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The inhibitory activities of the
2021-11-10

The inhibitory activities of the compounds with the modification of the amino group against human liver FBPase are summarized in . Replacement of the amino group of with hydrophobic substituent such as a methyl group () led to a substantial loss of activity (IC=995nM). Similarly, replacement with h
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Although exhibited high inhibitory activity was found
2021-11-10

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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br Methods and materials br Results br Discussion
2021-11-10

Methods and materials Results Discussion In this study we demonstrate that CF epithelial 94 8 exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsible for this ba
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br Materials and methods br Results br
2021-11-10

Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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V5 Epitope br Application of TIRFM to
2021-11-10

Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin V5 Epitope (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice
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Our biological data also showed that in presence
2021-11-10

Our biological data also showed that, in presence of LEDGF/p75, R or S of glycerol T instead of T4, T8 or T12 loop in the T30695-GQ differently affected the integration activity of the enzyme (Table 2), whereas the position but not the chirality of glycerol T affected the inhibitory efficiency of T3
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Introduction Pneumocystis pneumonia PCP is a respiratory inv
2021-11-10

Introduction Pneumocystis pneumonia (PCP) is a respiratory invasive infection caused by Pneumocystis jirovecii, an ubiquitous fungus. It is transmitted by air and mostly infects immunocompromised patients. PCP is characterized by respiratory complaints of cough, dyspnea, but also tachycardia, low g
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GPR A a G protein coupled receptor located
2021-11-09

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic ryanodine 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-med
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To test this concept we
2021-11-09

To test this concept, we took advantage of our large supply of various 2-pyridyl containing [3.1.0] cores (inactive with alkyl or aryl sulfonamides) and prepared the -methylimidazole sulfonamide analogs and (), as work form Merck demonstrated that the 2-pyridyl moiety was superior to the original 4-
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To shed more light on the binding of benzophenanthridine to
2021-11-09

To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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Uracil DNA glycosylase UDG is a highly conserved damage
2021-11-09

Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA pathways cu excision repair (BER) pathway which keeps the maintenance of genomic integrity and stability [[21], [22], [23]].
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Type diabetes mellitus is characterised by two major feature
2021-11-09

Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta (S)-(-)-Propranolol hydrochloride [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to
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Analysis of the GHSR screening data for inactive library
2021-11-09

Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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Among sensitizers tested in the previous study
2021-11-09

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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br Materials and methods br Results
2021-11-09

Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta Chaetocin sale [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract, adipo
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