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br Materials and methods br Conflicts of
2022-07-16
Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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In conclusion starting from the weakly
2022-07-16
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic mlkl led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally reported series around
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The galactosidase from Aspergillus oryzae is a monomeric
2022-07-16
The β-galactosidase from Aspergillus oryzae is a monomeric enzyme of 113 kDa [58] that has been widely used in GOS synthesis [49,53,[59], [60], [61]], exhibiting a high activity of lactose transgalactosylation [62]. Different immobilization methods have been used for the synthesis of lactose-derived
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The PK profile and tissue distribution
2022-07-16
The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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depicts the synthesis of series with a four step sequence
2022-07-16
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (–)
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6656 br STAR Methods br Introduction Arsenite is a well
2022-07-16
STAR★Methods Introduction Arsenite is a well-recognized toxic metalloid that commonly presents in the natural environment. Chronic exposure to arsenite can lead to a wide range of adverse health effects to human, including cancers, cardiovascular diseases, diabetes, skin lesion and neurodegene
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Overall we partially confirmed our predictions and
2022-07-15
Overall, we partially confirmed our predictions, and, when compared to the other existing dataset exploring the interaction among CRFR1, FAAH, and anxiety, our data are somewhat confirmatory. Demers and colleagues (Demers et al., 2016) found one (protective) CRFR1 minor allele (rs110402) and the (le
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Dysregulation of catecholaminergic neurotransmission particu
2022-07-15
Dysregulation of catecholaminergic neurotransmission, particularly the dopaminergic system, has long been correlated with the development of neuroinflammation and HAND. Studies specifically examining role of catecholamines in HIV pathogenesis, particularly focused on NeuroHIV, are relatively few. Ho
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While histone modifications can alter inter
2022-07-15
While histone modifications can alter inter-nucleosomal interactions that govern the compaction state of a chromatin fiber (Francis et al., 2004, Kalashnikova et al., 2013, Lu et al., 2008), the potential impact of histone modifications on higher-order chromosome organization beyond chromatin-fiber
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br Acknowledgments Work in SI
2022-07-15
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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STAR Methods br Acknowledgments We thank C Hong R
2022-07-15
STAR★Methods Acknowledgments We thank C. Hong, R. Huang, and Z. Yu at the HHMI Janelia cryo-EM facility for help with microscope operation and data collection. We thank A. Müller, W. Kan, and W. Weis for help with the SEC-MALS analysis and M. Elazar and J. Glenn for the use of equipment. P. Love
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Similarly towards the acylsulfamoyl benzoxaboroles
2022-07-15
Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chlori
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Subcellular domains where Rac is active show limited
2022-07-15
Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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(-)-epicatechin In this study we demonstrated that
2022-07-15
In this study, we demonstrated that while Cu(I) does not affect LPS induced iNOS (-)-epicatechin it inhibits NO release from microglia. Cu(I)-induced GSNOR inhibition and GSNO depletion is more in line with alternative (non-inflammatory) polarization. These results extend our previous findings that
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Waldeck Weiermair et al demonstrated that in endothelial cel
2022-07-15
Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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