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The first mammalian mutation linked to CR was identified
2020-02-17
The first mammalian mutation linked to CR was identified in golden hamsters (Mesocricetus auratus). The mutation was an autosomal allele first described in the late 1980s [8] and was identified using positional cloning [9]. These animals displayed a shortened period length (20h in homozygous animals
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Two isoforms of intracellular ER ER and ER after
2020-02-17
Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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Our observation that nuclear but not
2020-02-17
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant crm1 whereas cytoplasmic EP4 was commonly observed [13]. While G protein-coupled recepto
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br Summary and perspectives In recent decades enormous advan
2020-02-17
Summary and perspectives In recent decades, enormous advances have been achieved in the development of enzyme-activatable imaging probes, enabling the accurate detection of enzyme activity in vivo to better understand the biological function of enzymes in disease processes. Activatable probes are
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In principle in vitro techniques for assessing enzyme induct
2020-02-17
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized Reparixin L-lysine salt lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with rec
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Our previous studies indicate that EBI is involved in
2020-02-15
Our previous studies indicate that EBI2 is involved in the regulation of pro-inflammatory responses and inter-cellular communication under pathophysiological conditions such as LPS challenge (Rutkowska et al., 2016b). The data showed that media taken from LPS stimulated astrocytes induces macrophage
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We have previously reported DAPK inhibitors discovered throu
2020-02-14
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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br Results and discussion br Conclusions An
2020-02-14
Results and discussion Conclusions An optimization study of the dipeptidyl enoates was performed by chemical structure modifications (Fig. 5). Compound FGA50 displaying R configuration at C-3 was more active than its epimer FGA40. Two modifications of the chemical structure of FGA50 were done:
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br Materials and methods br Results Metabolic stability of c
2020-02-14
Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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Behaviors were compared between saline and amphetamine pre
2020-02-14
Behaviors were compared between saline and amphetamine pre-treatment groups at 24h and 2 weeks following the last treatment, or between pre-treatment groups that received vehicle or ASV-30 infusions, using separate two-way ANOVAs. Significant effects were analyzed further using Student–Newman–Keuls
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br Conflicts of interest br
2020-02-14
Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest
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In the particular case of metals several authors
2020-02-14
In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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It should be noted that not only glyphosate
2020-02-14
It should be noted that not only glyphosate but E2 at the same concentration range (10−11-10−7 M) also showed similar effects on the expression of the Cy3 maleimide (non-sulfonated) regulating proteins. Furthermore, we could not see a significant difference among this concentration range of glyphosa
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br Conflict of interest statement br Introduction
2020-02-14
Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle
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Verapamil a calcium channel blocker used clinically as a
2020-02-14
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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