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Furthermore in silico physicochemical characters and pharmac
2020-06-03
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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The Ewing sarcoma breakpoint region gene EWSR is a partner
2020-06-03
The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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br Methods Ventricular cardiomyocytes from adult male
2020-06-03
Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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Both receptors belong to the large family of G
2020-06-03
Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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Therefore HNE is an attractive therapeutic target and
2020-06-03
Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo
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Two primary members of the TRIM family TRIM and
2020-06-03
Two primary members of the TRIM family – TRIM5α and TRIM25 – function as antiviral effector and immune regulator, respectively. TRIM5α is one of the best characterized members of the TRIM family (both structurally and functionally) and reported to be an important ubiquitin-mediated regulator of a ma
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Until recently the first line treatment of RLS was
2020-06-03
Until recently, the first line treatment of RLS was the administration of low dose of three dopaminergic drugs, which has been approved by the US Food and Drug Administration and the European Medicines Agency for the treatment of moderate to severe RLS. These compounds are pramipexole (Mirapex), rop
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A recent study revealed that in human glioma cells
2020-06-03
A recent study revealed that in human glioma cells, DNA-PKcs interacted with the regulatory γ subunit of AMPK and positively regulated AMPK phosphorylation and activation under glucose-deprived conditions. This suggested that DNA-PK is an important regulator of AMPK activation in response to energy
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If the unwanted objects detected by
2020-06-03
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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Introduction DHFR is an important enzyme in
2020-06-03
Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic INNO-406 conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interruption of th
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That DGAT mediated hepatic steatosis
2020-06-03
That DGAT-mediated hepatic steatosis did not lead to insulin resistance was clearly demonstrated in Liv-DGAT2-low mice by their normal blood glucose and plasma insulin levels, normal glucose and insulin tolerance, normal insulin sensitivity by hyperinsulinemic-euglycemic clamp studies, and normal he
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ptio It has only recently been appreciated that antigen
2020-06-02
It has only recently been appreciated that antigen-activated ptio undertake two additional transient migrations during the early stages of T-dependent antibody responses. In the first of these, antigen-activated B cells migrate rapidly (within 2–3h) to the outer regions of the follicle before they r
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Structural homology modelling Intensive Phyre modelling
2020-06-02
Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino sphingosine australia sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E. co
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The CPA EoS was presented by Kontogeorgis et
2020-06-02
The CPA EoS was presented by Kontogeorgis et al., in 1996 [23]. The proposed equation is composed of two parts (SRK EOS + association term) such that it can well predict the thermodynamic behavior of hydrogen bonding materials as a result of considering the association term. Yakoumis et al. (1997) e
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br Acknowledgement This work was supported by
2020-06-02
Acknowledgement This work was supported by grant form EU (FP7 grant agreement no.: 266033 SPonge Enzyme End Cell for Innovative AppLication-SPECIAL). Introduction Prolyl 4-hydroxylases (P4Hs) have central roles in the synthesis of collagens and the regulation of oxygen homeostasis [1]. The po
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