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Steady state mRNA levels of CYP A isoforms were not
2021-02-07
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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In conclusion our work provides the preclinical evidence sho
2021-02-07
In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer cycloheximide solubility and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly
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A similar pattern was observed for both
2021-02-05
A similar pattern was observed for both tissues of P. harpagos, evidencing the absolute predominance of acetylcholinesterase. As observed, no effects were attributed to Iso-OMPA. The hypothesis that the major cholinesterasic form is AChE was reinforced considering the higher hydrolytic activity, whi
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The modes of action of insecticides are
2021-02-05
The modes of action of insecticides are classified by the Insecticide Resistance Action Committee (IRAC) [6]. In this classification, a large proportion of insecticides are categorized as nerve- and muscle-targeting insecticides, which encompass GABACl antagonists (Group 2) and GluCl allosteric modu
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We recently employed a functional
2021-02-05
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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The indigenous populations living at high mountain
2021-02-05
The indigenous populations living at high mountain regions of the Himalayas represent successful human gyy to hypoxia. These populations have undergone selective positive natural selection over millennia across several genomic loci and exhibit unique respiratory, cardiopulmonary and haematological
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br Acknowledgements br Introductio http www apexbt com
2021-02-04
Acknowledgements Introduction TB is also widely prescribed as a stain to identify proteoglycans and glycosaminoglycans (GAGs) in agarose gel electrophoresis (Dietrich and Dietrich, 1976; Coulson-Thomas et al., 2015). In addition, as adjunct to a photodynamic antimicrobial chemotherapy assay, T
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This review focuses on the
2021-02-04
This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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What is the predominant mechanism underlying the benefits of
2021-02-04
What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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br Conflicts of interest br Acknowledgements
2021-02-04
Conflicts of interest Acknowledgements This work was supported, in part or in whole, by the grants from the National Natural Science Foundation of China (11802056, 11772088), the China Postdoctoral Science Foundation (2018M640904), and the Fundamental Research Funds for the Central Universitie
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The synthetic route chosen for the
2021-02-04
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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While we previously demonstrated that TraG is inhibited by s
2021-02-04
While we previously demonstrated that TraG is inhibited by specific transglycosylase inhibitors and that enzymatic activity is strongly reduced upon mutation of the potential catalytic core (Arends et al., 2013), the enzymatic mechanism of both domains was not assigned. Here, by mass spectrometry an
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It was hypothesized that if modafinil acts primarily via
2021-02-04
It was hypothesized that if modafinil acts primarily via a noradrenergic mechanism, Dbh −/− mice should be non-responsive since they completely lack NE. In contrast, if modafinil acts mainly through DA systems, these mice should be hypersensitive. Modafinil was tested in Dbh −/− mice using both loco
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Because of the complexity of DNA damage and
2021-02-03
Because of the complexity of DNA damage and its repair, several pathways are candidates in HN2-induced DPC repair. Considering the 23kDa molecular weight of MGMT, NER may be ineffective for MGMT-adduct removal. This presumption is supported by that the mRNA level of ERCC1, a core gene in NER pathway
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Fig D shows that E lagascae VIR E gives
2021-02-03
Fig. 2D shows that E. lagascae VIR E gives two species of radioactive TAG: one represents 45% of total labelled TAG and the smaller more-polar spot (15%) is probably derived from the endogenous 1,2-divernolin instead of the exogenous 1,2-diolein. In this case, the total scintillation counts were gre
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