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To identify structurally novel autophagy inhibitors a medium
2022-07-12
To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 methysergide receptor stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected
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GSTP has an antiapoptotic activity
2022-07-12
GSTP1 has an antiapoptotic activity that is mediated by the inhibitory interaction with JNK1. Our data suggest that GSTP1 treatment is associated with a significant down-regulation of caspase expression. This might explain the reduction in infarct-related cardiomyocyte death and saving the cardiomyo
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Furthermore the higher expression levels of DNMT seemed to b
2022-07-12
Furthermore, the higher expression levels of DNMT1 seemed to be responsible for the elevated levels of methylation in the GSTP1 and TXNRD2 promoters in HMC. In the DNA methyltransferase family, the functions of DNMT1 and DNMT3, including 3a and 3b, were the most ubiquitously expressed in cells. DNMT
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Based on our finding that TFA modulates GlyR
2022-07-11
Based on our finding that TFA modulates GlyR function and reports that TFA-bound Colchicine can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Tipps et al., 2010). No d
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Acknowledgments br Introduction Type diabetes mellitus T
2022-07-11
Acknowledgments Introduction Type 2 diabetes mellitus (T2DM) is caused by relative insulin deficiency or insulin resistance in peripheral tissues. The clinical management of T2DM is achieved by controlling blood glucose levels. Current therapies available for treatment of T2DM include biguanides
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The HH signaling has also been implicated in the
2022-07-11
The HH signaling has also been implicated in the regulation of cancer stem PF-670462 (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignancies,
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The GAL also modified HT system Millon et
2022-07-11
The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B AZ3146 (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragment (
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All of the abovementioned effects of
2022-07-11
All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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In addition to the regulation of SV
2022-07-08
In addition to the regulation of SV exo- and L-NMMA citrate by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g. knockout of
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A biochemical characterisation of this
2022-07-08
A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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The measured ROcc values and mg kg respectively were
2022-07-08
The measured ROcc50 values (4.8 and 42 mg/kg, respectively) were lower than those estimated from the mouse free XAP044 concentrations (0.4 and 9.3 mg/kg for the sigma-1 and histamine H3 receptor, respectively) or rat CSF levels (0.65 and 4.5 mg/kg, respectively). This discrepancy is almost certainly
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This crosstalk may be responsible for the beneficial
2022-07-08
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on Ibandronate sodium pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dos
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The second approach to optimizing microsomal stability
2022-07-08
The second approach to optimizing microsomal stability in this series involved the strategic positioning of steric bulk along the tether as a means of encumbering the access of oxidative enzymes to the methylene bridge. This approach has been employed in other P2-P4 macrocyclic inhibitors of NS3/4A
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In order to study the role of haspin
2022-07-08
In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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br Materials and methods br Results br
2022-07-08
Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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