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To our knowledge BAY has not
2024-07-01

To our knowledge, BAY 60-6583 has not progressed to clinical development and remains to be the only ADORA2B agonist that has been developed.33, 34 Further development of similar compounds would be beneficial in future fibrosis research. One of the limitations of our study is being limited to in vit
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The total IgG concentration decreased from a mean of mg
2024-07-01

The total IgG concentration decreased from a mean of 997 mg/100 ml before treatment to a mean of 696 after treatment in the MuSK+MG patients, and from a mean of 1736 mg/100 ml to a mean of 802 mg/100 ml in the AChR+MG patients (normal values 723–1685 mg/100 ml). This decrement was also statistically
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Several studies have recently used optogenetics to selective
2024-07-01

Several studies have recently used optogenetics to selectively activate various cholinergic neurons (Jiang et al., 2014). However, most do not explicitly report direct release of GABA from cholinergic fibers, with the exception of our two studies described above (Saunders et al., 2015a, Saunders et
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The subdivision of HT receptors started
2024-07-01

The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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br Materials and methods br
2024-07-01

Materials and methods Results Discussion Recent studies have highlighted Azidobutyric acid NHS ester and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in v
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The identification of novel kinase inhibitor scaffolds
2024-07-01

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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The take home message here is that although Aurora A
2024-07-01

The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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The GRAVY value for a
2024-07-01

The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot
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In the case of DIA CN the docking
2024-07-01

In the case of DIA-4CN the docking results do not show any interaction between the iron atom and the inhibitor, presumably due to the reduced ability to form a complex involving the -CONN- moiety versus the bidentate -CONHNH- central group of HYD-4Me. This results in a considerable gap between the i
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Significant reductions in GYN cancer patient mortality
2024-07-01

Significant reductions in GYN cancer patient mortality and morbidity rates require treatments that proactively prevent and reverse resistance to chemotherapy and radiation. Combining chemotherapy and radiation with inhibitors of key DDR proteins targets is likely to enhance the ability of genotoxic
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Vascular interventional radiology VIR laboratories perform a
2024-06-28

Vascular interventional radiology (VIR) laboratories perform a myriad of procedures ranging from simple tunneled peripherally inserted central catheter lines to complex transjugular intrahepatic portosystemic shunt placements. Infections are a common complication in the VIR environment; thus, the pr
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Recent studies suggest that A
2024-06-28

Recent studies suggest that Aβ caused synapse damage as a consequence of aberrant cell signalling. As synthetic Aβ42 monomers activate the phosphatidylinositol-3-kinase pathway (Giuffrida et al., 2009) and insulin signalling (Giuffrida et al., 2012) it is possible that Aβ monomers and Aβ oligomers a
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Our results lead to the
2024-06-28

Our results lead to the discovery and characterization of VvAAT2, a gene potentially involved in acetate accumulation in grape berries discovered through amino-acid feeding experiments. Incubation with exogenous amino acids has also been a key in the discovery of new genes affecting fruit aromas [13
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br ABCA modulates intracellular sphingolipid metabolism
2024-06-28

ABCA2 modulates intracellular sphingolipid metabolism in the LE/LY Recycling of plasma membrane lipids that occurs by constitutive endocytosis and vesicularization of complex glycolipids, complex sphingolipids and cholesterol as well as free cholesterol liberated from LDL after receptor-mediated
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Adiponectin also works on AdipoR inducing
2024-06-28

Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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