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During the course of our research on mGlu PAMs the
2021-03-08

During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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The results of physical parameters of the prepared
2021-03-08

The results of physical parameters of the prepared samples are summarized in Table 2. The equivalent diameter ranged from 1.09 to 1.14 mm, which is within the required size distribution of 0.8–1.25 mm. A slight increase in size is probably caused by increasing the thickness of the second coat. To d
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Therefore the relationship between ChEs activity
2021-03-08

Therefore, the relationship between ChEs activity and polymorphisms in POT1, TERF1, TERT genes were explored in order to screen susceptible biomarkers in this study. Materials and methods Results Discussion However, genetic toxicity induced by OPs has not been fully investigated so far. Ca
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Recent advances in microarray and next generation sequencing
2021-03-08

Recent advances in microarray [32] and next-generation sequencing [33] based technologies have led to tremendous increases in information about the molecular mechanisms that are responsible for malignant transformation of rare and poorly understood soft tissue sarcomas. However, data interpretation
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br Conclusions br Conflicts of
2021-03-08

Conclusions Conflicts of interest Research funding This work was financially supported by Shanghai Committee of Science and Technology (No. 16431903800). Main Text Developmental processes make usage of a surprisingly limited number of morphogens and signaling components to control a ple
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br Author Contributions br Acknowledgments This work was sup
2021-03-08

Author Contributions Acknowledgments This work was supported, in part, by a grant from the National Cancer Institute of the National Institutes of Health under Grant U01CA202241 and National Institutes of Health under Grant R01NS083856. Introduction The Eph (erythropoietin-producing human
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Another important new result that has expanded the range
2021-03-08

Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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The Liver X Receptor and
2021-03-08

The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux
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Another critical finding in this study
2021-03-08

Another critical finding in this study is that the level of αSyn oligomers in the SN of σ1R−/− mice was progressively increased with age, whereas the levels of αSyn monomers and αSyn messenger RNA (data not shown) were not altered compared to WT mice. A number of studies reported that soluble αSyn m
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br Asb Proteins and Mitochondrial Function Mitochondria
2021-03-05

Asb Proteins and Mitochondrial Function Mitochondria are intracellular organelles in eukaryotic 5-Methoxy-CTP and are the main sites of oxidative phosphorylation and ATP production. In addition, mitochondria serve as signal transduction docking stations in pyroptosis and regulate a plethora of p
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br Results br Discussion The importance of mitochondria
2021-03-05

Results Discussion The importance of mitochondria for the initiation and progression of tumorigenesis is now emerging. It is evident that, despite the well-known Warburg effect, tumors have active mitochondrial bioenergetic metabolism (Marin-Valencia et al., 2012, Hensley et al., 2016). Disrup
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Our data indicate that the ability of
2021-03-05

Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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There are numerous resources clinicians may use to gather in
2021-03-05

There are numerous resources clinicians may use to gather information on the strength of evidence related to pharmacogenetic-based dosing and treatment decisions, as well as specific dosing guidelines, some of which are summarized in this review. These include resources from CPIC, which provides pee
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br CDK Inhibitors for the
2021-03-05

CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be
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R co localizes Golgi marker GM
2021-03-05

R co-localizes Golgi marker GM130 (Fig. 5). Our metabolic pulse-chase studies carried out in the presence of CSF-1 exposed the newly synthesized CSF-1R to its ligand, which promoted its rapid degradation. While this was clearly seen in control BMDMs, the mature band of CSF-1R remained intact for the
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