Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
Ning Yang, Meng Li, Xuefeng Li, Lunan Wu, Wenzhi Wang, Yaozeng Xu, Zhen Wang, Chen Zhu, Dechun Gen. MAGL blockade alleviates steroid-induced femoral head osteonecrosis by reprogramming BMSC fate in rat. Cellular and molecular life sciences : CMLS. vol 81. issue 1. 2024-10-05. PMID:39368012. |
blocking monoacylglycerol lipase (magl) could effectively ameliorate onfh by mitigating oxidative stress and apoptosis in bmscs induced by glucocorticoids (gc). |
2024-10-05 |
2024-10-08 |
rat |
Leejeong Kim, Guanghai Nan, Hee Young Kim, Myeounghoon Cha, Bae Hwan Le. Modulation of chemotherapy-induced peripheral neuropathy by JZL195 through glia and the endocannabinoid system. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. vol 180. 2024-10-03. PMID:39362070. |
this study aimed to investigate the effects of jzl195, an inhibitor of fatty acid amide hydrolase (faah) and monoacylglycerol lipase (magl), and explore the connection between cannabinoid receptors and tlr4 in glial cells. |
2024-10-03 |
2024-10-07 |
mouse |
Bernd Kuhn, Martin Ritter, Benoit Hornsperger, Charles Bell, Buelent Kocer, Didier Rombach, Marius D R Lutz, Luca Gobbi, Martin Kuratli, Christian Bartelmus, Markus Bürkler, Raffael Koller, Paolo Tosatti, Iris Ruf, Melanie Guerard, Anto Pavlovic, Juliane Stephanus, Fionn O'Hara, Dennis Wetzl, Wiebke Saal, Martine Stihle, Doris Roth, Melanie Hug, Sylwia Huber, Dominik Heer, Carsten Kroll, Andreas Topp, Manfred Schneider, Jürg Gertsch, Sandra Glasmacher, Mario van der Stelt, Andrea Martella, Matthias Beat Wittwer, Ludovic Collin, Jörg Benz, Hans Richter, Uwe Grethe. Structure-Guided Discovery of Journal of medicinal chemistry. 2024-10-03. PMID:39360636. |
structure-guided discovery of monoacylglycerol lipase (magl) is a key enzyme involved in the metabolism of the endogenous signaling ligand 2-arachidonoylglycerol, a neuroprotective endocannabinoid intimately linked to central nervous system (cns) disorders associated with neuroinflammation. |
2024-10-03 |
2024-10-05 |
Not clear |
Dexiao Zhu, Jian Zhang, Xiaokuang Ma, Mei Hu, Fei Gao, Jack B Hashem, Jianlu Lyu, Jing Wei, Yuehua Cui, Shenfeng Qiu, Chu Che. Overabundant endocannabinoids in neurons are detrimental to cognitive function. bioRxiv : the preprint server for biology. 2024-09-30. PMID:39345517. |
previous studies have demonstrated that inactivating monoacylglycerol lipase (magl), the primary enzyme responsible for degrading 2-ag in the brain, alleviates neuropathology and prevents synaptic and cognitive decline in animal models of neurodegenerative diseases. |
2024-09-30 |
2024-10-02 |
mouse |
Johannes Aebi, Kenneth Atz, Simon M Ametamey, Jörg Benz, Julie Blaising, Stefania Butini, Giuseppe Campiani, Erick M Carreira, Ludovic Collin, Eva De Lago, Thais Gazzi, Jürg Gertsch, Luca Gobbi, Wolfgang Guba, Javier Fernández-Ruiz, Jürgen Fingerle, Ahmed Haider, Yingfang He, Laura H Heitman, Michael Honer, Daniel Hunziker, Bernd Kuhn, Mauro Maccarrone, Hans Peter Märki, Rainer E Martin, Peter Mohr, Linjing Mu, Marc Nazaré, David F Nippa, Sergio Oddi, Fionn O'Hara, Pal Pacher, Julian Romero, Stephan Röver, Arne C Rufer, Roger Schibli, Gisbert Schneider, Antonia F Stepan, David A Sykes, Christoph Ullmer, Mario Van der Stelt, Dmitry B Veprintsev, Matthias B Wittwer, Uwe Grethe. Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects. Chimia. vol 78. issue 7-8. 2024-09-02. PMID:39221845. |
given its therapeutic significance, we have launched a series of drug discovery endeavors aimed at ecs targets, including peroxisome proliferator-activated receptors (ppars), cannabinoid receptors types 1 (cb1r) and 2 (cb2r), and monoacylglycerol lipase (magl), addressing a wide array of medical needs. |
2024-09-02 |
2024-09-04 |
Not clear |
Wilmarie Morales-Soto, Beatriz Thomasi, Brian D Gulbranse. Endocannabinoids regulate enteric neuron-glia networks and visceral hypersensitivity following inflammation through a glial-dependent mechanism. Glia. 2024-08-12. PMID:39132860. |
enteric glia modulate gut neurons that control motility and pain and express monoacylglycerol lipase (magl) which controls endocannabinoid availability. |
2024-08-12 |
2024-08-14 |
Not clear |
Quanwei Yu, Chao Song, Liyun Bi, Shuang Zhao, Qian Lei, Na Yang, Hai Chen, Yuxi Wang, Yang He, Hui Den. Design, synthesis and biological evaluation of naphthyl amide derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. Bioorganic & medicinal chemistry. vol 111. 2024-08-06. PMID:39106652. |
monoacylglycerol lipase (magl) is a key enzyme responsible for the metabolism of the endocannabinoid 2-arachidonoylglycerol (2-ag), and has attracted great interest due to its involvement in various physiological and pathological processes, such as cancer progression. |
2024-08-06 |
2024-08-09 |
Not clear |
Ming Jiang, Mirjam C W Huizenga, Florian Mohr, Avand Amedi, Renze Bakker, Richard J B H N van den Berg, Hui Deng, Tom van der Wel, Constant A A van Boeckel, Mario van der Stel. Structure-Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors. Journal of medicinal chemistry. 2024-07-11. PMID:38988250. |
monoacylglycerol lipase (magl) is the key enzyme for the hydrolysis of endocannabinoid 2-arachidonoylglycerol (2-ag). |
2024-07-11 |
2024-07-13 |
Not clear |
Hongqing Zhao, Yang Liu, Na Cai, Xiaolin Liao, Lin Tang, Yuhong Wan. Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs. Drug design, development and therapy. vol 18. 2024-06-17. PMID:38882045. |
more recent efforts have emphasized that inhibition of two major endogenous cannabinoid hydrolases, monoacylglycerol lipase (magl) and fatty acid amide hydrolase (faah), indirectly activates cannabinoid receptors by increasing endogenous cannabinoid levels in the synaptic gap, circumventing receptor desensitization resulting from direct enhancement of endogenous cannabinoid signaling. |
2024-06-17 |
2024-06-19 |
Not clear |
Alexis F League, Barkha J Yadav-Samudrala, Ramya Kolagani, Calista A Cline, Ian R Jacobs, Jonathan Manke, Micah J Niphakis, Benjamin F Cravatt, Aron H Lichtman, Bogna M Ignatowska-Jankowska, Sylvia Fittin. A helping HAND: therapeutic potential of MAGL inhibition against HIV-1-associated neuroinflammation. Frontiers in immunology. vol 15. 2024-06-05. PMID:38835765. |
alternatively, inhibiting monoacylglycerol lipase (magl) has demonstrated therapeutic potential through interactions with the endocannabinoid system. |
2024-06-05 |
2024-06-07 |
human |
Arlene Martínez-Rivera, Robert N Fetcho, Lizzie Birmingham, Jin X Jiu, Ruirong Yang, Careen Foord, Diego Scala-Chávez, Narmin Mekawy, Kristen Pleil, Virginia M Pickel, Conor Liston, Carlos M Castorena, Joshua Levitz, Ying-Xian Pan, Lisa A Briand, Anjali M Rajadhyaksha, Francis S Le. Elevating levels of the endocannabinoid 2-arachidonoylglycerol blunts opioid reward but not analgesia. bioRxiv : the preprint server for biology. 2024-05-20. PMID:38766079. |
here we show in male and female mice that enhancing levels of the ecb, 2-arachidonoylglycerol (2-ag), through pharmacological inhibition of its catabolic enzyme, monoacylglycerol lipase (magl), either systemically or in the ventral tegmental area (vta) with jzl184, leads to a substantial attenuation of the rewarding effects of opioids in male and female mice using conditioned place preference and self-administration paradigms, without altering their analgesic properties. |
2024-05-20 |
2024-05-27 |
mouse |
Kang Jun Cho, Mamoru Hashimoto, Sergei Karnup, Kanako Matsuoka, Tadanobu Kamijo, Joon Chul Kim, Jun Sung Koh, Naoki Yoshimur. Improvement of lower urinary tract dysfunction by a monoacylglycerol lipase inhibitor in mice with spinal cord injury. Neurourology and urodynamics. 2024-03-27. PMID:38533637. |
activation of the endocannabinoid system by monoacylglycerol lipase (magl) blockade may affect the lower urinary tract function. |
2024-03-27 |
2024-03-29 |
mouse |
Jens D Mikkelsen, Sanjay S Aripaka, Cansu B Egilmez, Burcu A Pazarla. Binding of the monoacylglycerol lipase (MAGL) radiotracer [ Neurochemistry international. 2024-03-06. PMID:38447759. |
binding of the monoacylglycerol lipase (magl) radiotracer [ monoacylglycerol lipase (magl) is a cytosolic serine hydrolase considered a potential novel drug target for the treatment of cns disorders including epilepsy. |
2024-03-06 |
2024-03-09 |
rat |
Qingjing Hao, Junwei Shi, Zhilan Zhang, Guoqing Yang, Yunbao Zhi, Ke Wang, Dingchen Ma, Shengnan Fu, Haijuan Dong, Zhuoer Zhi, Wenting Zhang, Tingting Li, Jinxin Wan. Discovery of a novel class of reversible monoacylglycerol lipase inhibitors for potential treatment of depression. European journal of medicinal chemistry. vol 268. 2024-03-01. PMID:38428273. |
biological studies on the endocannabinoid system (ecs) have suggested that monoacylglycerol lipase (magl), an essential enzyme responsible for the hydrolysis of 2-arachidonoylglycerol (2-ag), is a novel target for developing antidepressants. |
2024-03-01 |
2024-03-04 |
Not clear |
Clare M Diester, Hallie Balint, James C Gillespie, Aron H Lichtman, Laura J Sim-Selley, Dana E Selley, S Stevens Negu. The Journal of pharmacology and experimental therapeutics. 2024-01-23. PMID:38262742. |
mjn110 inhibits the enzyme monoacylglycerol lipase (magl) to increase levels of the endocannabinoid (ecb) 2-arachidonoylglycerol (2-ag), an endogenous high-efficacy agonist of cannabinoid 1 and 2 receptors (cb |
2024-01-23 |
2024-01-26 |
Not clear |
b' Estefan\\xc3\\xada Chamorro-Aguirre, Virginia L Gaveglio, Ana C Pascual, Susana J Pasquar\\xc3\\xa. The Metabolism of 2-arachidonoylglycerol in Rod Outer Segments Is Modulated by Proteins Involved in the Phototransduction Process. Molecular neurobiology. 2023-12-18. PMID:38109005.' |
we previously reported that 2-arachidonoylglycerol (2-ag) synthesis by diacylglycerol lipase (dagl) and lysophosphatidate phosphohydrolase (lpap) and hydrolysis by monoacylglycerol lipase (magl) in rod outer segments (ros) from bovine retina were differently modified by light applied to the retina. |
2023-12-18 |
2023-12-21 |
cattle |
Ming Jiang, Mirjam C W Huizenga, Jonah L Wirt, Janos Paloczi, Avand Amedi, Richard J B H N van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F Driever, Bogdan I Florea, Uwe Grether, Antonius P A Janssen, Thomas Hankemeier, Laura H Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F Stevens, Daan van der Vliet, Tom van der Wel, Matthias B Wittwer, Constant A A van Boeckel, Pal Pacher, Andrea G Hohmann, Mario van der Stel. A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence. Nature communications. vol 14. issue 1. 2023-12-05. PMID:38052772. |
monoacylglycerol lipase (magl) regulates endocannabinoid 2-arachidonoylglycerol (2-ag) and eicosanoid signalling. |
2023-12-05 |
2023-12-10 |
mouse |
Corina Andrei, Dragos Paul Mihai, Georgiana Nitulescu, Anca Ungurianu, Denisa Marilena Margina, George Mihai Nitulescu, Octavian Tudorel Olaru, Radu Mihai Busca, Anca Zanfiresc. Cetirizine and Levetiracetam as Inhibitors of Monoacylglycerol Lipase: Investigating Their Repurposing Potential as Novel Osteoarthritic Pain Therapies. Pharmaceuticals (Basel, Switzerland). vol 16. issue 11. 2023-11-25. PMID:38004429. |
considering that the endocannabinoid 2-arachidonoyl glycerol is involved in pain processing, increasing its concentration through monoacylglycerol lipase (magl) inhibition reduces pain in various animal models. |
2023-11-25 |
2023-11-28 |
Not clear |
Miriana Di Stefano, Samuele Masoni, Giulia Bononi, Giulio Poli, Salvatore Galati, Francesca Gado, Simone Manzi, Chiara Vagaggini, Annalaura Brai, Isabella Caligiuri, Kanwal Asif, Flavio Rizzolio, Marco Macchia, Andrea Chicca, Andrea Sodi, Valeria Di Bussolo, Filippo Minutolo, Philip Meier, Jürg Gertsch, Carlotta Granchi, Elena Dreassi, Tiziano Tuccinard. Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors. European journal of medicinal chemistry. vol 263. 2023-11-17. PMID:37976705. |
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. |
2023-11-17 |
2023-11-20 |
mouse |
Felix Wittig, Liza Pannenberg, Rico Schwarz, Sander Bekeschus, Robert Ramer, Burkhard Hin. Antiangiogenic Action of JZL184 on Endothelial Cells via Inhibition of VEGF Expression in Hypoxic Lung Cancer Cells. Cells. vol 12. issue 19. 2023-10-13. PMID:37830546. |
jzl184, an inhibitor of monoacylglycerol lipase (magl) and thus of the degradation of the endocannabinoid 2-arachidonoylglycerol (2-ag), mediates various anticancer effects in preclinical studies. |
2023-10-13 |
2023-10-15 |
human |