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In various models histamine has been shown
2021-11-29

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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In addition to the importance of
2021-11-29

In addition to the importance of heme as an enzymatic cofactor, heme also acts as an important iron source. In order to access the iron within heme, S. aureus encodes heme degrading enzymes known as heme oxygenases (Skaar et al., 2004b; Wu et al., 2005). The two heme oxygenases encoded by S. aureus,
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All the compounds and were assayed for their
2021-11-29

All the compounds –, , , –, , – and – were assayed for their potential cytotoxicity at a single dose of 10 µM on Huh7 cells. Interestingly, all compounds proved to be non toxic, with the exception of and which exhibited high cellular toxicity and therefore were excluded from further experiments (a
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Growing evidence suggests that the glycine site
2021-11-29

Growing evidence suggests that the glycine site seems to play a pivotal role in NMDAR-related function. For example, it Dehydroandrographolide has been demonstrated in a hippocampal slice study that the glycine site sub-serves the spatiotemporal detection of synaptic activity (Li et al., 2009). More
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In this study for the first time the
2021-11-26

In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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br Declaration of interest br Acknowledgments This
2021-11-26

Declaration of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 31471615), the Introduction of Talent Research Start-up Fund of Anhui Polytechnic University (No. 2017YQQ017) and the Pre-research Project of National Natural Sc
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GLP and glucose dependent insulinotropic peptide GIP are
2021-11-26

GLP-1 and glucose-dependent insulinotropic peptide (GIP) are gut hormones secreted from intestinal L Ki16198 and K cells, respectively. Together, these hormones account for the vast majority of the incretin effect, the enhanced postprandial insulin secretion observed in healthy adults (Dupre et al.
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Herein we describe the development of second
2021-11-26

Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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Canonical and non canonical Wnt signaling
2021-11-26

Canonical and non-canonical Wnt signaling pathways play essential roles in various cellular activities, including cell fate determination, proliferation, migration and gene expression [57]. The canonical Wnt pathway (β-catenin dependent pathway), is activated by the binding of Wnt ligands, leading t
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b-raf inhibitors MMV s distinct mode of inhibition
2021-11-26

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Occupying at least of brain volume
2021-11-26

Occupying at least 50% of ACP-196 volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses [29].
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EZH mutations or amplifications have been found in
2021-11-26

EZH2 mutations or amplifications have been found in a broad spectrum of human cancers including B cell lymphoma, ovarian cancer, breast cancer, melanoma, bladder cancer, gastric cancer, and other cancers (Kim and Roberts, 2016). Given the evidence of EZH2 as a cancer driver, numerous efforts have be
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In addition the interplay of membrane curvature induced tens
2021-11-26

In addition the interplay of membrane curvature induced tension at the fusion pore and Mianserin HCl australia induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity warran
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The exocytosis promotion is triggered upon the binding
2021-11-26

The Arecaidine but-2-ynyl ester tosylate promotion is triggered upon the binding of Ca2+ to the C2 domains of two key protein groups, i.e. complexin and certain synaptogamins (Lai et al., 2017; Rizo and Xu, 2015). The first step of the vesicle fusion is the priming of the secretory vesicles, involv
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wnt inhibitor The variants all occurred at residues conserve
2021-11-26

The 17 variants all occurred at residues conserved among vertebrates (Figure 1B) and in regions depleted in missense variants in gnomAD. Indeed, when we assessed missense tolerance ratios for TRRAP, we observed that most of the 17 variants were in regions intolerant to missense variants (Figure 2B).
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