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br Conclusions We concluded that the inhibitory effects of
2022-04-18

Conclusions We concluded that the inhibitory effects of propofol on fMMYALF-induced neutrophil activation are mediated by competition with FPR1, which inhibits receptor-mediated downstream signaling and inflammatory responses such as oxidative burst, elastase release, and chemotactic migration (F
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br Discussion and concluding remarks FPR is considered to be
2022-04-18

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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Chemotherapeutic approaches to glioblastoma which are highly
2022-04-18

Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this
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The product chain length determination
2022-04-18

The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino GDC-0199 residues in each subfamily of -prenyltransferases have enabled the understanding of the basic catalytic
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br Acknowledgments Work in SI
2022-04-16

Acknowledgments Work in SI’s laboratory is supported by grant IM 20/4-1 from the Deutsche Forschungsgemeinschaft, Bonn (Germany) and grant EKFS 2012_A309 from the Else Kröner Fresenius Stiftung, Bad Homburg (Germany). FW’s group is supported by the Dr Vaillant Foundation and the Dutch Burns Found
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Different crystal structures of both
2022-04-16

Different crystal structures of both HOs were reported and showed that the three-dimensional structures of proteins (HO-1: PDB code 1N45, HO-2: PDB code 2QPP) are predominantly in an α-helical conformation, with the heme packed between two helices (distal and proximal), and present a remarkable stru
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Under increased drug pressure more protease variants with mo
2022-04-16

Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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Mapping PPI networks is challenging
2022-04-16

Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of Cobimetinib in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature. Fur
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Introduction Epigenetic mechanisms modulate heritable phenot
2022-04-16

Introduction Epigenetic mechanisms modulate heritable phenotypic changes that are not dictated by changes in DNA sequences. The link between epigenetic modifications and cancer development has been established [1], [2]. Histone modifications represent an important class of epigenetic mechanisms tha
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We also examined possible involvement of the
2022-04-16

We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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GPR is a G protein
2022-04-16

GPR55 is a G protein-coupled receptor that has pro-oncogenic properties and whose expression correlates with tumor aggressiveness and increased activation of extracellular signal-regulated kinase (ERK) cascade [12]. Elevated expression of GPR55 has been linked to aggressiveness in human pancreatic,
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2768 Screening of the compounds allowed
2022-04-16

Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detri
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Since KYNA concentrations are increased by aerobic
2022-04-16

Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid
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Michiel S van der Heijden had full access
2022-04-15

Michiel S. van der Heijden had full access to all CEP-18770 data in the study and takes responsibility for the integrity of the data and the accuracy of the data analysis. Wang, Sustic, de Oliveira, van den Heuvel, Bernards, van der Heijden. Wang, Sustic, de Oliveira, van de Ven. Wang, Sustic
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Brain derived neurotrophic factor BDNF is the most abundant
2022-04-15

Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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