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In our current work we have undertaken liquid phase combinat
2020-10-30
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised AS1842856 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised mo
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Although DAPK has been implicated in neuronal death in ische
2020-10-30
Although DAPK has been implicated in neuronal death in ischemic stroke and neurodegenerative diseases, such as Alzheimer’s disease (Shamloo et al., 2005, Duan et al., 2013), the mechanisms about how DAPK regulates cell death are still elusive. In the present study, we investigated the signal transdu
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In conclusion we developed a new
2020-10-30
In conclusion, we developed a new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model that can be useful for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. In addition, we have shown that the dual CysLT1/2 receptor antagonist ONO-6950 can exert protective effect agai
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br Author Contributions br Funding Canadian Institutes of He
2020-10-30
Author Contributions Funding Canadian Institutes of Health Research, operating grant NMD-83126 and the internal funding from the National Research Council Canada, Charlottetown, PE, Canada. Disclosure Statement Acknowledgements Introduction Cholesterol is an essential structural comp
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br Acknowledgments This work was supported by R
2020-10-30
Acknowledgments This work was supported by Région Auvergne “Nouveau chercheur”. This study has been performed with the assistance of Christelle Damon-Soubeyrand for histology technical assistance using “Anipath” Platform (GReD) and Sandrine Plantade, Keredine Ouchen and Philippe Mazuel for animal
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Introduction Proteins play an important role in
2020-10-30
Introduction Proteins play an important role in cellular functions; however, being and remaining properly folded is necessary for their function. Understanding the stability of the protein is necessary to investigate the folding of proteins, as well as their conformation, functions and interactions
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A cocktail approach can detect the activities
2020-10-29
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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br Conflicts of interest br Financial support NZ is an
2020-10-29
Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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Prote There have been two reports
2020-10-29
There have been two reports of tumor shrinkage in response to dasatinib treatment in lung SCC patients harboring the DDR2 kinase domain S768R mutation., In the first case described by Hammerman et al. a combination of erlotinib (an epithelial growth factor receptor inhibitor) and dasatinib was admin
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ER 50891 receptor Unlike the CRF receptor the CRF a
2020-10-29
Unlike the CRF1 receptor, the CRF2(a) receptor binds and is activated by agonists with a broad range of potencies. Therefore, we assessed the ability of strong and weak ligands to desensitize retinoblastoma CRF2(a) receptors. Although stresscopin\'s N-terminus is two ER 50891 receptor longer than t
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br Experimental section br Results br Discussion In
2020-10-29
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised tachykinin receptor did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a p
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The strong adsorption of amines to the
2020-10-29
The strong adsorption of amines to the stationary phase of gas chromatography (GC) columns causes issues such as tailing, ghosting and low reproducibility [12], [13]. A common practice to overcome this problem is the chemical derivatisation of amines prior to GC analysis [14]. Comprehensive reviews
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Prenylation may turn a flavonoid from
2020-10-29
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformat
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br Introduction Hematopoietic stem cells and
2020-10-29
Introduction Hematopoietic stem prolyl hydroxylase and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation of leukemia, as well
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br Introduction Prostaglandin E PGE signals through
2020-10-29
Introduction Prostaglandin E2 (PGE2) signals through 4 separate G-protein coupled receptor sub-types (EP1, EP2, EP3 and EP4) to elicit a variety of physiological and pathophysiologic effects. EP2 and EP4 increase cAMP levels in the cell via adenylate cyclase activation, whereas EP3 inhibits cAMP
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