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Introduction Rotavirus RV a member
2020-05-12
Introduction Rotavirus (RV), a member of Reoviridae family, is a non-enveloped virus which has a double-stranded RNA genome of 11 segments surrounded by three concentric protein layers. It has been reported to cause estimated 25% of moderate-to-severe illnesses (Kotloff et al., 2013) and 30% of tot
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As part of a program to explore the key
2020-05-12
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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69 0 The absorption rate of polyphenols into the body
2020-05-12
The 69 0 rate of polyphenols into the body is usually low. For example, the absorption rate of epigallocatechin gallate (EGCG), an active component in GP, is approximately 1% (Chen et al., 1997). To increase absorption of GP in the body, people have been increasing their intake of functional foods
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The synthetic route chosen for the preparation of the substr
2020-05-11
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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An analysis of EBI expression on dendritic cells
2020-05-11
An analysis of EBI2 expression on dendritic cells (DCs) showed that EBI2 is highly expressed on CD4+ conventional cDCs. In line with this mice deficient for EBI2 largely lack this subset of cDCs in the spleen. Furthermore, the localization of the residual cells is disturbed [10,11]. It was found tha
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br Conclusions Cereal seeds like the
2020-05-11
Conclusions Cereal seeds, like the seeds of all plants, are responsible for the development, protection, dispersal, and nutrition of the next generation. Moreover, cereal caryopses have a high nutritional value for humans and animals. The stable and proper growth of cereal seeds is made possible
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For LAU extracted ion chromatograms of the
2020-05-11
For LAU 399, extracted epirubicin chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are show
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Introduction Cytochrome P CYP A
2020-05-11
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The 1,3-PBIT dihydrobromide receptor level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug res
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bacteriological Pyrazolopyrimidines are bioisostere of purin
2020-05-11
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase bacteriological [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour an
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The synthesis of tricyclic analogs
2020-05-11
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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Many PIM inhibitors have been
2020-05-11
Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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This study showed that ER redox disturbance
2020-05-11
This study showed that ER-redox disturbance-associated ER stress is linked to cytoplasmic chaperone signaling, including HSP90 stability and its client protein, eNOS. The highly increased PERK and IRE-1α lead to dissociation with the chaperone protein, thereby decreasing HSP90 stability (Fig. 5B). S
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In conclusion we have identified Ednra as a downstream
2020-05-11
In conclusion, we have identified Ednra as a downstream direct target of Hoxa9 and Meis1. Upregulation of Ednra has a role in the progression of Hoxa9+Meis1-induced leukemia and targeting Ednra together with other chemotherapies may have therapeutic benefits for leukemia [30]. Ednra inhibitors in th
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The isomeric phenyloxazole not only
2020-05-11
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand VO-Ohpic trihydrate (as seen in compound pairs – and –) decre
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Two GPCR subtypes of interest in the myocardium
2020-05-09
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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