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AZD8186 Since we found that the pharmacokinetic properties o
2020-10-10

Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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Beside the previously reported Topo
2020-10-10

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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The importance of mitochondria as
2020-10-10

The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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The different diagnostic outcomes of the
2020-10-10

The different diagnostic outcomes of the two assays are also dependent on the used stimuli. The QuantiFERON-CMV assay targets CD8 + T Efaproxiral Sodium by using peptides whereas the T-Track-CMV targets CD4+ and CD8 + T cells by stimulation with two viral proteins [18]. In our study, a specificity
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It would be very useful if unphosphorylated CK s
2020-10-10

It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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Several CHK inhibitors have been reported in the literature
2020-10-10

Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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AMG 487 br Materials and methods br Results br Discussion En
2020-10-09

Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow
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During the past few years
2020-10-09

During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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Contrary to the downregulation of
2020-10-09

Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic Phosphate Colorimetric Assay Kit (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggres
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To analyze EBI expression and its function
2020-10-09

To analyze EBI2 expression and its function in T cells in vivo, we created an EGFP reporter/knockout mouse strain, termed EBI2EGFP. This mouse strain in heterozygous configuration allows for a systematic analysis of the expression of EBI2 in distinct cell types in steady-state and under inflammatory
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HCV has evolved mechanisms to evade humoral immune responses
2020-10-09

HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 am 580 of the N-terminus of E2, which is referred to as the hypervariable regi
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R547 Immunofluorescence assays were performed to
2020-10-09

Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the R547 generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with anti-gE1CT); the pa
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Total synthesis requires the two key
2020-10-09

Total synthesis requires the two key intermediates 3 and 7, which were synthesized using the route described in below. Phenylethylamine 3 was readily synthesized from vanillin or isovanillin; the overall yield was 50–52%. To prepare the intermediates 7, bromination of 2-(4-hydroxyphenyl) acetate wi
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sphingosine 1-phosphate receptor modulator That DGAT mediate
2020-10-08

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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br Materials and methods br Results The i v
2020-10-08

Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha
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