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Michiel S van der Heijden had full access to all
2022-05-04

Michiel S. van der Heijden had full access to all Biotin-azide 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, Sus
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protease inhibitors br Drug design Over the past decades
2022-04-29

Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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br Development of calibrators and controls for DiXaIs
2022-04-29

Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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cal a Despite a large amount of uptake for both nanoparticle
2022-04-29

Despite a large amount of uptake for both nanoparticles, only after transport across intestinal epithelia do the nanoparticles really contribute to improving absorption. Though the transport of nanorods across monolayer was a little bit more than nanospheres, the total transport was less than 2% (A1
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To understand the structural basis for
2022-04-29

To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pock
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Antigen presentation of incoming viral particles
2022-04-29

Antigen presentation of incoming viral particles has been well studied for diverse viruses in antigen-presenting cells (APCs), mostly in dendritic cells and macrophages in the context of the exogenous antigens’ pathway to prime the CD8+ T cells. However, CD4+ T cells are not known as efficient APCs,
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Distribution of histamine receptors in the intestines varies
2022-04-29

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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Bile acids synthesized in the liver
2022-04-29

Bile acids synthesized in the liver are secreted into the intestinal tract to facilitate the digestion and DTP3 of nutrients. Most bile acids are reabsorbed by the ileum and are transported back to the liver via the portal blood circulation. Recently, bile acids have also been considered as hepatomi
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It is an open question if these in
2022-04-29

It is an open question if these in vitro findings have implications for the use of sGC activators in the in vivo situation and in patients. Assuming that incorporation in de novo synthesised enzyme occurs during therapy, one might speculate that the duration of drug administration has an influence o
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Compared with the tetrazole derivative the potency of
2022-04-29

Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, such
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The present study chose the fdh gene the
2022-04-29

The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss
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Glutamate is a ubiquitous principal excitatory neurotransmit
2022-04-26

Glutamate is a ubiquitous principal excitatory neurotransmitter in the FTI 277 HCl that plays a central role in a variety of brain functions (Delgado, 2013, Hawkins, 2009). Several studies reported that CSF glutamate was associated with mental illness, including major depressive disorder, anxious a
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For the two KO models CX
2022-04-25

For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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Serotonin hydroxytryptamine HT is a monoamine with dual func
2022-04-25

Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the maleate as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Condron, 201
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The first FPR ligand described is the
2022-04-25

The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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