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As part of a program to explore the key binding
2021-02-07
As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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Sulfo-NHS-LC-Biotin Introduction Formate dehydrogenase enzym
2021-02-07
Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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Cy5 NHS ester We found that both DDR and DDR ECD increased
2021-02-07
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a re
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Several highly potent CysLT receptor antagonists with
2021-02-07
Several highly potent CysLT1 receptor antagonists with large structural mln4924 mg have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazol
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br Nuclear export and the functions of
2021-02-05
Nuclear export and the functions of CRM1 The nuclear envelope provides a compartmentalized intracellular environment for DNA replication, the synthesis of RNA, and production of ribosomes, and, as such, it can regulate cellular biological processes including apoptosis and proliferation. Nucleocyt
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The eNOS bp VNTR polymorphism has been found to be
2021-02-05
The eNOS 27-bp VNTR polymorphism has been found to be associated with altered plasma NO levels. This polymorphism also has been associated with many vascular diseases including hypertension, diabetic retinopathy, and diabetic nephropathy in various populations. Notably, our results were different fr
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Auranofin Introduction With an annual world production of
2021-02-05
Introduction With an annual world production of around 750 million tons, wheat is grown on more agricultural area than any other food crop and is the main source of plant protein in human nutrition [1,2]. Wheat is composed of 8–15% protein, from which 85–90% is gluten [3]. The unique viscoelastic a
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During the past few years several studies have addressed mac
2021-02-05
During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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The expression of EBI has
2021-02-05
The expression of EBI2 has been found to be dysregulated in several types of B cell malignancies and is thus reduced in e.g. diffuse large B-cell lymphomas [12] and chronic lymphocytic leukemia [13] and increased in post-transplantation lymphoproliferative disorders (PTLDs) [14]. EBI2 is also highly
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In the context of E ligase drug
2021-02-04
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 AS6
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Because aspirin and ibuprofen are NSAIDs both
2021-02-04
Because aspirin and ibuprofen are NSAIDs, both cause a variety of adverse effects, including stomach ulcers, stomach bleeding, coagulation disorders, Golgicide A and cerebral microbleeds [13]. Moreover, both cause liver damage [10]. Laster [14] reported a patient with pericarditis treated with aspi
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Furthermore the Langerhans cell infiltrate
2021-02-04
Furthermore, the Langerhans cell infiltrate in skin biopsies from RG7155-treated patients will be analyzed since keratinocyte derived IL-34 was identified as their survival factor (Greter et al., 2012). Microglia, the other macrophage population regulated by neural progenitor and glial cell-derived
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The conventional medical therapy for IBD
2021-02-04
The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f
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Prenylation may turn a flavonoid from an agonist to
2021-02-04
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 conformati
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A more refined picture of cholinesterase activity patterns
2021-02-04
A more refined picture of cholinesterase activity patterns may be obtained by measuring ChE activity of the same sample before and after addition of certain cholinesterase inhibitors, with differential specificity for different components of total ChE activity, such as BW284c51 (BW1,5-bis-(4-allyldi
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