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br Conclusions br Declaration of interest br Acknowledgement
2020-03-16
Conclusions Declaration of interest Acknowledgements Introduction Uncorrected obesity has been a major health problem and the prevalence of obesity is fast rising reaching an epidemic proportion [[1], [2], [3]]. Ample of clinical and experimental evidence has suggested that obesity leads
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Moreover Hypericum perforatum L was also included in the
2020-03-16
Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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br Conflict of interests br Introduction Ubiquitylation is
2020-03-16
Conflict of interests Introduction Ubiquitylation is a post-translational modification which impacts almost every biological process in the cell. Dysregulation of the ubiquitylation pathway is associated with several diseases, including cancer, neurodegenerative disorders, and immunological dy
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In contrast to SQLE HMGCR could be efficiently degraded
2020-03-16
In contrast to SQLE, HMGCR could be efficiently degraded in multidrug resistant lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our
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This pathway appears to have importance in
2020-03-16
This pathway appears to have importance in epilepsy. DGKε(−/−) mice had significantly fewer motor seizure and epileptic events compared with DGKε(+/+) mice [18]. This could be explained by the fact that in the knockout mice a greater fraction of the SAG would be converted to 2-AG. 2-AG itself is kno
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Midazolam oral clearance is used for
2020-03-16
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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In rats exposed to day of nicotine withdrawal h
2020-03-16
In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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In cholesterol synthesis HMG CoA reductase
2020-03-16
In cholesterol synthesis, HMG-CoA reductase is the rate limiting step in cholesterol biosynthesis. Statins or HMG-CoA reductase inhibitors are commonly used for management of hypercholesterolemia. The presence of an HMG-like moiety on these drugs allows them to competitively bind to the catalytic do
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NPC L NPC Niemann Pick C
2020-03-16
NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol ldk378 from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cholesterol-lower
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Another milestone in the field is the de
2020-03-16
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of Nuclear/Cytosol Fractionation Kit , it has been widely applied as a useful chemical probe to discriminate EPAC related s
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Molidustat In the phase I AURA trial
2020-03-13
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for Molidustat 19 deletions, 86% for L858R a
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br Experiments and Methods br
2020-03-13
Experiments and Methods Results and Discussion Conclusions Here, the interactions between two newly-synthesized carbazole derivative—cationic δ,δ′‑diazacarbazoles and DNA were characterized by several spectroscopic means, including UV–Vis and fluorescence, AFM and fluorescence imaging. The
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br Materials and methods br Results br
2020-03-13
Materials and methods Results Discussion In general, CI symptoms are often visible only after the chilled products have been removed from coolstore to a warmer temperature (Schirra and Cohen, 1999). However, in the present work, \'satsuma’ mandarin fruit stored at 2°C showed chilling sympto
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br Conflict of interest br Acknowledgments We thank Jianru Z
2020-03-13
Conflict of interest Acknowledgments We thank Jianru Zuo (Institute of Genetics and Developmental Biology, Chinese Academy of Sciences, Beijing, China) for providing fbr11-1 seeds. We are grateful to Carol MacKintosh and the DSTT at the University of Dundee (UK) for anti-RD21 antibodies. This
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(±)-J 113397 van Linden et al developed a comprehensive
2020-03-13
van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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