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Cells undergoing EMT display a downregulation of
2021-10-12
Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the RGDS peptide cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are specialized
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Another important question is what ligand s bind
2021-10-12
Another important question is what ligand(s) bind to GPR84 in vivo? Previous studies have identified medium-chain FFAs of 9 to 14 carbons in length and two other organic molecules (6-n-octylaminouracil and 3,3′-diindolylmethane) as agonists of GPR84 in vitro (Wang et al., 2006, Suzuki et al., 2013).
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The saturated carbocyclic derivatives pyrazoles M and
2021-10-12
The saturated carbocyclic derivatives, pyrazoles (2.5μM and 5.2μM) and (9.0μM and 2.5μM), provided little improvement in potency when compared to the linear alkyl derivatives, whereas the C5-phenyl derivative (0.31μM and 0.43μM) showed promise as a scaffold for further structural modifications.
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br Materials and methods br Results br Discussion Since s
2021-10-12
Materials and methods Results Discussion Since 1990s, solving structures for most DNA glycosylases by X-ray crystallography significantly advanced mechanistic understanding of the catalytic activity and substrate specificity of this important class of DNA repair enzymes. However, static str
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After brain injury adenosine levels rapidly increase in
2021-10-12
After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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br Acknowledgements br Introduction Ghrelin is a
2021-10-11
Acknowledgements Introduction Ghrelin is a potent orexigenic hormone and growth hormone secretagogue mainly derived from the stomach [1], [2], [3], [4], [5]. Other pleiotropic actions of the hormone include those that are glucoregulatory, food reward-enhancing, gastric motility-enhancing, and
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GSK has also been used as
2021-10-11
GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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1 98 Thus both in Drosophila and mammals
2021-10-11
Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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br Materials and methods br Results Our data indicated
2021-10-11
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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While PLGA implants could be
2021-10-11
While PLGA implants could be beneficial for regenerative angiogenesis in the context of wound healing, they self-flagellation could also lead to adverse effects. Indeed, extracellular acidification inhibits osteoblast proliferation, differentiation, and extracellular matrix mineralization, which mi
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br The mode of binding of ligands to
2021-10-11
The mode of binding of ligands to GPR35 As noted above, although kynurenic EZLink Sulfo-NHS-SS-Biotin Kit 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 GPR3
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As natural ligands of GPR several
2021-10-11
As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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In recent years several DPP IV inhibitors have already
2021-10-11
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 SKI-606 with a unique xanthine scaffold developed through high-throughput
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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 Results br Discussion We have reported the crystal struct
2021-10-11
Results Discussion We have reported the crystal structures of VcmN, the high-resolution structures of this MATE transporter from a pathogenic bacterium. The structures display distinct conformations of TM1, as a consequence of their unique hydrogen-bonding networks. We interpret this result to
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