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br Materials and methods br Results br Discussion Both
2022-05-10

Materials and methods Results Discussion Both EMT of the tubular epithelial Shikonin and the activation of fibroblasts are critical factors in the pathogenesis and progression of renal interstitial fibrosis. Accumulating evidence implicates EMT in the onset and pathogenesis of renal inters
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A second feature of the
2022-05-10

A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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GPR has been implicated in neuropathic and inflammatory
2022-05-10

GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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Continuing studies of endocannabinoid ligands at GPR
2022-05-10

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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In mice iNKT cells are most frequent
2022-05-10

In mice, iNKT cells are most frequent (20–30%) among liver T lymphocytes, while they only constitute 0.4–1% of the total T cells in thymus, bone marrow, spleen, lymph node, and intraepithelial lymphocytes. In humans, iNKT cells constitute approximately only a 0.1–0.2% of the peripheral blood T lymph
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GLP is known to be expressed in a subset
2022-05-10

GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1
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We first set out to
2022-05-10

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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In summary we have designed
2022-05-10

In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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However even if immunological tests with
2022-05-10

However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21
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The aim of our study was
2022-05-10

The aim of our study was to investigate the polymorphisms of RAGE and glyoxalase I gene and sRAGE serum levels in patients with pathological pregnancy trying to describe the genetic background of pathological pregnancy or to find a new biochemical marker (sRAGE) of these pathological states in preg
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Our inhibitor studies revealed the
2022-05-10

Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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br Brief overview of the
2022-05-10

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 BIIB021 sale (GABA), the primary inhibitory neurotransmitter. Togethe
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br Regulation of Glu transporters The
2022-05-10

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino SB939 calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcription o
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Our results indicate that abcb is
2022-05-10

Our results indicate that abcb5 is likely to be a XT in zebrafish ionocytes, although, like renal cells, the phenotypes observed likely arise from the action of multiple transporters. Zebrafish lack an abcb1 ortholog, and abcb4 and abcb5 have been identified as the P-glycoproteins in zebrafish (Fis
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Ca independent release of L C glutamate and GABA that
2022-05-10

Ca2+-independent release of L-[14C]glutamate and [3Н]GABA that occurs via transporters working in the reverse mode also insignificantly increased in vitamin D3 deficiency despite decreased GAT-3 and EAAC-1 Thioguanine and neurotransmitter uptake efficacy Fig. 3, Fig. 6 A). However, the upward tende
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