Results 31 to 40 of about 3,186 (156)

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

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

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.
openaire   +2 more sources

Research Review: What we have learned about the endocannabinoid system in developmental psychopathology. [PDF]

J Child Psychol Psychiatry
Background The endocannabinoid (eCB) system, the primary target of cannabis, has gained significant attention as a potential novel therapeutic approach for treating a range of psychiatric disorders characterized by dysregulation of stress, emotion, and social behavior.
Tansey RC, Ferger MD, Marusak HA, Mayo LM.   +3 more
europepmc   +2 more sources

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
doaj   +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

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
openaire   +3 more sources

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

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