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In order to consolidate our genetic
2022-02-22

In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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Introduction Glucose dependent insulinotropic polypeptide GI
2022-02-22

Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G
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These reports have gradually established G quadruplex bindin
2022-02-22

These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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Introduction Ventilator induced lung injury VILI is the most
2022-02-21

Introduction Ventilator-induced lung injury(VILI) is the most common complication in the mechanical ventilation in clinic. Repetitive opening and closing of more at high pressures during artificial ventilation would generate shear stress and then lead to the damage of cell junction and dysregulati
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More specific quantitative assays for DiXaIs are based on
2022-02-21

More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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br Although there are growing
2022-02-21

Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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The transcription factor Nrf is a master
2022-02-21

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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The translation of the HCV genomic RNA is initiated
2022-02-21

The translation of the HCV genomic RNA is initiated in a different manner, referred to as internal initiation: the 40S subunit directly forms a binary complex with the HCV genomic RNA via an internal RNA sequence called IRES, which is located in the 5′-UTR (Pestova et al., 1998, Tsukiyama-Kohara et
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br Conflict of interest statement br
2022-02-21

Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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br Glucocorticoid receptor and metabolic syndrome GCs acting
2022-02-18

Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g
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AACOCF3 Clinical trials of all GSIs
2022-02-18

Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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Activation of FXR or TGR inhibits
2022-02-18

Activation of FXR or TGR5 inhibits inflammatory response via repressing NF-κB activity [1]. FXR is not expressed or expressed at a very low level in macrophages [45] (data not shown), but highly expressed in hepatocytes. In contrast, TGR5 is expressed in macrophages but not in hepatocytes. Our data
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br Acknowledgments This research was supported in part by Na
2022-02-18

Acknowledgments This research was supported in part by National Institutes of Health IDeA Program COBRE grant GM110732; a USDA National Institute of Food and Agriculture Hatch project; and the Montana State University Agricultural Experiment Station. Introduction Propofol (2,6-Diisopropylphen
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Tail group SAR of the imidazole derived analogs is
2022-02-18

Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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BMH-21 receptor Although our knowledge of how FAs affect
2022-02-18

Although our knowledge of how FAs affect GLP-1-producing L-cells is sparse and incomplete, increased intracellular ceramide [6], ER stress [12], and increased production of ROS [9] are indicated mediators of the lipotoxicity induced by SFA (16:0). However, the role for/interaction between these medi
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