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Mapping PPI networks is challenging as it is
2021-10-18
Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of molarity calc in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature. F
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One of the mechanism of regulation of NO content
2021-10-18
One of the mechanism of regulation of NO content in plant cells is it scavenging by GSH leading to formation of GSNO [59]. This reaction, depending on NO level and availability of glutatione in its reduced form, influences cellular redox potential by lowering GSH content and in consequence may impac
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br Materials and methods br Results Our data indicated that
2021-10-18
Materials and methods Results Our data indicated that 1,8-cineol leads to a noticeable but not significant (p = 0.07) 45% decreased phosphorylation of GSK-3α/β at Ser-9/21. Phosphorylation of GSK-3α/β at Tyr-279/216 was not affected (Fig. 1A/B). To ensure, that the decreased phosphorylation of
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Lipid sensing GPCRs as therapeutic
2021-10-18
Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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Much of the understanding of this system has come
2021-10-18
Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] an
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In recent years several DPP IV inhibitors
2021-10-18
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic PHA-793887 with a unique xanthine scaffold developed through high-through
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The dorsal horn of the spinal
2021-10-18
The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,
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In order to discover novel small molecule compounds with the
2021-10-18
In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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The effect of GCK NES mutations on
2021-10-18
The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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Another small compound targeting IBAT
2021-10-18
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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However Gingrich and Hen reported
2021-10-16
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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br Conclusions Osteoclcastogenesis is regulated by multiple
2021-10-16
Conclusions Osteoclcastogenesis is regulated by multiple signal transduction pathways. To maintain bone homeostasis, osteoclast cells must achieve a balance regulation of formation, function, and trafficking of its precursors. Here, we proposed a model in which crosstalk between Fas and S1P/S1P1
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Data are expressed as means SE Statistical
2021-10-16
Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of U87MG KPT-185 expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, insert). E
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br Although there are growing bodies
2021-10-16
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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br Heme oxygenase inhibitors Historically the first
2021-10-16
Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron umbelliferone of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to
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