Results 1 to 10 of about 4,187 (189)

New Disulfiram Derivatives as MAGL-Selective Inhibitors [PDF]

Molecules, 2021
Monoacylglycerol lipase (MAGL) is a key enzyme in the human endocannabinoid system. It is also the main enzyme responsible for the conversion of 2-arachidonoyl glycerol (2-AG) to arachidonic acid (AA), a precursor of prostaglandin synthesis.
Ziad Omran
doaj   +4 more sources

The biological functions of monoacylglycerol lipase (MAGL) in cancer [PDF]

Saudi Pharmaceutical Journal
Cancer is a metabolic disease marked by disruptions in lipid metabolism, which significantly influences tumor development. The synthesis and breakdown of lipids, governed by various enzymes, play a vital role in this process.
Faris Almutairi
doaj   +3 more sources

Discovery of MAGL Inhibition by Lophine Derivatives: An Unexpected Finding from Chemiluminescent Assay Development [PDF]

Molecules
The inhibitory effects of two novel lophine derivatives were unexpectedly discovered during the development of a chemiluminescent monoacylglycerol lipase (MAGL) assay.
Roberta Ottria, Silvana Casati, Ornella Xynomilakis, Aleksandar Veselinović, Pierangela Ciuffreda   +4 more
doaj   +4 more sources

Notoginsenoside R1, a Metabolite from Panax notoginseng, Prevents Paclitaxel-Induced Peripheral Neuropathic Pain in Mice [PDF]

Molecules
Development of paclitaxel-induced neuropathic pain (PINP) during chemotherapy may lead to paclitaxel discontinuation, potentially compromising effective anticancer therapy. PINP can manifest as allodynia.
Muneerah Al-Musailem, Willias Masocha, Altaf Al-Romaiyan   +2 more
doaj   +2 more sources

Correlation Between In Silico Docking/Simulation Results and In Vitro MAGL Inhibition Potency of Selected Triterpenes [PDF]

Current Issues in Molecular Biology
Monoacylglycerol lipase (MAGL) degrades the endocannabinoid 2-arachidonyl glycerol. MAGL inhibitors, such as the triterpene pristimerin, alleviate neuropathic pain in animal models.
Willias Masocha, Mohammed A. Khedr
doaj   +2 more sources

MAGL-18c attenuates LPS-induced sepsis-associated liver injury by inhibiting TGF-β/Smad signaling and remodeling medium- and long-chain fatty acid metabolism [PDF]

Frontiers in Immunology
IntroductionSepsis is a major global health burden associated with high mortality and multiple organ dysfunction, among which liver injury is a key determinant of poor prognosis.
Ying Wang, Meijia Li, Zixia Liang, Yunyu Wang, Honghua Li, Shirong Li, Xu Jiao, Na Guo, Guoxin Dai, Guimin Zhang, Guimin Zhang, Xiaoyan Lu, Jingchun Yao, Jingchun Yao, Jingchun Yao   +14 more
doaj   +2 more sources

Dualsteric Agonist for M2 Muscarinic Receptor Causes Oxidative Stress and Mitochondrial Alteration in Human Glioblastoma Cancer Stem Cells. [PDF]

J Neurochem
Dualsteric agonist N8‐iper shows cytotoxic effects on glioblastoma cancer stem cells, but not on human normal astrocytes. Lipid accumulation appears as a consequence of cytotoxic stress; in fact, they are not present in healthy astrocytes. ABSTRACT Glioblastoma (GB) is the most malignant form of human brain tumor, characterized by heterogeneous cell ...
Guerriero C, De Nuccio C, Petrone M, Rinaldi T, Cirigliano A, Visentin S, Bernardo A, Conti L, Matera C, De Amici M, Dallanoce C, Tata AM.   +11 more
europepmc   +2 more sources

Enhancement of the endocannabinoid system through monoacylglycerol lipase inhibition relieves migraine-associated pain in mice [PDF]

The Journal of Headache and Pain
Background Migraine affects over 1 billion people worldwide and is a leading cause of disability. Targeting the cannabinoid system offers a promising approach for pain and migraine relief.
Elizaveta Mangutov, Yaseen Awad-Igbaria, Kendra Siegersma, Francois Gastambide, Ayodeji A. Asuni, Amynah A. A. Pradhan   +5 more
doaj   +2 more sources

MAGL targeted PROTAC degrader simultaneously enhances P53 for synergistic treatment of glioblastoma stem cell [PDF]

Cell Death Discovery
Glioblastoma (GBM) stands as the most fatal brain tumor due to limited therapeutic options and high rates of drug resistance. Current surgical and pharmacological interventions usually fail to eradicate the aggressive GBM stem cells (GSCs), which leads ...
Zheng Yuan, Meixia Guo, Yue Zhang, Yilin Deng, Biao Sun, Yaning Hou, Xin Wang, Xiong Jin, Yang Liu, Bingyang Shi, Jinlong Yin   +10 more
doaj   +2 more sources

Inhibition of endocannabinoid hydrolases MAGL, FAAH and ABHD6 by AKU-005 reduces ex vivo cortical spreading depression [PDF]

The Journal of Headache and Pain
Background Migraine is a common neurovascular disorder that remains currently untreated in half of the patients. One third of migraine patients experience aura, which is associated with the development of cortical spreading depolarization (CSD), a wave ...
Flavia Brugia, Konstantin Ivanov, Auni Aroviita, Raisa Giniatullina, Marko Lehtonen, Tarja Malm, Juha Savinainen, Rashid Giniatullin, Adriana Della Pietra   +8 more
doaj   +2 more sources