EC Number   |
Protein Variants |
Reference |
|---|
   3.1.1.116 | more |
a dominant negative Sp1 is shown to bind to the GC-box and to suppress DAGLalpha promoter activity specifically in NS cells |
761722 |
| 3.1.1.116 | more |
brain regional CB1 receptor-Gi/o-activity largely remains unaltered in DAGLalpha-knockout and DAGLb-knockout mice when compared to wild-type littermates. Following comprehensive pharmacological blockade of 2-AG hydrolysis, brain sections generate sufficient amounts of 2-AG to activate CB1 receptors throughout the regions endowed with these receptors. As demonstrated by LC/MS/MS, this pool of 2-AG is generated via tetrahydrolipstatin-sensitive enzymatic pathways distinct from DAGLalpha or DAGLbeta. Blockade of endocannabinoid hydrolysis by the irreversibly acting inhibitor MAFP evokes CP55,940-mimicking [35S]GTPgammaS binding responses throughout the CB1 receptor enriched brain regions of DAGLalpha-KO, DAGLbeta-KO, and WT mice brain sections. No statistically significant difference is observed in CP55,940-evoked regional CB1 receptor activity between DAGLb-KO and wild-type mice whereas in certain hippocampal regions of DAGLalpha-KO mice (hippocampus-overall, hippocampus-CA3 and hippocampus-dentate gyrus), sub-maximal concentrations of CP55,940 evoke a statistically significant increase in CB1 receptor activity. The observed labelling patterns evoked by both MAFP and CP55,940 are abolished with the CB1 receptor-selective antagonist AM251, confirming that responses are being mediated via the CB1 receptors. Comparison of 2-AG and anandamide (AEA, the other principal endocannabinoid) levels between unprocessed cryosections of DAGLalpha-KO, DAGLbeta-KO and wild-type mice brains |
761038 |
| 3.1.1.116 | more |
brain regional CB1 receptor-Gi/o-activity largely remains unaltered in DAGLalpha-knockout and DAGLbeta-knockout mice when compared to wild-type littermates. Following comprehensive pharmacological blockade of 2-AG hydrolysis, brain sections generate sufficient amounts of 2-AG to activate CB1 receptors throughout the regions endowed with these receptors. As demonstrated by LC/MS/MS, this pool of 2-AG is generated via tetrahydrolipstatin-sensitive enzymatic pathways distinct from DAGLalpha or DAGLbeta. Blockade of endocannabinoid hydrolysis by the irreversibly acting inhibitor MAFP evokes CP55,940-mimicking [35S]GTPgammaS binding responses throughout the CB1 receptor enriched brain regions of DAGLalpha-KO, DAGLbeta-KO and WT mice brain sections. No statistically significant difference is observed in CP55,940-evoked regional CB1 receptor activity between DAGLb-KO and wild-type mice whereas in certain hippocampal regions of DAGLalpha-KO mice (hippocampus-overall, hippocampus-CA3, and hippocampus-dentate gyrus), sub-maximal concentrations of CP55,940 evoke a statistically significant increase in CB1 receptor activity. The observed labelling patterns evoked by both MAFP and CP55,940 are abolished with the CB1 receptor-selective antagonist AM251, confirming that responses are being mediated via the CB1 receptors. Comparison of 2-AG and anandamide (AEA, the other principal endocannabinoid) levels between unprocessed cryosections of DAGLalpha-KO, DAGLbeta-KO and wild-type mice brains |
761038 |
| 3.1.1.116 | more |
construction of DAGLalpha knockout mice. Cholinergic innervation of CA1 pyramidal cells of the hippocampus is sensitive to the genetic disruption of 2-arachidonoylglycerol (2-AG) signaling in DAGLalpha null mice. A hybrid COS-7-cholinergic neuron co-culture system demonstrates that heterologous DAGLalpha overexpression spherically excludes cholinergic growth cones from 2-AG-rich extracellular environments, and minimizes cell-cell contact in vitro. CB1R-mediated exclusion responses lasts 3 days, indicating sustained spherical 2-AG availability. Extracellular 2-AG concentrations can be sufficient to activate CB1Rs along discrete spherical boundaries to modulate neuronal responsiveness. When co-culturing cholinergic neurons and COS-7-DAGLalpha cells for 1-3 days in vitro (DIV), parent COS-7 cells attract cholinergic neurites, which course on or along COS-7 plasmalemmas already by 1 DIV. Accordingly, the distance between cholinergic GCs and the opposing membrane of COS-7 cells gradually decreases as a factor of time. In contrast, 55.0% of cholinergic GCs are prevented from approaching the proximal COS-7 cell's plasmalemma upon DAGLalpha overexpression by 3 DIV. DAGLalpha overexpression spherically excludes cholinergic GCs, as reflected by their significantly increased distance to the surface of COS-7-DAGLalpha cells. DAGLalpha overexpression does not affect the angle at which GCs approach COS-7-DAGLalpha cells, the length of cholinergic neurites, the distance between cholinergic and COS-7 somata, and the survival of p75NTR1 neurons in vitro, excluding delayed morphogenesis or neuronal migration as confounding factors. Yet DAGLalpha overexpression no longer affects neurite growth, confining endocannabinoid action to affecting GC motility but no other forms of e.g. contact guidance. Focal and extracellular 2-AG can alter the positioning of cholinergic GCs. DAGLalpha overexpression in COS-7 cells is the only variable that contributes to the phenomena, supporting a role for intercellular 2-AG signaling |
762410 |
| 3.1.1.116 | more |
generation and cell-cycle analysis of enzyme deficient siDAGLA cells. Overexpression of DAGLA controls cellular proliferation in OSCC cells and clinical samples through cell-cycle progression. DAGLA-positive OSCC is correlated highly with the primary tumoral size. OSCC cells (KOSC-2 and Ho-1-N-1) are injected subcutaneously into the backs of female nude mice. The tumoral volume of the orlistat-treated group is clearly smaller than that of the control group. DAGLA inhibitor orlistat does not affect the body weight of the mice compared with the control group |
761044 |
| 3.1.1.116 | more |
generation of mutant Daglbeta-/- mice, analysis of the membrane proteome of transiently transfected HEK-293T cells overexpressing mouse DAGLbeta. Using a combination of inhibitors and knockout mice, strong evidence is generated that both DAGLbeta and PLA2G4A contribute to prostaglandin production in lipopolysaccharide-stimulated macrophages |
761970 |
| 3.1.1.116 | more |
genotyping, three SNPs in the DAGLA gene, rs879486(C_8906779_10), rs9735635(C_25958391_10) and rs3741252/Pro899Leu(C_25959741_10), are used for screening as tag SNPs across the gene. One of those SNPs, rs879486, is excluded from the final analysis in all the subjects, since rs879486 does not show association with alcoholism in the Japanese subjects. But associations are observed for the other two polymorphisms, rs9735635 and rs3741252/Pro899Leu, in the screening. Significant differences are found between those two polymorphisms and alcoholism in the Japanese population studied |
760319 |
