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br Conclusion br Introduction The
2022-02-11

Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri
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Excessive extracellular glutamate may induce excitotoxic neu
2022-02-11

Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much
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br NMDA receptor LBDs The study of
2022-02-11

NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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Hippocampal lesioned mice were less able to
2022-02-11

Hippocampal-lesioned mice were less able to withhold responding during a DRL-10 requirement (i.e. when the animals had to wait 10s between lever presses), and were thus less efficient than sham operated controls. In contrast, GluR-A−/− mice did not differ from wild-type mice when the DRL requirement
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Receptors for glucagon Gcgr GLP Glp r and GLP
2022-02-11

Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the AZ 960 receptor for the rec
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Ulimorelin also known as TPZ is a macrocyclic molecule
2022-02-11

Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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br Conflict of interest br Introduction Since its discovery
2022-02-11

Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood OPP (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-activated K+ chann
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br Results and discussion The
2022-02-10

Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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br FREE FATTY ACID RECEPTOR GPR br
2022-02-10

FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty diltiazem hcl receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and they are
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Macrophage populations are prominent in active IBD Strober a
2022-02-10

Macrophage populations are prominent in active IBD (Strober and James, 1986) as compared to healthy donors. Further, percentages of macrophages are increased in DSS-induced colitis (Grose et al., 2001, Ogawa et al., 2004). IBD is also linked to an influx of neutrophils and depletion of neutrophils b
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notch inhibitor br Drugs approved or in development To
2022-02-10

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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Regulation of gene expression in mammalian cells is governed
2022-02-10

Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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The inhibition of HDAC increases the level of histone
2022-02-10

The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity an
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Studies with GSNOR knockout mice reported decreased CD cells
2022-02-10

Studies with GSNOR knockout mice reported decreased CD4+ indocid and increased CD19+ cells (B-cell) in the blood [31] as well as demyelination, neurodegeneration, and neuropathic pain [29]. To understand the basis of these differences in immune function of GSNOR knockout mice and GSNO treated mice,
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br Materials and methods br Results Human
2022-02-10

Materials and methods Results Human adipocytes, differentiated from fibroblastic preadipocytes in culture, were incubated with IL-33 for either 3 or 24 h to examine acute and prolonged responses to the cytokine. Low, medium and high concentrations of IL-33 were employed. IL-33 had no significa
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