzyme of the endocannabinoid system is monoacylglycerol lipase (MAGL). This enzyme, which metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG), has attracted great interest due to its involvement in several physiological and ...
Tiziana Perin, Rizzolio F., Sandra Glasmacher, Gertsch, Jürg, Tuccinardi T., Poli, Giulio, Elisa Giovannetti, Filippo Minutolo, Giovannetti, Elisa, Macchia, Marco, Carlotta Granchi, Flavio Rizzolio, Bononi, Giulia, Gori, Eleonora, Gori E., Stefano Palazzolo, Canzonieri V., Isabella Caligiuri, Rebecca Ferrisi, Rizzolio, Flavio, Glasmacher S., Andrea Chicca, Perin, Tiziana, Gertsch J., Macchia M., Palazzolo, Stefano, Bononi G., Palazzolo S., Granchi, Carlotta, Marco Macchia, Sodi, Andrea, Minutolo, Filippo, Sodi A., JÃrg Gertsch, Caligiuri I., Eleonora Gori, Giulio Poli, Granchi C., Gertsch, J. rg, Giulia Mantini, Glasmacher, Sandra, Vincenzo Canzonieri, Chicca, Andrea, Giovannetti E., Canzonieri, Vincenzo, Ferrisi, Rebecca, Mantini, Giulia, Andrea Sodi, Ferrisi R., Perin T., Chicca A., Poli G., Tuccinardi, Tiziano, Giulia Bononi, Mantini G., Caligiuri, Isabella, Minutolo F., Tiziano Tuccinardi   +57 more
core   +1 more source

Monoacylglycerol Lipase Is a Therapeutic Target for Alzheimer's Disease

Cell Reports, 2012
Alzheimer's disease (AD) is the most common cause of dementia among older people. There are no effective medications currently available to prevent and treat AD and halt disease progression.
Rongqing Chen, Jian Zhang, Yan Wu, Dongqing Wang, Guoping Feng, Ya-Ping Tang, Zhaoqian Teng, Chu Chen   +7 more
doaj   +1 more source

An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present)

, 2020
Introduction: Monoacylglycerol lipase (MAGL) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol.
Tuccinardi T., Bononi G., Poli G., Rizzolio F., Macchia M., Minutolo F., Granchi C.   +6 more
core   +1 more source

Is there a role for cannabidiol in obesity, metabolic syndrome and binge eating?

British Journal of Pharmacology, EarlyView.
Cannabidiol (CBD) is one of the most abundant phytocannabinoids isolated from the Cannabis sativa plant. CBD is a lipophilic, non‐intoxicating substance that differently from Δ9‐tetrahydrocannabinol (Δ9‐THC) does not present the typical profile of a drug of abuse.
Luca Botticelli, Emanuela Micioni Di Bonaventura, Giacomo Einaudi, Gustavo Provensi, Alessia Costa, Claudio D'Addario, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura   +7 more
wiley   +1 more source

A Dysregulated Endocannabinoid-Eicosanoid Network Supports Pathogenesis in a Mouse Model of Alzheimer's Disease

Cell Reports, 2012
Although inflammation in the brain is meant as a defense mechanism against neurotoxic stimuli, increasing evidence suggests that uncontrolled, chronic, and persistent inflammation contributes to neurodegeneration. Most neurodegenerative diseases have now
Justin R. Piro, Daniel I. Benjamin, James M. Duerr, YeQing Pi, Cathleen Gonzales, Kathleen M. Wood, Joel W. Schwartz, Daniel K. Nomura, Tarek A. Samad   +8 more
doaj   +1 more source

Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

The Journal of Headache and Pain, 2023
Background Engaging the endocannabinoid system through inhibition of monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), degrading endocannabinoids (endoCBs) 2-arachidonoylglycerol (2-AG) and anandamide (AEA), was proposed as a ...
Adriana Della Pietra, Georgii Krivoshein, Konstantin Ivanov, Raisa Giniatullina, Henna-Kaisa Jyrkkänen, Ville Leinonen, Marko Lehtonen, Arn M. J. M. van den Maagdenberg, Juha Savinainen, Rashid Giniatullin   +9 more
doaj   +1 more source