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Recently accumulated evidence has revealed a close link of F
2022-03-25

Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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Isoniazid australia Contrary to the transient nature of sign
2022-03-24

Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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EZH interaction with HADC and HDAC through the EED subunit
2022-03-24

EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic Tylosin
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Zanamivir Over the years a number of studies have
2022-03-24

Over the years, a number of studies have reported results concerning the behavior of the two endothelin receptor subtypes, ETA and ETB, that do not fit the classical model of two G protein-coupled receptors acting independently of one another. For example, in the rat anterior pituitary gland, both E
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Histone demethylases are involved in the
2022-03-24

Histone demethylases are involved in the transcriptional output of the AR and hypoxia signaling pathways, and thus contribute to prostate cancer development [12]. For example, the histone demethylase KDM3A serves as a transcriptional coactivator of HIF1α and AR in regulation of their target genes [1
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br Acknowledgments This work was supported by
2022-03-24

Acknowledgments This work was supported by the National Natural Science Foundation of China (31100111), the Nature Science Research Project of Anhui Province (1508085MC43), the subject construction project from Anhui Academy of Agricultural Sciences (14A1110). We would like to acknowledge the tec
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br Conclusion Leukocytes adhesion to endothelial cells is on
2022-03-24

Conclusion Leukocytes adhesion to endothelial cells is one of the most critical event in the inflammatory response. In presented paper using a relevant model of adhesion we have demonstrated that histamine influence eosinophils adhesion to endothelium. This effect appears to be mediated by H4 his
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Multi targeting agents are of
2022-03-24

Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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microRNAs miRNAs of approximately nucleotides play vital rol
2022-03-24

microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme
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Lastly certain populations of immune cells may be
2022-03-24

Lastly, certain populations of immune cells may be Hh responsive. Although PC have not been demonstrated in healthy liver-resident macrophages or lymphocytes, macrophages in injured livers have been shown to produce Hh ligands[58], [100], [101] and treating liver-derived macrophages with neutralisin
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In human platelets only and
2022-03-24

In human platelets, only α1 and β1 isoforms of sGC are expressed in equimolar concentrations (3700 copies for β1, and 3500 copies for α1 per platelet) [57] [62]. sGC, is usually a heterodimer and contains heme as cofactor which is required for high-affinity NO binding and stimulation of its activit
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To investigate the simultaneous effects of possible confound
2022-03-24

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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The recently de orphaned G protein coupled receptor GPCR
2022-03-24

The recently de-orphaned G-protein coupled receptor (GPCR), GPR55, is activated endogenously by L-α-lysophosphatidylinositol (LPI), a lipid signaling molecule, as well as N-arachidonoyl glycine (NAGly) and numerous endo, phyto, and synthetic cannabinoids (Oka et al., 2007, Henstridge et al., 2010, H
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As preclinical toxicity and efficacy both appear to
2022-03-24

As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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Fatty acids have been repeatedly
2022-03-24

Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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