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Hymenialdisine the most potent inhibitor of parasite TgCK en
2020-03-04
Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this Cathepsin Inhibitor 1 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibit
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Our data indicate that the ability of these promiscuous
2020-03-04
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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The transcriptome analysis of barley seeds in two tissue
2020-03-04
The transcriptome analysis of barley seeds in two tissue fractions: starchy endosperm/aleurone and embryo/scutellum, during maturation, desiccation and germination, revealed the large group of GA-responsive genes (Sreenivasulu et al., 2008). These transcripts have been divided into two groups. Nearl
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br Material and methods br Results
2020-03-04
Material and methods Results Discussion Monomeric CDK5 shows no enzymatic activity and requires the association with a regulatory partner for activation (Dhavan and Tsai, 2001). Here, we found that CDK7 might be one of the partners required for activation of CDK5 in the skin tissue, based o
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In the context of E ligase drug
2020-03-03
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 GK9
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Everolimus treatment showed an increase in the number
2020-03-03
Everolimus treatment showed an increase in the number of plaques and a reduction in plaque size, depending on concentration and treatment time (Fig. 1, Fig. 2). Everolimus-pretreated secreted frizzled related protein adsorbed less virus with more plaque formation in the initial phase of infection (F
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As the first allotetraploid fish in the world our
2020-03-03
As the first allotetraploid fish in the world, our lab selectively breed the allotetraploid hybrid fish (4nAT, 4n = 200) from the distant hybridization offspring F3 of female Red Crucian Carp (Carassius auratus red var., abbreviated as RCC, 2n = 100) and male Common Carp (Cyprinius carpio L., abbrev
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br Conclusion br Acknowledgments br Introduction Arsenic As
2020-03-03
Conclusion Acknowledgments Introduction Arsenic (As) is one of the most toxic metals derived from the natural environment in soil, air and well water. It has two oxidative states: a trivalent form, arsenite, and a pentavalent form, arsenate. The inorganic As is more toxic than organic As. A
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This paper proposes an acceptance process
2020-03-03
This paper proposes an acceptance process and evaluation criteria, specialized for the dedication of indirect COTS SW as well as direct ones. (Step 1) It first recognizes an indirect COTS SW as a target of dedication, unlike EPRI NP-5652/TR-106439. (Step 2) It then determines the safety category of
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Through the process of alternative
2020-03-03
Through the process of alternative splicing, the IKZF1 gene is capable of encoding a large number of Ikaros isoforms (Molnar et al., 1996). Some of these isoforms were shown to have distinct functions (Li et al., 2011, Ronni et al., 2007). Ikaros protein contains four zinc fingers at the N-terminus
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br Methods br Results IAA
2020-03-03
Methods Results IAA-94 abrogated the protective effects of IPC as it increased myocardial infarction (MI) due to IR injury in vitro (Diaz et al., 1999), and also prevented cyclosporine A mediated cardioprotection (Diaz et al., 2013). Moreover, IAA-94-sensitive currents were observed in cardiac
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br Materials and methods br Results br Discussion In
2020-03-03
Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o
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CC-4047 br Results br Discussion The
2020-03-03
Results Discussion The nitric oxide-cyclic guanosine monophosphate pathway plays an important role in normal EF, and oral PDE-5Is were developed in the late 90s after the discovery that ED occurs when there is a problem with this pathway. Since then, several PDF-5Is with different pharmacokine
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The CysLT receptor antagonist BayCysLT
2020-03-03
The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear BTB06584 mg into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret et
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During the past decade it became
2020-03-03
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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