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Two different genes encode GSK isoforms
2022-10-10
Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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KYNA has been shown to regulate
2022-10-10
KYNA has been shown to regulate iNKT cytokine release (Fallarini et al., 2010) and at high concentrations to reduce LPS-induced TNFα release from cultured peripheral blood mononuclear nucleoside transporters (Wang et al., 2006). Our results show that elevating KYNA to “exercised” levels is sufficie
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Among the various delivery strategies
2022-10-10
Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for a
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Due to the requirement of high end methods such as
2022-10-09
Due to the requirement of high-end methods such as total internal reflection fluorescence (TIRF) microscopy to visualize lipid rafts, isolation procedures are employed to study the protein content of lipid rafts [29]. The different methods utilized to isolated lipid rafts and other low density micro
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PSB 0777 ammonium salt Besides the described effects on gros
2022-10-09
Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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In order to test whether the enhanced hyperpolarization
2022-10-09
In order to test whether the enhanced hyperpolarization in the presence of increasing amounts of extracellular Ca2+ could be due to an ionophore effect of NS309, red cell uptake of 45Ca and partition of 45Ca into a water/n-octanol phase +/−100 μM NS309 were determined. However, no indication of iono
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G quadruplex DNA structures may exist in either positive or
2022-10-08
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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High lipophilicity of seems to cause poor PK profiles
2022-10-08
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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So what makes a FFAR agonist different and interesting As
2022-10-08
So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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In the present study VTE recurrence occurred in a non
2022-10-08
In the present study, VTE recurrence occurred in a non-cancer patient during edoxaban administration, representing recurrence rates of 1.7% in non-cancer patients and 0.8% in all patients. In a sub-analysis of cancer patients [27] and the main analysis [19] in the HOKUSAI-VTE trial, recurrent VTE oc
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This study appears to provide an additional example albeit
2022-10-08
This study appears to provide an additional example, albeit an unanticipated one, of the importance of renal ETB receptor function in the normal control of blood pressure and salt and water homeostasis. ETB receptor-deficient rats, collecting duct-specific ETB receptor knockout mice, and rats chroni
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GSK dimethylpiperidin yl butoxy phenyl piperidine carbonyl
2022-10-08
GSK-835726 (3-[4-[4-[4-[4-(3,3-dimethylpiperidin-1-yl)butoxy]phenyl]piperidine-1-carbonyl]naphthalen-1-yl]propanoic acid) is a dual H1/H3 receptor antagonist with the potential to be used in allergic rhinitis. Likewise GSK-1004723, the drug-likeness criteria have not been passed by this drug candida
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In our previous studies examining erectile responses in sGC
2022-10-04
In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogenou
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The ketone body receptor HCA
2022-10-04
The ketone body receptor HCA2 is most likely not active under normal conditions, since local levels and plasma levels of ketone bodies such as β-HB are too low to activate the receptor. However, overnight fasting or prolonged starvation results in plasma levels of the ketone body in the millimolar r
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INTRODUCTION Scar formation and tissue regeneration
2022-10-04
INTRODUCTION Scar formation and tissue regeneration are opposite results of the wound healing process. Although fibrosis is more common after skin injury, full skin regeneration results in complete replacement of adnexa and function. Examples of tissue regeneration in mammalian systems include annu
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