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br Acknowledgments The research leading to these results was
2022-08-09

Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/
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The effect of on the
2022-08-08

The effect of on the conformational of G-quadruplexes was investigated with circular dichroism (CD) spectroscopy. In the absence of , the CD spectra of parallel G-quadruplex exhibited a characteristic positive peak at about 265 nm, and a negative peak at about 240 nm; antiparallel G-quadruplex sh
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The anti platelet functions of ZGR were confirmed by
2022-08-08

The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati
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Potential platelet related mechanisms that might explain an
2022-08-08

Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu
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Despite the two models for the HIV IN
2022-08-08

Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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For further understanding of the
2022-08-05

For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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br Rho family GTPases are molecular switches
2022-08-05

Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany
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Pyridoxine HCl synthesis Chronic exposure of cells to cytoto
2022-08-05

Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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br Discussion Recent progresses in osteoblast
2022-08-05

Discussion Recent progresses in osteoblast biology reveal that aerobic glycolysis was the main pathway to supply energy and materials that need by osteoblast differentiation [3]. In current study, we showed that LA enhanced the effect of PTH on osteblast differentiation and revealed an unrecogniz
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The GPR receptor is also emerging
2022-08-05

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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Despite having potent activity and good solubility
2022-08-05

Despite having potent activity and good solubility, showed inhibitory activities against cytochrome P450 (CYP) 2C8, 2C9, and 2C19 with an IC value of less than 10 μM. In general, the specificity of the compound to the target should improve and the off-target risk such as CYP inhibitory activity sho
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Oxidative stress results from the disequilibrium
2022-08-05

Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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br Reaction mechanism The dissimilarity between monofunction
2022-08-05

Reaction mechanism The dissimilarity between monofunctional and bifunctional glycosylases is that the monofunctional glycosylases removes the substrate base, leaving an intact AP site while the bifunctional glycosylases have an additional lyase activity. This intrinsic lyase activity is present i
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Several groups studied CTD mouse models which largely mimick
2022-08-05

Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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We recently reported the first cyclopropene analog
2022-08-05

We recently reported the first cyclopropene-analog of the amino omaveloxolone neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworkers) [28]
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