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br Secretase modulators a loss of pharmacology
2021-09-26

γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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br Acknowledgement This work was supported by National Scien
2021-09-26

Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H
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br ACKNOWLEDGMENTS br Introduction Odorant
2021-09-26

ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed an
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br FPRs regulate anti microbial responses The classic eviden
2021-09-26

FPRs regulate anti-microbial responses The classic evidence supporting FPR as an anti-microbial receptor is that bacteria are the major biological source of chemotactic formyl peptides, fMLF binds to FPR and fMLF activates chemotactic and anti-microbial responses in neutrophils 2., 3.. Recently,
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Here we investigated on epigenetic regulatory
2021-09-26

Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me
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The translational relevance of our findings remains
2021-09-26

The translational relevance of our findings remains uncertain at this point. On the one hand, there have been reports to suggest that boosting KDM4 activity may engender beneficial effects in vivo. For instance, Li et al. have show that KDM4 interacts with β-catenin to mediate Wnt signaling in hepat
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In conclusions it is hypothesized that caffeine administrati
2021-09-26

In conclusions, it is hypothesized that caffeine administration could lead to an increase in histamine neuronal activation or release of histamine [38] to induced locomotor stimulation via H1 receptor activation. In addition, the present study also propose that the spaced administration of caffeine
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br FFA GPR was deorphanised as the second receptor
2021-09-24

FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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With this goal in mind we proceeded to
2021-09-24

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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After initial validation of the
2021-09-24

After initial validation of the ability of Ad5-Cre virus to express Cre recombinase protein in glial cells in vitro and in vivo, we employed this virus to induce site-specific deletion of our target GlyT1 in the thalamus, through injection of the cKO GlyT1 mice. This transgenic line was constructed
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Like other RNA viruses HCV also exhibits a high degree
2021-09-24

Like other RNA viruses HCV also exhibits a high degree of genetic diversity, creating a major challenge for the development of both HCV vaccines and pan-genotypic therapeutics (Timm and Roggendorf, 2007). The virus has a total of seven genotypes, with >50 subtypes and millions of quasispecies (Cuype
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The effects of these steroids namely the decrease in
2021-09-24

The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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In this study with the use
2021-09-24

In this study, with the use of 13C515N2-labeled glutamine, we observed that 13C515N2-labeled glutamine produces a wide range of NAAG isotopologues and its precursors: NAA and glutamate. The NAAG production from glutamine is consistently more elevated in MYC-ON lymphoma and OVCAR4 compared to MYC-OFF
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Introduction Glucose is the most important energy carrier of
2021-09-24

Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula
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Pyrogallol is an organic gallic acid converting compound tha
2021-09-24

Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic Camptothecin is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce pyrogallol (a
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