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In anticipation of an approach based on
2019-10-02
In anticipation of an approach based on modification of the cyclohexylacetic aromatase inhibitors subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to
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The small GTPase Ran regulates karyopherin cargo interaction
2019-10-02
The small GTPase Ran regulates karyopherin–cargo interactions and the directionality of karyopherin-mediated transport. Like other Ras-family GTPases, Ran cycles between GTP- and GDP-bound states, and the two surface loops in Ran, referred to as the switch I and switch II loops, undergo significant
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Taking into account that Gr dysfunction is involved in the
2019-10-02
Taking into account that Gr dysfunction is involved in the molecular mechanisms underlying HPA axis disorder (Li et al., 2017b) and Gr activity has been reported to be lowered in patients with severe mood disorders (Rush et al. 1996) and in adult rats (Green et al. 2016), PFOS could alter HPA axis a
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Present study observed failure of PPE usage by the majority
2019-10-02
Present study observed failure of PPE usage by the majority of workers, which may be notable problem and may create a significant health effects due to pesticide exposure. Non-usage of PPE and its ill effects have been reported among farmers in Brazil [24,25] and Nepal [26]. It was reported that use
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AON successfully alleviated the myotonic phenotype in DM mod
2019-10-02
AON successfully alleviated the myotonic phenotype in DM model mice [18], [23]. To screen for an optimal AON sequence, we used 25-mer phosphorothioate 2′ O-methyl RNA molecules that covered the exon 6B or exon 7A. Unexpectedly, AON 7A (+63−8) which covers the boundary of intron 7A and exon 7A enhanc
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We consider the following perturbation of problem where
2019-10-02
We consider the following perturbation of problem (2):where ∊>0 is an identity element. For a given ∊, we solve problem (3) to get the solution (x, y, λ). As ∊ decreases slowly toward 0, the optimum of F follows to the global optimum of F0. This set of constraint conditions is called the central pat
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br Results and discussion br
2019-10-02
Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of th
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Prostaglandin E PGE is involved in
2019-10-02
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 Funding This work was partly supported by the grant
2019-10-02
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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s6 kinase Recent pharmaceutical research in the field of res
2019-10-01
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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At ngL DEX did not affect
2019-10-01
At 3000ngL−1, DEX did not affect our investigated parameters, suggesting that DEX is regulated by CYP450 in a biphasic way, a response to xenobiotics that is not uncommon (Heinrichs et al., 1994). These data might also suggest that fish adapted to DEX exposure. It was previously shown that, dependin
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br Results and discussion Compounds were
2019-10-01
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Our present results support a major role
2019-10-01
Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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Our present results support a major role
2019-10-01
Our present results support a major role of EP1 receptors in peripheral heat sensitization and a smaller contribution to central heat sensitization but no contribution to mechanical sensitization. While the contribution of peripheral EP1 receptors to heat hyperalgesia is in good agreement with the a
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Acidosis has lethal consequences but alkalosis due
2019-10-01
Acidosis has lethal consequences, but alkalosis (due to chloride depletion, potassium depletion, and excess mineralocorticoid) is not tolerated as well (Luke and Galla, 2012). In this regard, efforts to restore pH to normal physiological level, in the most benign way should be the goal of researcher
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