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In an effort to further improve the intrinsic
2021-11-08

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl group
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Indeed GSTP mRNA appears to be already highly stable in
2021-11-08

Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia done with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular model and the exp
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To facilitate the development of novel diagnostic and therap
2021-11-08

To facilitate the development of novel diagnostic and therapeutic interventions in NASH, a plethora of animal models have been used to identify molecular targets that are involved in the onset and progression of NASH. In view of recent advances in the understanding of the pathogenesis of NASH and pr
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To determine the functional consequences of HIV
2021-11-08

To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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Cichlasoma dimerus as most teleost fish species present neur
2021-11-08

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most eph receptor species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (Gonzál
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Meanwhile a myriad of studies using tissue and
2021-11-08

Meanwhile a myriad of studies using tissue- and cell type-specific deletion of GPX4 have provided evidence that various tissues/cells, such as distinct neuronal cell populations including glutamatergic neurons of the forebrain [24], Purkinje cells of the cerebellum [74] and motor neurons [75], photo
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449 br Materials and methods br Results br Conclusions
2021-11-08

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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BIBW 2992 The lower number of samples
2021-11-08

The lower number of samples tested for the comparison between cobas 4800 HIV-1 and RealTime HIV-1, especially at or below 50 copies/mL (Table 6), could limit our ability to discern a difference in the ability of the various assays to identify patients with virological failure. However, the 95% CI ar
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br Although there are growing bodies of
2021-11-08

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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Background Chronic hepatitis C virus HCV infection is a majo
2021-11-08

Background Chronic hepatitis C virus (HCV) infection is a major public health concern, with 71 million people infected worldwide [1]. Treatment options have improved with the availability of interferon-free direct-acting antiviral (DAA) therapies with cure in >95% of people [2]. However, broadening
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Initially the synthesized compounds from were evaluated for
2021-11-06

Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic liothyronine sodium having si
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In conclusion we demonstrated that the atypical high basal
2021-11-06

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 Indirubin results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl− loc
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Because of the relationship between carbohydrate consumption
2021-11-06

Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of 6063 through analysis by glycemic index (GI) and Englyst assay, for example (Englyst, Kingman, & Cu
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Many natural flavonoids have been identified as influencing
2021-11-06

Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la
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To understand the impact of alterations in brain
2021-11-06

To understand the impact of alterations in BCATc Inhibitor 2 zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-released with
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