Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
Obaid Afzal, Suresh Kumar, Rajiv Kumar, Ahmad Firoz, Manu Jaggi, Sandhya Baw. Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors. Bioorganic & medicinal chemistry letters. vol 24. issue 16. 2015-03-06. PMID:25011912. |
monoacylglycerol lipase (magl) is one of the key enzymes of the endocannabinoid system (ecs). |
2015-03-06 |
2023-08-13 |
human |
Andrea Chicca, Diego Caprioglio, Alberto Minassi, Vanessa Petrucci, Giovanni Appendino, Orazio Taglialatela-Scafati, Jürg Gertsc. Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system. ACS chemical biology. vol 9. issue 7. 2015-02-26. PMID:24831513. |
while most changes on this element were detrimental for activity, ring-opening cross metathesis of 1 with ethyl acrylate followed by amide functionalization generated a series of new monocyclic amides (11a, 11b, 11c) that not only retained the cb2 receptor functional agonism of 1 but also reversibly inhibited fatty acid amide hydrolase (faah), the major endocannabinoid degrading enzyme, without affecting monoacylglycerol lipase (magl) and α,β hydrolases 6 and 12. |
2015-02-26 |
2023-08-13 |
Not clear |
Mariateresa Cipriano, Sandra Gouveia-Figueira, Emma Persson, Malin Nording, Christopher J Fowle. The influence of monoacylglycerol lipase inhibition upon the expression of epidermal growth factor receptor in human PC-3 prostate cancer cells. BMC research notes. vol 7. 2015-02-23. PMID:25012825. |
in the present study, we investigated whether similar effects are seen following inhibition of the endocannabinoid hydrolytic enzyme monoacylglycerol lipase (mgl). |
2015-02-23 |
2023-08-13 |
human |
Yan Zheng, Xiao-Li Wang, Feng-Feng Mo, Min L. Dexamethasone alleviates motion sickness in rats in part by enhancing the endocannabinoid system. European journal of pharmacology. vol 727. 2015-01-29. PMID:24508383. |
we used hplc-ms/ms to measure the plasma concentrations of anandamide and 2-arachidonoylglycerol+1-arachidonoylglycerol, and we employed real-time quantitative pcr (qrt-pcr) and/or western blot analysis to assay the expression of n-acylphosphatidyl-ethanolamine hydrolyzing phospholipase d, sn-1-selective diacylglycerol lipase, fatty acid hydrolase, monoacylglycerol lipase and endocannabinoid cb1 receptor in the dorsal vagal complex and stomach of rats exposed to a motion sickness protocol. |
2015-01-29 |
2023-08-12 |
rat |
Jian Zhang, Mei Hu, Zhaoqian Teng, Ya-Ping Tang, Chu Che. Synaptic and cognitive improvements by inhibition of 2-AG metabolism are through upregulation of microRNA-188-3p in a mouse model of Alzheimer's disease. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 34. issue 45. 2015-01-20. PMID:25378159. |
we showed previously that inhibition of monoacylglycerol lipase (magl), the primary enzyme that metabolizes the endocannabinoid 2-arachidonoylglycerol (2-ag) in the brain, robustly reduces aβ by inhibiting β-site amyloid precursor protein cleaving enzyme 1 (bace1), a key enzyme responsible for aβ formation. |
2015-01-20 |
2023-08-13 |
mouse |
Juha R Savinainen, Emilia Kansanen, Tatu Pantsar, Dina Navia-Paldanius, Teija Parkkari, Marko Lehtonen, Tuomo Laitinen, Tapio Nevalainen, Antti Poso, Anna-Liisa Levonen, Jarmo T Laitine. Robust hydrolysis of prostaglandin glycerol esters by human monoacylglycerol lipase (MAGL). Molecular pharmacology. vol 86. issue 5. 2015-01-07. PMID:25140003. |
the primary route of inactivation of the endocannabinoid 2-arachidonoylglycerol in the central nervous system is through enzymatic hydrolysis, mainly carried out by monoacylglycerol lipase (magl), along with a small contribution by the α/β-hydrolase domain (abhd) proteins abhd6 and abhd12. |
2015-01-07 |
2023-08-13 |
human |
Simon Nicolussi, Juan Manuel Viveros-Paredes, María Salomé Gachet, Mark Rau, Mario Eduardo Flores-Soto, Martina Blunder, Jürg Gertsc. Guineensine is a novel inhibitor of endocannabinoid uptake showing cannabimimetic behavioral effects in BALB/c mice. Pharmacological research. vol 80. 2015-01-06. PMID:24412246. |
noteworthy, guineensine did not inhibit endocannabinoid degrading enzymes fatty acid amide hydrolase (faah) or monoacylglycerol lipase (magl) nor interact with cannabinoid receptors or fatty acid binding protein 5 (fabp5), a major cytoplasmic aea carrier. |
2015-01-06 |
2023-08-12 |
mouse |
Tiziano Tuccinardi, Carlotta Granchi, Flavio Rizzolio, Isabella Caligiuri, Vittoria Battistello, Giuseppe Toffoli, Filippo Minutolo, Marco Macchia, Adriano Martinell. Identification and characterization of a new reversible MAGL inhibitor. Bioorganic & medicinal chemistry. vol 22. issue 13. 2014-12-30. PMID:24853323. |
monoacylglycerol lipase is a serine hydrolase that play a major role in the degradation of 2-arachidonoylglycerol, an endocannabinoid neurotransmitter implicated in several physiological processes. |
2014-12-30 |
2023-08-13 |
Not clear |
Jae Won Chang, Armand B Cognetta, Micah J Niphakis, Benjamin F Cravat. Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition. ACS chemical biology. vol 8. issue 7. 2014-11-11. PMID:23701408. |
we exploit the proteome-wide specificity of hfip carbamates to create in situ imaging probes for the endocannabinoid hydrolases monoacylglycerol lipase (magl) and α-β hydrolase-6 (abhd6). |
2014-11-11 |
2023-08-12 |
mouse |
B M Ignatowska-Jankowska, S Ghosh, M S Crowe, S G Kinsey, M J Niphakis, R A Abdullah, Q Tao, S T O' Neal, D M Walentiny, J L Wiley, B F Cravatt, A H Lichtma. In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects. British journal of pharmacology. vol 171. issue 6. 2014-11-05. PMID:23848221. |
since monoacylglycerol lipase (magl) has been firmly established as the predominant catabolic enzyme of the endocannabinoid 2-arachidonoylglycerol (2-ag), a great need has emerged for the development of highly selective magl inhibitors. |
2014-11-05 |
2023-08-12 |
Not clear |
D M Kerr, B Harhen, B N Okine, L J Egan, D P Finn, M Roch. The monoacylglycerol lipase inhibitor JZL184 attenuates LPS-induced increases in cytokine expression in the rat frontal cortex and plasma: differential mechanisms of action. British journal of pharmacology. vol 169. issue 4. 2014-10-08. PMID:23043675. |
jzl184 is a selective inhibitor of monoacylglycerol lipase (magl), the enzyme that preferentially catabolizes the endocannabinoid 2-arachidonoyl glycerol (2-ag). |
2014-10-08 |
2023-08-12 |
rat |
Eszter Horváth, Stephen G Woodhams, Rita Nyilas, Christopher M Henstridge, Masanobu Kano, Kenji Sakimura, Masahiko Watanabe, István Katon. Heterogeneous presynaptic distribution of monoacylglycerol lipase, a multipotent regulator of nociceptive circuits in the mouse spinal cord. The European journal of neuroscience. vol 39. issue 3. 2014-09-25. PMID:24494682. |
monoacylglycerol lipase (mgl) is a multifunctional serine hydrolase, which terminates anti-nociceptive endocannabinoid signaling and promotes pro-nociceptive prostaglandin signaling. |
2014-09-25 |
2023-08-12 |
mouse |
Ahmet Ulugö. The endocannabinoid system as a potential therapeutic target for pain modulation. Balkan medical journal. vol 31. issue 2. 2014-09-10. PMID:25207181. |
cannabinoid therapy re-gained attention only after the discovery of endocannabinoids and fatty acid amide hydrolase (faah) and monoacylglycerol lipase (magl), the enzymes playing a role in endocannabinoid metabolism. |
2014-09-10 |
2023-08-13 |
Not clear |
Joel E Schlosburg, Steven G Kinsey, Bogna Ignatowska-Jankowska, Divya Ramesh, Rehab A Abdullah, Qing Tao, Lamont Booker, Jonathan Z Long, Dana E Selley, Benjamin F Cravatt, Aron H Lichtma. Prolonged monoacylglycerol lipase blockade causes equivalent cannabinoid receptor type 1 receptor-mediated adaptations in fatty acid amide hydrolase wild-type and knockout mice. The Journal of pharmacology and experimental therapeutics. vol 350. issue 2. 2014-08-26. PMID:24849924. |
complementary genetic and pharmacological approaches to inhibit monoacylglycerol lipase (magl) and fatty acid amide hydrolase (faah), the primary hydrolytic enzymes of the respective endogenous cannabinoids 2-arachidonoylglycerol (2-ag) and n-arachidonoylethanolamine, enable the exploration of potential therapeutic applications and physiologic roles of these enzymes. |
2014-08-26 |
2023-08-13 |
mouse |
Astrid Bergerot, Mark Rigby, Guy Bouvier, Païkan Marcagg. Persistent posttetanic depression at cerebellar parallel fiber to Purkinje cell synapses. PloS one. vol 8. issue 7. 2014-08-21. PMID:23922966. |
we rule out endocannabinoid signaling since the inhibition of type 1 cannabinoid receptors, monoacylglycerol lipase or vanilloid receptor 1, or incubation with anandamide had no detectable effect. |
2014-08-21 |
2023-08-12 |
mouse |
Carolina Costola-de-Souza, Alison Ribeiro, Viviane Ferraz-de-Paula, Atilio Sersun Calefi, Thiago Pinheiro Arrais Aloia, João Antonio Gimenes-Júnior, Vinicius Izidio de Almeida, Milena Lobão Pinheiro, João Palermo-Net. Monoacylglycerol lipase (MAGL) inhibition attenuates acute lung injury in mice. PloS one. vol 8. issue 10. 2014-08-05. PMID:24204926. |
endocannabinoid signaling is terminated by enzymatic hydrolysis, a process that, for 2-arachidonoylglycerol (2-ag), is mediated by monoacylglycerol lipase (magl). |
2014-08-05 |
2023-08-12 |
mouse |
Miquel Bioque, Borja García-Bueno, Karina S Macdowell, Ana Meseguer, Pilar A Saiz, Mara Parellada, Ana Gonzalez-Pinto, Roberto Rodriguez-Jimenez, Antonio Lobo, Juan C Leza, Miguel Bernard. Peripheral endocannabinoid system dysregulation in first-episode psychosis. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 38. issue 13. 2014-07-01. PMID:23822951. |
protein expression of cannabinoid receptor 2 (cb2), the protein levels of the main endocannabinoid synthesizing enzymes n-acyl phosphatidylethanolamine phospholipase (nape) and diacylglycerol lipase (dagl), and of degradation enzymes fatty acid amide hydrolase (faah) and monoacylglycerol lipase (magl) were determined by western blot analysis in peripheral blood mononuclear cells (pbmcs). |
2014-07-01 |
2023-08-12 |
human |
Micah J Niphakis, Armand B Cognetta, Jae Won Chang, Matthew W Buczynski, Loren H Parsons, Frederika Byrne, James J Burston, Victoria Chapman, Benjamin F Cravat. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors. ACS chemical neuroscience. vol 4. issue 9. 2014-04-14. PMID:23731016. |
monoacylglycerol lipase (magl) is a principal metabolic enzyme responsible for hydrolyzing the endogenous cannabinoid (endocannabinoid) 2-arachidonoylglycerol (2-ag). |
2014-04-14 |
2023-08-12 |
rat |
Himiko Suzuki, Yuki Ito, Yuki Noro, Mamoru Koketsu, Michihiro Kamijima, Motohiro Tomizaw. Organophosphate agents induce plasma hypertriglyceridemia in mouse via single or dual inhibition of the endocannabinoid hydrolyzing enzyme(s). Toxicology letters. vol 225. issue 1. 2014-03-06. PMID:24361246. |
diverse serine hydrolases including endocannabinoid metabolizing enzymes fatty acid amide hydrolase (faah) and monoacylglycerol lipase (magl) have been suggested as secondary targets for organophosphate (op) agents to exert adverse toxic effects such as lipid homeostasis disruption. |
2014-03-06 |
2023-08-12 |
mouse |
Ioannis Karageorgos, Thomas E Wales, David R Janero, Nikolai Zvonok, V Kiran Vemuri, John R Engen, Alexandros Makriyanni. Active-site inhibitors modulate the dynamic properties of human monoacylglycerol lipase: a hydrogen exchange mass spectrometry study. Biochemistry. vol 52. issue 29. 2014-02-20. PMID:23795559. |
human monoacylglycerol lipase (hmgl) regulates endocannabinoid signaling primarily by deactivating the lipid messenger 2-arachidonoylglycerol. |
2014-02-20 |
2023-08-12 |
human |