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During the course of the development of
2021-09-17
During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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Studies regarding secretase nowadays aim at
2021-09-17
Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran
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Based on the previous report that FXR
2021-09-17
Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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There are many kinds of neurological disorders and
2021-09-17
There are many kinds of neurological disorders and neuropsychiatric diseases, like stroke, dementia, schizophrenia and so on. Among these disorders, the most important reason for choosing depression in our study is that FXR has already been demonstrated to regulate the function of CREB, which is clo
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dopamine-2 receptor antagonist CC is a widespread disorder
2021-09-17
CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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Lenvatinib is an orally available multi targeted tyrosine ki
2021-09-17
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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Moreover studies on subcellular localization of FBPase in ca
2021-09-17
Moreover, studies on subcellular localization of FBPase in carp heart and smooth muscle revealed nuclear localization of the enzyme. Previously, we have unequivocally demonstrated the presence of FBPase in the nuclei of mammalian cardiomyocytes (Gizak and Dzugaj, 2003) and myocytes (Gizak et al., 20
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234 2 Despite these data implicating Kdm b
2021-09-16
Despite these data implicating Kdm6b as a positive regulator of neuronal differentiation, and surprisingly, given the evidence that germline knockouts die perinatally due to an inability to breathe, the brains of Kdm6b knockout mice are remarkably normal in gross morphology [26,]. Interestingly, Kdm
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The H R antagonist cimetidine Tagamet became the
2021-09-16
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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The second class of proteins necessary for maintaining
2021-09-16
The second class of proteins necessary for maintaining nor-Binaltorphimine dihydrochloride dynamics is chromatin modifiers, which are considered ‘writers’ and ‘erasers’ and are responsible for modifications of histone N-terminal tails. These post-translational modifications can have direct or indir
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Egypt has the highest prevalence of HCV
2021-09-16
Egypt has the highest prevalence of HCV worldwide with almost 20% of the population being infected. The HCV subtype 4a belonging to genotype 4 (HCV-4) is the most common genotype in Egypt [25], [26], [27], [28]. The sequence of the NS5A/NS5B junction for the Egyptian genotype 4 is Glu-Asp-Val-Val-Cy
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Egypt has the highest prevalence of HCV
2021-09-16
Egypt has the highest prevalence of HCV worldwide with almost 20% of the population being infected. The HCV subtype 4a belonging to genotype 4 (HCV-4) is the most common genotype in Egypt [25], [26], [27], [28]. The sequence of the NS5A/NS5B junction for the Egyptian genotype 4 is Glu-Asp-Val-Val-Cy
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LY 235959 Urinary As species monomethylated MMAV percentage
2021-09-16
Urinary As species monomethylated (MMAV) percentage might increase and As species dimethylated (DMAV) percentage might decrease with increasing As exposure dosage (Lindberg et al., 2008). The limited methylation capacity associated with increased of As exposure dosage might probably explained throug
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br Acknowledgments br Introduction Guanosine cyclic monophos
2021-09-16
Acknowledgments Introduction Guanosine 3′,5′-cyclic monophosphate (cGMP) is a signaling molecule with key roles in diverse (patho) physiological responses and processes in numerous prokaryotes and all eukaryotes. The number of reports stating the role of cGMP in different processes in plants i
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To investigate the simultaneous effects of possible confound
2021-09-16
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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