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br Chemistry Analog has been previously reported by our
2021-11-09

Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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The overall very satisfactory potency profile of compounds a
2021-11-09

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic p-selectin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sen
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br Melanoma cell lines There is suggestive epidemiological e
2021-11-09

Melanoma cell lines There is suggestive epidemiological evidence that omega-3 PUFA can be preventative against melanoma, although the mechanisms of this relationship has not been extensively investigated [65], [66]. A 2014 study demonstrated that DHA inhibited cell proliferation in vitro in A2058
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br Materials and methods This is
2021-11-09

Materials and methods This is a retrospective case-controlled study. The cases were selected based on the presence or absence of preeclampsia. Women enrolled in the study delivered singleton pregnancies at our institution from June 2003 to July 2004. Preeclampsia is defined as elevated blood pres
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The iAs mainly metabolized in the liver to generate MMA
2021-11-09

The iAs mainly metabolized in the liver to generate MMA and DMA. DMA, MMA and iAs were excreted through the urine (Khaleghian et al., 2014; Wei et al., 2017a). Pearson correlation coefficient was used to explore associations between concentrations of three arsenic species in urine and gene expressio
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In the FARM motifs of GGPPSs hydrophobic amino acids
2021-11-09

In the FARM motifs of GGPPSs, hydrophobic a66 australia are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase (G
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Thus from this preliminary study a working model of HIV
2021-11-09

Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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The more important effect of pitolisant is related
2021-11-09

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced PD 0332991 release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers
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G protein coupled receptors GPCRs constitute
2021-11-08

G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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br Gastrointestinal peptides and intestinal health Gastroint
2021-11-08

Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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Moreover there is a third possible GnRH agonist
2021-11-08

Moreover, there is a third possible GnRH agonist target – the endometrium. The human endometrium has been shown to express high levels of both GnRH and GnRH receptors (Maggi et al., 2016), and GnRH agonists affect the function of the urokinase-type plasminogen activator/plasminogen activator inhibit
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Acknowledgements br Introduction The neurotransmitter glycin
2021-11-08

Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is
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br Regulation of Glu transporters The pivotal
2021-11-08

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino rxr receptor calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcri
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br Materials and Methods br Results
2021-11-08

Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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br Acknowledgements br Introduction Aminoacyl tRNA
2021-11-08

Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino ML324 and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid is transferred
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