Association between alcoholism and the gene encoding the endocannabinoid synthesizing enzyme diacylglycerol lipase alpha in the Japanese population.
Sign Up to like & getrecommendations! Published in 2018 at "Alcohol"
DOI: 10.1016/j.alcohol.2017.09.005
Abstract: The endocannabinoid system has been recognized to be involved in neuropsychiatric diseases. 2-arachidonoyl glycerol (2-AG) is one of the two main endocannabinoids, and their regulation could play roles in disorders under environmental influence. This study… read more here.
Keywords: diacylglycerol lipase; alcoholism; enzyme diacylglycerol; japanese population ... See more keywords
Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors
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DOI: 10.1021/acs.jmedchem.9b00686
Abstract: Drug discovery programs of covalent irreversible, mechanism-based enzyme inhibitors often focus on optimization of potency as determined by IC50-values in biochemical assays. These assays do not allow the characterization of the binding activity (Ki) and… read more here.
Keywords: leaving group; diacylglycerol lipase; molecular dynamics; structure kinetics ... See more keywords
Liposomal Delivery of Diacylglycerol Lipase-Beta Inhibitors to Macrophages Dramatically Enhances Selectivity and Efficacy in Vivo.
Sign Up to like & getrecommendations! Published in 2018 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.7b00657
Abstract: Diacylglycerol lipase-beta (DAGLĪ²) hydrolyzes arachidonic acid (AA)-containing diacylglycerols to produce bioactive lipids including endocannabinoids and AA-derived eicosanoids involved in regulation of inflammatory signaling. Previously, we demonstrated that DAGLĪ² inactivation using the triazole urea inhibitor KT109… read more here.
Keywords: diacylglycerol lipase; inhibitors macrophages; delivery; lipase beta ... See more keywords