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Further research should indeed focus on
2021-12-22

Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t
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In conclusion a series of new carboxamido aryl isoxazoles wa
2021-12-21

In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed
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Long term effects of prolonged darkness
2021-12-21

Long-term effects of prolonged darkness on specific physiological activities were also monitored at different leaf positions. Basically, stomatal conductance and CO2 assimilation were different at various leaf stages and were decreased or inhibited significantly within 24 h in all leaf positions upo
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Despite the rapid development of synthetic ligands
2021-12-21

Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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br Synthetic Antagonists for FFA To date
2021-12-21

Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this
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Moreover we revealed that alanine
2021-12-21

Moreover, we revealed that β-alanine and taurine, a structural analog of β-alanine, have different receptor affinity in the SG neurons of the spinal dorsal horn. Additionally, previous studies indicate that taurine regulates nociceptive information at the spinal cord level, and we have previously de
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The general synthetic routes leading to
2021-12-21

The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic XL184 analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth mentioning that
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Caffeine decreased EAAT and EAAT expression levels in P
2021-12-21

Caffeine decreased EAAT1 and EAAT2 NVP-BKM120 levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resume, our da
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The previous studies focused on
2021-12-21

The previous studies focused on the regulation of GK activity by nutrients directly or nutritional hormones (Panserat et al., 2014), there was still a lack of studies paid attention to GK both in activity level and transcriptional level. Besides, the GK regulation by dietary ion channel has been de
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A group of small molecule
2021-12-21

A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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Based on the collective experience to
2021-12-21

Based on the collective experience to date, it is likely that a much more comprehensive assessment of GSI selectivity for inhibition of multiple substrates, as well as biomarkers to track inhibition of non-APP substrates in vivo will be needed to support future efforts to develop substrate selective
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FBPase deficiency is a very rare inborn error
2021-12-21

FBPase deficiency is a very rare inborn error of fructose 2-Deoxyadenosine 5-diphosphate of autosomal recessive inheritance. This disorder usually occurs in the first year of life through ketotic hypoglycemia and lactic acidosis triggered by catabolic episodes such as prolonged fasting or febrile i
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br Experimental procedures br Results br Discussion
2021-12-21

Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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The organ culture method has previously shown
2021-12-20

The organ culture method has previously shown to be a suitable model for investigations of receptor upregulation on vascular smooth muscle cells (Adner et al., 1996). In our study, the organ culture method was applied in order to examine whether LPS from P.g. was capable of altering the gene express
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br Results br Discussion Our current study
2021-12-20

Results Discussion Our current study demonstrates that the sustained activation of Yap overrides the p27-mediated checkpoint, at least in part, through the degradation of FoxO family proteins, allowing polyploid cells to proliferate inappropriately with mitotic defects and resulting in centros
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