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High throughput screening HTS of
2020-05-25
High throughput screening (HTS) of the AstraZeneca LY2940680 collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and was
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br Methods and materials br Cyclooxygenase COX is
2020-05-22
Methods and materials Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic dca to sdf receptor to prostaglandin, prostacyclins and thromboxanes., , , Two distinct isoforms of COX were initially discovered: COX-1 is a constitutive, housekeeping enzyme that is expre
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br Results br Discussion This study assesses
2020-05-22
Results Discussion This study assesses impacts of HLA-DPB1 and CMV reactivation on GVHD, relapse, and OS after allo-HSCT. Here we demonstrate that HLA-DPB1 and CMV reactivation both increase aGVHD risk independently. Consistent with reported data, we show that HLA-DPB1 mismatching is associate
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ERR induces the expression of P c in MA cells
2020-05-22
ERRγ induces the expression of P450c17 in MA-10 cells and in mouse primary Leydig cells (Fig. 2). Deletion mutant analysis of putative ERRγ-binding sites in the P450c17 promoter suggested that only the proximal third site located between −269 bp and −136 bp within the P450c17 promoter is functional
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Despite the significant increase in Bdnf mRNA levels after
2020-05-22
Despite the significant increase in Bdnf1 mRNA levels after DNMT inhibition, the expression of Bdnf4 and Bdnf9 was unaltered. It is particularly surprising that Bdnf4 is not affected by the DNMT inhibitor, as the promoter of the Bdnf4 exon is known to be susceptible to epigenetic changes (Kotera et
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Studies of Jelski and Szmitkowski
2020-05-22
Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between PFI 3 of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activity in cancer cells are
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Substitutions on the benzene ring
2020-05-22
Substitutions on the benzene ring of the phenyl acetic CTX0294885 moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the aryloxy
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The conventional medical therapy for IBD consists
2020-05-22
The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f
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Finally the recent work to define the microcircuitry of the
2020-05-22
Finally, the recent work to define the microcircuitry of the central amygdala and the role of specific cell populations in fear conditioning can stand as a useful model for advances in preclinical alcohol research. To date, the role of the amygdala in alcohol-related behaviors, and reward-related be
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tranylcypromine mg Our results show that COX and
2020-05-21
Our results show that COX-1 and COX-2 inhibition improve cognitive performance and decrease the neuronal insult during HH. However, when a neuroinflammatory response was observed, COX-1 inhibition was more effective than COX-2 inhibition at reducing microglial activation and augmenting pro-inflammat
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dizocilpine br Epac in cardiovascular pathophysiology Epac o
2020-05-21
Epac in cardiovascular pathophysiology Epac orchestrates signaling actors that regulate fundamental cellular functions and general biological effects. However, some important gaps still remain in the knowledge of the physiopathological role of Epac in the heart. So far, Epac has been implicated i
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In bone PGE exerts both
2020-05-21
In bone, PGE2 exerts both anabolic and catabolic effects [6], [7], [8], [9]. Administration of PGE2 to mice lacking each of the four prostanoid receptors identified EP4 as the primary mediator of PGE2-induced bone formation [10]. While the role of EP1 in osteoblastic differentiation and bone metabol
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br Conclusions We can conclude
2020-05-21
Conclusions We can conclude that Arg293 is important but not indispensable for MeGlcA recognition by EcXyn30A since the R293A variant still retains activity and preference for MeGlcA-substituted substrates. The substrate specificity of GH30_8 glucuronoxylanases is most probably determined by an o
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br Materials and methods br Results br
2020-05-21
Materials and methods Results Discussion Although some conditioning therapies have provided satisfactory clinical outcomes, mammalian species have little or no ability to replace injured cardiac tissue [34]. Therefore, therapeutic strategies based on the prevention, rather than treatment af
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br Acknowledgments This work was supported
2020-05-21
Acknowledgments This work was supported by a grant from the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquitin (Ub) has been considered as one of the most import
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