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In recent years the use of liquid chromatography
2020-10-13
In recent years, the use of liquid chromatography/tandem mass spectrometry (LC–MS/MS) has become a preferred approach to measure drugs and metabolites in biological fluids due to its very high selectivity and sensitivity [17], [18], [19], [20], [21], [22], [23], [25], [30]. The great sensitivity of
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This review focuses on the
2020-10-13
This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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Estrogen treatment in postmenopausal women requires combinat
2020-10-12
Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr
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The liposomes as a FDA approved drug delivery carrier
2020-10-12
The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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Ro3306 sale Elastase belongs to chymotrypsin family of prote
2020-10-12
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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br DDR mediated signaling DDRs initiate
2020-10-12
DDR-mediated signaling DDRs initiate signaling pathways in a context and cell type-dependent manner. For instance, DDR1 was reported to activate ERK in vascular smooth muscle biotin 100 mg (Lu et al., 2011), to inhibit ERK in mesangial cells (Curat and Vogel, 2002), and to have no effect on ERK a
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Nanocomposite films with a GNP
2020-10-10
Nanocomposite films with a GNP-DNA filler concentration of 20 wt%, 30 wt%, and 40 wt% were investigated by electrical impedance spectroscopy before and after UV-C irradiation (Fig. 2). EIS data were fitted to a RC-circuit model and surface resistivity values were calculated from the fitted resistanc
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br Conclusions In this paper we describe the
2020-10-10
Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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br Sphingosine kinase One of the enzymes closely related
2020-10-10
Sphingosine kinase One of the enzymes closely related to DGKs are the sphingosine kinases (SKs). These enzymes catalyze the conversion of sphingosine (Sph) to sphingosine-1-phosphate (S1P). SKs and DGKs are closely related lipid kinase in term of basic enzymology and the mechanism of regulation a
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br Conclusions In Summary a multilayer screening of
2020-10-10
Conclusions In Summary, a multilayer screening of xanthones of natural origin (Xanthone-NPs) was undertaken against Pf-DHFR. The Re-rank score of screened compounds was size normalized and interaction profile was generated using experimentally known inhibitors. Three compounds X5, X113A and X164B
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Ingested folate needs to be chemically modified in order to
2020-10-10
Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic inositol phosphatase (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N
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br Materials and methods br Acknowledgements SD was
2020-10-10
Materials and methods Acknowledgements SD was supported by a pre-doctoral research fellowship from the Flanders Agency for Innovation and Entrepreneurship (VLAIO-Flanders, Belgium). YB is supported by a postdoctoral fellowship from Research Foundation Flanders (FWO, Belgium). We thank Isabelle
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Recent pharmaceutical research in the field of
2020-10-10
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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Steady state mRNA levels of CYP A
2020-10-10
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 Results br Discussion br Experimental Procedures br
2020-10-10
Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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