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The intracellular redox situation of
2020-04-02
The intracellular redox situation of MC3T3-E1 Trimidox after exposure with fluoride has been investigated and results revealed that the generation of ROS increased at a concentration-dependent manner, which indicated that NaF induced oxidative stress damage in MC3T3-E1 cells. Fluoride-mediated indu
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Finally we have determined for the first
2020-04-02
Finally, we have determined for the first time that aromatase enzyme activity is necessary to observe IGF-1-dependent Pleuromutilin sale receptor activation. Neuroestrogen synthesis has been shown to be important for the maintenance of synaptic spine density in hippocampal slice cultures (Kretz et a
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br Conclusions In this paper we describe the recombinant exp
2020-04-02
Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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Compound was advanced to a chronic efficacy study
2020-04-02
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, uk5099 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily for
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br Cysteine proteases as molecular targets for trypanosomati
2020-04-01
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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A summary of the drug CDK hydrophobic hydrogen bonding H
2020-04-01
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different VAS2870 the same value [77], which facilitates comparisons among different p
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Ung et al examined a
2020-04-01
Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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The question remained as to
2020-04-01
The question remained as to why hCrm1 was functional and mCrm1 was not in terms of Rev and HIV mRNA nuclear export, and previously we proposed three possibilities (Elinav et al., 2012). One was that human gonadotropin releasing hormone agonist had a positively acting factor that somehow stabilized
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Mouse Cyp a is a homologous isoform
2020-04-01
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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br GPCRs form heterotetramers In addition to homodimers and
2020-04-01
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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We hypothesized that the atopic phenotype
2020-04-01
We hypothesized that the atopic phenotype may be partially influenced by an altered binding and/or signalling due to the amino-acid substitution in the receptor protein. The principal aim of this study was to investigate the signalling mechanisms of the variants CysLT1-G300S and CysLT1-I206S induced
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In humans CYP A major isoforms of
2020-04-01
In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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Additionally of outmost important is the location
2020-04-01
Additionally, of outmost important is the location of the different CpG islands in relation to the transcription starting site (TSS) of the promoter as well as their interaction with transcription activators or repressors. It has been shown that methylation at the downstream region of the TSS in the
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73122 br Author Contributions br Funding Canadian
2020-04-01
Author Contributions Funding Canadian Institutes of Health Research, operating grant NMD-83126 and the internal funding from the National Research Council Canada, Charlottetown, PE, Canada. Disclosure Statement Acknowledgements Introduction Cholesterol is an essential structural comp
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In this report we established mouse models suitable
2020-04-01
In this report, we established mouse models suitable for human retinal cell transplantation by introducing phosphodiesterase 6B (Pde6b) mutant allele from retinal degeneration (rd) mouse models into NOG background. Pde6b (rd1) and Pde6b (rd10) mice are well-studied and frequently used animal models
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