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TPEN Recent research has focused on identifying key
2022-01-30

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty TPEN receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contributes to GLP-1 relea
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The precise mechanism by which erastin inhibits SLC A mediat
2022-01-30

The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A
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br Materials and methods br Results br Discussion ERK signal
2022-01-30

Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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Our results further indicate that
2022-01-29

Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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While more detailed molecular studies on
2022-01-29

While more-detailed molecular studies on the mechanistic basis for heightened H3 receptor function in PAE rats are underway, we have also been exploring whether PAE alters other markers of histaminergic neurotransmission in affected brain regions. One question is whether PAE affected the number of h
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Sitafloxacin Hydrate br Results br Discussion Our current st
2022-01-29

Results Discussion Our current study demonstrates that the sustained activation of Yap overrides the p27-mediated checkpoint, at least in part, through the degradation of FoxO family proteins, allowing polyploid cells to proliferate inappropriately with mitotic defects and resulting in centros
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br Acknowledgements This research was supported by the Natur
2022-01-29

Acknowledgements This research was supported by the Natural Sciences and Engineering Council of Canada (NSERC) Discovery Grant awarded to RGM. LMW was supported in part by fellowships from the University of Regina and the Government of Saskatchewan Fish and Wildlife Development Fund (FWDF). We wo
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Several layers of regulation for this canonical activation o
2022-01-29

Several layers of regulation for this canonical activation of the HH pathway exist. First, the protein kinase A (PKA), the casein kinase 1α (CK1α) and GSK3β can phosphorylate and mark for proteosomal degradation the GLI transcription factors. [36] Second, Suppressor of Fused (SUFU) binds to GLI and
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Decreasing GSK activity has therapeutic benefits in animal
2022-01-29

Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic zotarolimus australia injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregul
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tnf alpha inhibitors br The mode of binding of ligands
2022-01-29

The mode of binding of ligands to GPR35 As noted above, although kynurenic tnf alpha inhibitors is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importa
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br RNA preparation cDNA synthesis and RT PCR
2022-01-29

RNA preparation, cDNA synthesis and RT-PCR Trizol reagent (Invitrogen, Carlsbad, CA, USA) was used to extract total RNA from tissues according to the manufacturer’s protocol and isolated RNA quantity was determined by UV spectrophotometry (Nanodrop, Thermo Scientific, USA) and RNA integrity was v
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In summary we discovered azaindole substituted hydroxypyrido
2022-01-29

In summary, we discovered 7-azaindole substituted -hydroxypyridone as a potent zinc-binding GLO1 inhibitor (IC=11nM) through lead generation from HTS and structure-based inhibitor design. The X-ray cocrystal structure and the comparison of binding energies with the indole counterpart revealed that
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By regulation of synaptic glutamate concentration
2022-01-29

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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There are two ways to transport
2022-01-29

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty 3-Bromopyruvic acid transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is re
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Multiple mechanisms have been suggested by
2022-01-29

Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased me
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