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Nevertheless because of the preclinical work and the interfe
2021-05-10
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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br Methods Ventricular cardiomyocytes from adult male
2021-05-10
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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In the present study it was particularly
2021-05-10
In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including amantadine hcl
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Moreover Hypericum perforatum L was also included in the
2021-05-10
Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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br Materials and methods br Results br Discussion We
2021-05-10
Materials and methods Results Discussion We recently detected phosphorylation of tyrosine Y102 in BPV-1 E2 and reported that FGFR3 binds to E2 and limits E1 dependent viral DNA replication (Culleton et al., 2017, Xie et al., 2017). In the current study, we addressed the potential role of ot
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br Methods br Results br Discussion Preclinical data indicat
2021-05-10
Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the (+)-Apogossypol with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not signif
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In vitro work by us and
2021-05-10
In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan
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Here we examine the associations between serum pro and anti
2021-05-10
Here, we examine the associations between serum pro and anti-inflammatory cytokines and cognitive functioning in early-stage bipolar I disorder (BDI) patients. As per previous studies, ‘early-stage’ was defined as being within three years of the first manic episode (Kauer-Sant'Anna et al., 2009). We
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In conclusion high methylation levels of CDKL were observed
2021-05-10
In conclusion, high methylation levels of CDKL2 were observed both in HCC cell lines and tissues, which showed a negative association with mRNA expression. Moreover, treatment with demethylation agent in HCC cell lines could upregulate CDKL2 mRNA expression. The discovery of the epigenetic modificat
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CXC chemokines are primarily expressed in immune organs and
2021-05-10
CXC chemokines are primarily expressed in immune organs and the central nervous system: the mouse thymus and spleen (Heesen et al., 1996), chicken bursa (Liang et al., 2001), primate (Macaca mulatta) Pam3CSK4 (Federsppiel et al., 1993) and cattle locus coeruleus, cerebellum and pons (Rimland et al.
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Compounds were screened for their activity against the hERG
2021-05-10
Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo
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Elevated homocysteine has been considered to
2021-05-08
Elevated homocysteine has been considered to be a risk factor for vascular dysfunction, vascular disease, and preeclampsia , . The methionine-homocysteine metabolism is responsible for supplying COMT with the methyl-group donor (-adenosyl methionine; SAM) necessary for 2-ME synthesis, and alteration
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Our previous high throughput screening HTS
2021-05-08
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based px12 assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23], [2
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Prostaglandin E PGE is involved in several
2021-05-08
Prostaglandin E2 (PGE2) is involved in several biological processes such as renal function, inflammation, angiogenesis, and tumor growth. The various biological effects of PGE2 are mediated by the so-called E-type prostanoid receptors (EP1 to EP4). Among these, the EP4 receptor has been well studied
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br Materials and methods br Results br
2021-05-08
Materials and methods Results Discussion Although some conditioning therapies have provided satisfactory clinical outcomes, mammalian species have little or no ability to replace injured cardiac tissue [34]. Therefore, therapeutic strategies based on the prevention, rather than treatment af
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