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VUF 10166 First we synthesized inhibitor following the paten
2020-03-20

First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidin
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Some limitations of this study must be
2020-03-20

Some limitations of this study must be noted. First, since the pretransplant evaluation of the T-cell immune response was performed just before transplantation, we cannot establish whether samples obtained at different times before the transplant would offer similar results, since end terminal disea
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We have previously reported the characterization of
2020-03-20

We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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Although many of the genetic changes remain
2020-03-20

Although many of the genetic changes remain to be elucidated, there is evidence to support a difference in incidence and rate of rupture of cerebral aneurysms between men and women, and between pre- and postmenopausal women, suggesting that aneurysm formation may be affected by hormonal changes.18,
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The transcription factor CREB has
2020-03-20

The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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br Materials and methods br Results br
2020-03-20

Materials and methods Results Discussion Cells in the human body, especially in the cardiovascular and musculoskeletal systems, undergo a variety of mechanical stimuli. In order to ensure human movement, the strength of stretching muscles acts on cartilage and bone, moving joints through te
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br Proteases with special focus on cysteine proteases br
2020-03-18

Proteases with special focus on cysteine proteases Vaccination using cysteine proteases as antigens with special emphasis on DNA-vaccines Concluding remarks In spite of the great potential of DNA vaccines, the technology has not been as revolutionary as expected in higher mammals. In fish,
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Zoniporide hydrochloride Natural and synthetic glucocorticoi
2020-03-18

Natural and synthetic glucocorticoids perform their biological action in the organism through receptor-dependent mechanisms (e.g., by binding to the glucocorticoid receptors). It has been determined that glucocorticoid receptors cross-talk with other nuclear receptors, including AhR (Celander et al.
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Besides the regulation of the stress responses CRF
2020-03-18

Besides the regulation of the stress responses, CRF and the urocortins have been implicated in drug addiction (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). For instance nicotine, the addictive substance of tobacco, can activate the HPA axis, just like any other stressor may do, although its imp
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Recently Schenck et al identified an active site asparagine
2020-03-18

Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat
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We experienced difficulties in observing maturation
2020-03-18

We experienced difficulties in observing maturation of hESC retinas in rd1 mice even with immunosuppression, but with NOG-rd1-2J mice the transplanted hESC retinas consistently developed mature ONL with rod and cone opsins. Furthermore, graft photoreceptors show signs of developing IS/OS structures
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Here we report for the first time that EphB
2020-03-18

Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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It has been reported that PGE increases expression of the
2020-03-18

It has been reported that PGE2 increases expression of the survivin mRNA (Baratelli et al. 2005) and promotes the stabilization of the survivin protein in some tumor pak4 (Krysan et al. 2003). However, it is unclear whether PGE2 affects the expression of survivin mRNA or promotes the stabilization o
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br Methods br Results br
2020-03-18

Methods Results Discussion With this study, we provided evidence that acriflavine can interfere with EMT and UPR, two well-described pathways associated with cancer aggressiveness. And, because drug resistance is also clearly associated with the mesenchymal state [36], blocking of the epith
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Several main strategies for targeting E s described
2020-03-18

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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