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The H R antagonist JNJ
2021-10-12
The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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DNA methylation is a kind of epigenetic modifications
2021-10-12
DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam
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It was reported that GPR is expressed on macrophages in
2021-10-12
It was reported that GPR120 is expressed on macrophages in adipose tissue (Oh et al., 2010). Whether GPR120-positive beta-lactamase in human and rat pancreas belongs to macrophages was studied. CD68 is a transmembrane glycoprotein that is highly expressed by human monocytes and tissue macrophages (H
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Strengths The primary feature of GPR
2021-10-12
Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L PCI-34051 mg as well as glucose-dependent insulin secretion and insulin promoter activity enhancement in pan
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In order to elucidate the reasons of
2021-10-12
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen S1RA of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM), while the simp
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By association a possible mechanism which may
2021-10-11
By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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Contrary to the transient nature of signal transmission
2021-10-11
Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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It is known that microglial function and
2021-10-11
It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial Torin 2 (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism. Since this alcohol-induced mi
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Histone demethylases are involved in the transcriptional
2021-10-11
Histone demethylases are involved in the transcriptional output of the AR and hypoxia signaling pathways, and thus contribute to prostate cancer development [12]. For example, the histone demethylase KDM3A serves as a transcriptional coactivator of HIF1α and AR in regulation of their target genes [1
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Two genes PATL and RASSF
2021-10-11
Two genes (PATL2 and RASSF1), whose relationship to HIV infection had not previously been reported, were identified in this study. Although PATL2 and RASSF1 have been implicated in cell division and tumor suppression, respectively (Scheller et al., 2007, Rather et al., 2014, Liu et al., 2002), their
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Using embelin and its analogs as surrogate GPR
2021-10-11
Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er
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br Since viral infections result in polarization
2021-10-11
Since viral infections result in polarization of naïve CD4 T cells into both Th1 and Tfh subsets (although to variable degrees depending on the nature of the pathogen), a lot of effort has been devolved to the question of whether type I IFNs play a role in CD4+ T cell polarization. In vitro studie
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br Brief overview of the glutamate system and
2021-10-11
Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric ace inhibitors (GABA), the primary inhibitory neurotransmitter. Toget
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geldanamycin By regulation of synaptic glutamate concentrati
2021-10-11
By regulation of synaptic glutamate concentration, glutamate transporters play an important role in limiting glutamate signaling and controlling the activation of glutamate receptors (Rimmele and Rosenberg, 2016). Reduced glutamate transport is thought to underlie the pathogenesis of numerous neurol
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GCK MODY is the most common form of MODY
2021-10-11
GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare
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