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A number of synthetic GPR agonists have been reported to
2021-09-16
A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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Moreover we revealed that alanine and taurine
2021-09-16
Moreover, we revealed that β-alanine and taurine, a structural analog of β-alanine, have different receptor affinity in the SG neurons of the spinal dorsal horn. Additionally, previous studies indicate that taurine regulates nociceptive information at the spinal cord level, and we have previously de
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br Conflict of interest br Funding br Acknowledgements br In
2021-09-16
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino saquinavir derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediate
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Several studies have found decreased astroglial and
2021-09-16
Several studies have found decreased astroglial and neuronal cell numbers and Propidium iodide damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000, Gullapalli et al.,
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The effect of the selected compounds on NF
2021-09-16
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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In the present study we set out to
2021-09-16
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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Based on the previous report that FXR regulated PEPCK
2021-09-15
Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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We next determined the selectivity profile of the most poten
2021-09-15
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty regadenoson receptor receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinit
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br The potential of EPA Ffar signaling as a novel
2021-09-15
The potential of EPA-Ffar4 signaling as a novel intervention for HFpEF Conclusions and future directions Optimization of ω3-PUFA/EPA-therapy based upon titration to achieve therapeutic levels: A pressing clinical challenge is to continue to define the benefit of ω3-PUFA/EPA-therapy. Recent ana
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sesamin However Gingrich and Hen reported that absence of th
2021-09-15
However, Gingrich and Hen reported that absence of the gene at all stages of ontogenesis of mice may interfere with the normal developmental program and/or the organism may undergo changes in other systems to compensate for gene absence (46). In addition, potentially altered maternal behavior of GPR
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Immunohistochemistry using anti FFAR antibodies revealed imm
2021-09-15
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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To date increasing evidence has demonstrated
2021-09-15
To date, increasing evidence has demonstrated that dysregulated lncRNAs are closely associated with the tumorigenesis and development of HCC via ceRNA modes [29,30]. LncRNAs could bind with special miRNAs and abrogate the inhibitory effect of these miRNAs on their targeted transcripts. For example,
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br Materials and methods br
2021-09-15
Materials and methods Results Discussion In this study, we demonstrated that, at the level of hREECs, blockade of the ETA receptor partially inhibited the effect of NPY on the secretion of ET-1. This suggests that the secreted ET-1 by NPY contributes, in part, to its own secretion via activ
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br Effects of norepinephrine on HIV infection The few in
2021-09-15
Effects of norepinephrine on HIV infection The few in vitro studies specifically examining the effects of norepinephrine on HIV infection suggest that this catecholamine can influence the HIV replication process, although the precise mechanism is unclear. Cole and colleagues found concentrations
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Acetylation of histones by histone acetyltransferases stimul
2021-09-15
Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing androgen receptor structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recent
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