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To test our refinement protocol we considered
2022-05-16

To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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br Brief overview of the glutamate system and rationale for
2022-05-16

Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric nor-Binaltorphimine dihydrochloride (GABA), the primary inhibitory ne
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It was previously proposed that
2022-05-16

It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the phosphodiesterase via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in th
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The findings in mice were
2022-05-16

The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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The caseins are a family of milk phosphoproteins whose biolo
2022-05-16

The caseins are a family of milk phosphoproteins whose biological function is to provide supersaturating concentrations of calcium, phosphates, and essential TWS119 mg to the neonate (Vonderhaar and Ziska, 1989). α- and β-caseins, the most abundant of the milk caseins, are described as calcium sens
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In terms of stimulation oxytocin dopamine noradrenaline
2022-05-16

In terms of stimulation, oxytocin, dopamine, noradrenaline, adrenaline and glucagon have all been reported to increase ghrelin secretion (Mundinger et al., 2006, Iwakura et al., 2011, de la Cour et al., 2007, Gagnon and Anini, 2013). Stimulatory effects on ghrelin secretion have also been observed w
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To improve the preferential GalR binding we
2022-05-16

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Liver is the house for
2022-05-16

Liver is the house for a variety of xenobiotic-metabolizing benzydamine that produce reactive oxygen species as well as reactive metabolites (Johansson et al., 2009; Noh et al., 2017; Puntarulo and Cederbaum, 1998). When the enzymes act upon pre- or pro-haptens, the chemicals would be activated to r
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G quadruplex DNA structures may exist in either
2022-05-16

G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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Having shown that some of
2022-05-16

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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In addition we assessed the viability
2022-05-16

In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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br Introduction Isoprenoid structures play an essential role
2022-05-16

Introduction Isoprenoid structures play an essential role in biology and over 30,000 natural products of this class are known (Greenhagen et al., 2003). Like other animals, insects require these compounds for many disparate processes, including electron transport (e.g., ubiquinones), protein glyc
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resveratrol Dysregulation of the HPA axis resulting
2022-05-16

Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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Last we demonstrate that the role
2022-05-16

Last, we demonstrate that the role of EZH2 as a transcriptional activator, with AR being a key target, coexists with its conventional catalytic role in gene repression and plays important oncogenic functions in AR-driven PCa (Figure 7F). Enzymatic EZH2 inhibitors such as EPZ and GSK126, although eff
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According to previous methods several mobile phase compositi
2022-05-16

According to previous methods, several mobile phase compositions and gradient programmes were assayed to get the best resolved peaks for HA and MHA [12], [13], [24]. Considering the slightly structural differences of the analytes, a mobile phase consisting in two eluents of different polarity and p
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