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LB-100 br Acknowledgments This research was supported
2021-09-14

Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio
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GIPR genes were not found in any of the
2021-09-14

GIPR genes were not found in any of the available bird genome as well as the genomes of several species of fish (Tables S3 and S4). The genomic neighborhoods surrounding the GIPR genes in species that have them was generally conserved (see Fig. 8), and like GLP2R, those fish that did have a Gipr gen
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Cx is the major molecule involved in the dynamic
2021-09-14

Cx43 is the major molecule involved in the dynamic life cycle of GJIC (Cusato et al., 2006). Initially generated Cx43 exist in the cytoplasm and correctly transfer it to the plasma membrane during its life cycle (Ji et al., 2018). To understand the toxic effects of MC-LR on GJIC, Cx43 localization w
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hydroxylase Regarding IAV types of hemagglutinin and types o
2021-09-14

Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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L-817,818 The normal function of the FBPase
2021-09-14

The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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Recently considerable effort has been invested
2021-09-14

Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most w
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The site of paracetamol action remains controversial Some
2021-09-14

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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Mammals adapt to prolonged periods of food scarcity by relea
2021-09-14

Mammals adapt to prolonged periods of food scarcity by releasing FFAs from adipose tissue and transforming them into energy-rich ketone bodies that are used as fuel by brain, muscle, and other organs (Kersten, 2014, Grabacka et al., 2016). Ketogenesis occurs primarily in hepatocytes, but its rate is
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Obesity is one of the
2021-09-14

Obesity is one of the worldwide concerns, with high prevalence and adverse effects on human health and life expectancy. According to the World Health Organization (WHO), obesity is defined as abnormal or excessive fat accumulation in the body with body mass index (BMI) of 30 or more. Obesity increas
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Biochemical and genetic studies indicate that the
2021-09-14

Biochemical and genetic studies indicate that the endosomal sorting complex required for transport (ESCRT) machinery is crucial for Hh exovesicle packaging and morphogen gradient function 39., 43., 44.. In vertebrates, ESCRT proteins promote the release of Shh exovesicles to maintain progenitor cell
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The replacement of the P butyl urea
2021-09-14

The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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Wortmannin The selection of mutations in vivo with
2021-09-14

The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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An alternative approach to improving pharmacokinetic profile
2021-09-14

An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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br Glycoprotein Production br Strategies to Obtain Glycoprot
2021-09-14

Glycoprotein Production Strategies to Obtain Glycoprotein Compositional Homogeneity Glycoproteins are modified by glycosyltransferases and glycosylhydrolases in the ER and Golgi; however, the degree of remodeling for each glycan on each protein is not explicitly defined by a template (Moremen
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br Materials and Methods br Results br Discussion A model
2021-09-13

Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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