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Andexanet alfa works as a
2021-11-09

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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c di gmp The finding that a peptide consisting of
2021-11-09

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino c di gmp ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its b
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Two typical properties of Gi o protein
2021-11-09

Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s
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N-acetyl D-galactosamine br Experimental procedures br Resul
2021-11-09

Experimental procedures Results Hdc-KO mice show basal activation of the MAPK and AKT/GSK3β pathways in the dorsal striatum (Rapanelli et al., 2014). These signaling pathways are differentially regulated by the H3 receptor in dMSNs and iMSNs in wild-type mice (Rapanelli et al., 2016). To bette
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In recent years the Hippo signaling pathway has
2021-11-09

In recent years, the Hippo signaling pathway has emerged as an important regulator balancing cell proliferation and differentiation [[5], [6], [7]]. The pathway components, first described in the fruit fly Drosophila melanogaster, are highly conserved across different phyla [6]. The signaling pathwa
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Several studies have also suggested that Wnt signalling can
2021-11-09

Several studies have also suggested that Wnt signalling can in turn stimulate the transcriptional activity of Yap/Taz (Figure 2, Figure 3). In the Azzolin model, Yap/Taz not only block β-catenin signalling, but their association with Axin1 and/or β-catenin also maintains them in an inactivate state
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Similarly towards the acylsulfamoyl benzoxaboroles
2021-11-08

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 chl
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Anidulafungin In summary we propose a model
2021-11-08

In summary, we propose a model that explains the possible mechanism the HULC mediates activation of HBV in liver cancer Anidulafungin (Fig. 8). In the model, HULC promotes the expression of miR-539 by stimulating HBx-co-activated STAT3. Then, miR-539 down-regulates APOBEC3B, leading to an increase
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The number of small molecule GSK inhibitors
2021-11-08

The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop
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br Materials and methods br Results br
2021-11-08

Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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GPR A a G protein coupled receptor located mainly on
2021-11-08

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Stattic sale [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-media
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cannabinoid receptor As GLO is the major detoxification
2021-11-08

As GLO1 is the major detoxification system of reactive dicarbonyls, it is plausible that differences in production and activity of the enzyme influences AGE production and the development and/or modulation of diabetic neuropathy. Glo1 exists as a copy number variant (CNV) in many inbred strains mice
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A major hurdle in purifying a membrane protein is
2021-11-08

A major hurdle in purifying a membrane protein is finding a detergent that can preserve the protein, after releasing it from a given membrane, in a stable and non-aggregated state during purification steps [18,50]. The ability of various detergents used to solubilize and purify membrane proteins has
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br Restart of Stalled Replication Forks By
2021-11-08

Restart of Stalled Replication Forks By preventing the replisome from unwinding duplex DNA, ICLs stall progression of the replication fork, which in turn results in genomic instability 41., 42.. As in prokaryotes, the conventional mechanism of ICL repair in eukaryotes involves the combined activi
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p16 However ghrelin has a short half life
2021-11-08

However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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