Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency.
Laitinen T1, Navia-Paldanius D, Rytilahti R, Marjamaa JJ, Kařízková J, Parkkari T, Pantsar T, Poso A, Laitinen JT, Savinainen JR.
Molecular pharmacology.Mol Pharmacol.2014 Mar;85(3):510-9. doi: 10.1124/mol.113.090795. Epub 2013 Dec 24.
Considerable progress has been made in recent years in developing selective, potent monoacylglycerol lipase (MAGL) inhibitors. In the investigations of measures to inhibit this enzyme, less attention has been paid to improving our understanding of its catalytic mechanisms or substrate preferences. I
A mechanism regulating G protein-coupled receptor signaling that requires cycles of protein palmitoylation and depalmitoylation.
Jia L1, Chisari M, Maktabi MH, Sobieski C, Zhou H, Konopko AM, Martin BR, Mennerick SJ, Blumer KJ.
The Journal of biological chemistry.J Biol Chem.2014 Feb 28;289(9):6249-57. doi: 10.1074/jbc.M113.531475. Epub 2014 Jan 2.
Reversible attachment and removal of palmitate or other long-chain fatty acids on proteins has been hypothesized, like phosphorylation, to control diverse biological processes. Indeed, palmitate turnover regulates Ras trafficking and signaling. Beyond this example, however, the functions of palmitat
Lipid signaling cascades of orexin/hypocretin receptors.
Kukkonen JP.
Biochimie.Biochimie.2014 Jan;96:158-65. doi: 10.1016/j.biochi.2013.06.015. Epub 2013 Jun 28.
Orexins - orexin-A and orexin-B - are neuropeptides with significant role in regulation of fundamental physiological processes such as sleep-wakefulness cycle. Orexins act via G-protein-coupled OX1 and OX2 receptors, which are found, in addition to the central nervous system, also in a number of per
Biological and Pharmaceutical Bulletin 34(2), 191-196, 2011
… When cells were treated with methyl arachidonyl fluorophosphonate used as an inhibitor of group IVC PLA2, the fatty acid-induced deposition of TG was partially but significantly suppressed at 48 h, although no significant inhibition was observed at 24 h. …
Journal of pharmacological sciences 108(1), 79-88, 2008-09-20
… An inhibitor of phospholipase A2, methyl arachidonyl fluorophosphonate (MAFP), and inhibitors of P450s inhibited the VEGF and EPO induction of HUAEC and Hep3B, respectively, under hypoxia. …
Presynaptic monoacylglycerol lipase activity determines basal endocannabinoid tone and terminates retrograde endocannabinoid signaling in the hippocampus
Journal of Neuroscience 27(5), 1211-1219, 2007-01-31
… We found that MGL inhibitors, methyl arachidonoyl fluorophosphonate and arachidonoyl trifluoromethylketone, caused a gradual suppression of cannabinoid-sensitive IPSCs in cultured hippocampal neurons. …
Thermo Scientific Serine Hydrolase Probes are ActivX Fluorophosphonate (FP) and other tagged phosphonate probes to purify or assay serine hydrolase active sites using fluorescence, biotin-affinity, or mass spectrometry. Features of ...
New fluorophosphonate probes selectively label and enrich active serine hydrolases by Ryan D. Bomgarden, Ph.D.; Chris L. Etienne, Ph.D.; Rosa I. Viner, Ph.D.1 ... The Thermo Scientific ActivX Serine Hydrolase Probes consist of a ...