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AGN 194310 Dormancy is a physiological state
2022-01-29

Dormancy is a physiological state when viable seeds do not germinate. Seed stratification, a commonly used technique, is used for dormancy removal and can be performed in moisture for an experimentally revealed time at warm or cold temperatures. All conditions depends on plant species (Dębska et al.
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Calcium mobilization FLIPR assay CHO
2022-01-29

Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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br FXR Agonists Azepinol b indole hEC
2022-01-29

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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Next we investigated the accumulation of H ribavirin in
2022-01-29

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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VEGFR Tyrosine Kinase Inhibitor II Several studies have foun
2022-01-29

Several studies have found decreased astroglial and neuronal cell numbers and VEGFR Tyrosine Kinase Inhibitor II damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000, G
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Whereas accurate measurement of glucagon in humans has been
2022-01-29

Whereas accurate measurement of glucagon in humans has been possible since the early 1950s proper measurements in rodents, have not. That said, plasma concentrations of glucagon have been reported in rodent studies [21] using C-terminal specific methods but what has been lacking is the secretory dyn
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The significance of A and tau as
2022-01-29

The significance of Aβ and tau as therapeutic targets is not only derived from pathological evidence of postmortem brain but also from biochemical analysis of cultured human neurons. This is largely based on the induced pluripotent stem cell (iPSC) technology that has been established to study Aβ, t
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The highest metabolic stability observed for compound k
2022-01-28

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intraveno
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In enzyme assays it is
2022-01-28

In enzyme assays, it is convenient to quantify the product formed in the enzyme reaction, where a decrease in the concentration of product indicates enzyme inhibition [35], [36], [37], [38]. In the present study, substrates were carefully chosen so that they are specific to each enzyme. Known natura
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Histone acetylation is regulated by
2022-01-28

Histone acetylation is regulated by two groups of enzymes, histone acetyltransferases (HATs) and deacetylases (HDACs), with antagonizing functions (Wang et al., 2009b). Among members of HATs, p300 and CBP are homologous. Both are global transcriptional co-activators (Ogryzko et al., 1996), and play
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In summary P P macrocyclization proved to be
2022-01-28

In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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Mathematical models play an important role in understanding
2022-01-28

Mathematical models play an important role in understanding and predicting the dynamic process of HBV infection. In the 1990s, Nowak et al. proposed a basic model to analyze the effect of antiviral treatment on reducing viral loads (Nowak et al., 1996). Since then, many different mathematical models
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CONUT score is an effective detector of predicting
2022-01-28

CONUT score is an effective detector of predicting OS and RFS in HCC patients. We found that patients with a damaged immune-nutrition status had significantly poor OS and RFS. Our initial literature review also retrieved other studies evaluating the survival of HCC patients using CONUT score [36,48,
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The gsnor ko plants contain elevated amount of low and
2022-01-28

The gsnor-ko plants contain elevated amount of low and high molecular weight S-nitrosothiols (SNO) indicating that GSNOR activity controls the level of both GSNO and indirectly protein-SNOs [13], [17], [18]. GSNOR deficiency has been shown to cause pleiotropic plant growth defects, impaired plant di
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Introduction Glycogen synthase kinase GSK is
2022-01-28

Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and cytokine receptor is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolidatio
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