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A phenylacetic acid derivative discovered in a high throughp
2019-07-12

A phenylacetic Losartan what derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediate
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The notion that a small subset of
2019-07-12

The notion that a small subset of inducible cellular transcripts, encoding immunological important factors, is translocated across the nuclear envelope by the karyopherin CRM1 is gaining support from various recent studies. For example, experimental evidence has been provided demonstrating that the
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br Results and discussion br Conclusion
2019-07-12

Results and discussion Conclusion Experimental section Pharmacological studies Introduction Survival analysis is a set of statistical methods that aim at modeling the relationship between a set of predictor variables and an outcome variable and, in particular, prediction of the time w
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The hepatic constitutive levels of CYP
2019-07-12

The hepatic constitutive levels of CYP1A2 were minimal and were below detectable limits in the kidney, indicating an organ-specific trend which has been reported by other groups (Hawke and Welch, 1985, Paolini et al., 1997, Parkinson, 1996, Villard et al., 1998). Retinol administration did not have
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ER redox imbalance leads to the accumulation
2019-07-12

ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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ERR is expressed in several adult and embryonic
2019-07-12

ERRγ is expressed in several adult and embryonic tissues but its biological role is still largely unknown [21]. Overexpression of ERRγ in breast cancer correlates with a favorable outcome [22]. In addition, ERRγ has been reported to inhibit the growth of prostate tumor (S)-10-Hydroxycamptothecin [2
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The aim of the present study was to
2019-07-11

The aim of the present study was to investigate the acute effects of THC on resting state the person neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological MRI study. Ac
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Here we report for the first
2019-07-11

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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br Sources of funding br Disclosures br Acknowledgments br I
2019-07-11

Sources of funding Disclosures Acknowledgments Introduction Insulin secretion from pancreatic β cells is a fundamental process to maintain blood glucose homeostasis. During glucose-stimulated insulin secretion, high glucose causes closure of ATP-sensitive K+ channels (KATP channels), sub
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In rodents Wang et al Wang and
2019-07-11

In rodents (Wang et al., 2003, Wang and Tsirka, 2005b, Zhu et al., 2012) and humans (Wang et al., 2011), the major forms of cell death after ICH are necrosis and apoptosis. In the perihematomal region of rodents, the number of necrotic and apoptotic cells peaks at 72h post-ICH (Matsushita et al., 20
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The synthetic route chosen for the preparation
2019-07-11

The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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The applications of fungal enzymes in paper industry
2019-07-11

The applications of fungal enzymes in paper industry involve biobleaching of pulp, pulp de-inking, degradation of dissolved and suspended organic compounds in concentrated effluents of mills and enhanced fibrillation. Enzymes usage is encouraged in paper industry in order to reduce the use of chemic
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Naltrindole hydrochloride br Acknowledgments This work was s
2019-07-11

Acknowledgments This work was supported by Région Auvergne “Nouveau chercheur”. This study has been performed with the assistance of Christelle Damon-Soubeyrand for histology technical assistance using “Anipath” Platform (GReD) and Sandrine Plantade, Keredine Ouchen and Philippe Mazuel for animal
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The inhibition of DNMT using AZA dC or
2019-07-11

The inhibition of DNMT1 using 5-AZA-dC or DNMT1 siRNA increased TIMP2 protein and mRNA expression, suggesting that TIMP2 expression is down-regulated by DNA methylation in the HDFs. In addition, 5-AZA-dC treatment led to a dose-dependent decrease of DNMT1 protein expression. 5-AZA-dC is a cytosine a
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br Results and discussion br Conclusion
2019-07-11

Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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