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Herein the interactions of etamicastat nepicastat
2019-07-16
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the Dihydroeponemycin exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCR
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Several studies have shown that independently of body
2019-07-15
Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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In the present work we have investigated
2019-07-15
In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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Nowadays colorimetric assay has been applied in detecting DN
2019-07-15
Nowadays, colorimetric assay has been applied in detecting DNA MTase activity. Li et al. used DNA modified gold nanoparticles (AuNPs) coupled with enzyme-linkage reactions to detect the activity of methylases [20]. In a previous study, our group presented a label-free colorimetric method, using unmo
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br Experimental All starting materials
2019-07-15
Experimental All starting materials and reagents were purchased from Sigma-Aldrich, Merck and Loba Chemie. Thin layer chromatography (TLC) was performed on silica gel G60 F254 (Merck) plates and eluted with the mobile phase n-hexane: ethyl acetate (70:30%v/v). Melting points were recorded on auto
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br Use of recombinant collagen to study DDR
2019-07-15
Use of recombinant collagen to study DDR–collagen interactions Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to
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DAPK is involved in the p dependent
2019-07-15
DAPK-1 is involved in the p53 dependent apoptotic pathway and it is a mediator of γ-interferon induced apoptosis. DAPK-1 is also involved in other death signaling pathways (tumor necrosis factor-α, CD95 and transforming growth factor-β) and it blocks tumor metastasis in vivo. The loss of DAPK mRNA e
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br Cytokine profile in MPN Results
2019-07-15
Cytokine profile in MPN: Results from experimental investigation Cytokines are small molecules constituted by proteins or glycoproteins, which regulate the immune cell function and the immune system. They are secreted mainly by immune SP600125 for but also by other cells such as epithelial cells
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Steady state mRNA levels of CYP
2019-07-15
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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br Materials and methods br Results and
2019-07-15
Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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Compounds were screened for their
2019-07-15
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Introduction The first reference to a
2019-07-15
Introduction The first reference to a possible involvement of orexins in the effects of drugs of abuse appeared in 2003 and showed that orexigenic peptide neurons respond to the chronic administration of morphine followed by abrupt withdrawal symptoms caused by opioid receptor antagonists (Georgesc
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Citrus comprising some of the most widely
2019-07-15
Citrus [29], comprising some of the most widely cultivated fruit crops worldwide, has been consumed as a food and dietary supplement. According to traditional Chinese medicine, dry pericarp of Citrus, as a Chinese herbal remedy, is capable of regulating Qi and expelling phlegm, and has been used to
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Over the last decade numerous studies have
2019-07-15
Over the last decade, numerous studies have evaluated the acute, short-term, and medium-term impact of pulmonary vasodilators on Fontan physiology.23., 24., 25., 26., 27., 28., 29., 30., 31. Although different 10Panx for of medications have been evaluated, phosphodiesterase-5 (PDE-5) inhibitors hav
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br Funding This work was supported by the National
2019-07-15
Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo
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