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In this study we have investigated
2022-08-16
In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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br Materials and methods br Results br Discussion In
2022-08-16
Materials and methods Results Discussion In this study, we identified a novel AMP scolopendrasin X from Scolopendra subspinipes mutilans through genome analysis. Scolopendrasin X stimulated neutrophil activity, resulting in calcium increase, chemotactic migration, and superoxide anion produ
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Next we were interested in replacing the
2022-08-16
Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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LSD also contributes to the regulation of specific programs
2022-08-16
LSD1 also contributes to the regulation of specific programs of gene expression in postmitotic, fate-committed neurons. Perhaps its most specialized role is in the complex series of epigenetic regulatory events that permit each olfactory sensory neuron to express one and only one of the thousands of
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Currently the computational chemical biology has been applie
2022-08-16
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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bioactive australia br TGR agonists current developments and
2022-08-15
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and bioactive australia of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutica
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br Introduction Cell surface receptors are central to the
2022-08-15
Introduction Cell surface receptors are central to the interaction of cells with their surroundings and play an important role in determining functional responses. These receptors are integral membrane proteins responsible for the binding of extracellular signaling molecules and transduction into
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In parallel we were also preparing and evaluating other pipe
2022-08-15
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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If some of the experimentally determined
2022-08-15
If some of the experimentally determined tRNAGlu identity elements are unique to E. coli, then there also must be some unique phylum-specific residues in the corresponding GluRS (E. coli in particular, and proteobacteria in general) as well. In this paper we focus on identifying such residues in E.
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Moreover to evaluate the properties of
2022-08-15
Moreover, to evaluate the properties of immobilized β-glucosidase further, the anti-protease test was also carried out. The result showed that the residual activity of the β-glucosidase@ZIF-8 was higher than that of the nano-SiO2@β-glucosidase and free β-glucosidase. Because free β-glucosidase and t
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Given the proposed importance of conformational dynamics to
2022-08-13
Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of TP-0903 binding, using changes in the enzyme's intrinsic fluorescence
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The Hedgehog Hh pathway is linked to
2022-08-13
The Hedgehog (Hh) pathway is linked to the development of several types of epithelial cancers (Rubin and de Sauvage, 2006). A paracrine mechanism has been implicated in CAF activation, with Hh ligands secreted by cancer cells activating the glioma-associated transcription factors (Gli) in surroundin
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br Preclinical development of GIP agonists
2022-08-13
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a
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BHQ In order to test whether the enhanced hyperpolarization
2022-08-13
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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Enhancer of Zeste Homolog EZH is a core component
2022-08-13
Enhancer of Zeste Homolog 2 (EZH2) is a core component of the Polycomb Repressive Complex2 (PRC2) which also includes SUZ12 and EED. PRC2 represses gene transcription through trimethylation of Lys27 of histone H3 (H3K27), and contribute to the maintenance of cell identity, C34 regulation and oncoge
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