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Given the potency enhancing effect of the butyl
2019-11-22
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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Our study revealed elevated basal Akt phosphorylation in die
2019-11-22
Our study revealed elevated basal Akt phosphorylation in diet-induced obesity, the effect of which was reversed by ETAKO. Activation of Akt promotes cardiac hypertrophy via a number of cellular mechanisms including activation of its downstream targets such as mTOR and GSK3β [45, 46]. Short-term acti
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It has previously been established that DDRs play
2019-11-22
It has previously been established that DDRs play an important role in collagen regulation in at least two distinct ways: (1) activation of DDRs by collagen results in up-regulation of the matrix metalloproteinases, which results in cleavage and degradation of the ECM20., 21., [22] and (2) Sildenafi
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To further define the importance
2019-11-22
To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H
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To further determine the cell death
2019-11-21
To further determine the cell death, the CHZ868 receptor in flasks were harvested after OGD or LTD4 treatment, washed twice with PBS, and evaluated with Annexin V (AV)-FITC apoptosis detection kit I (BD Biosciences Pharmingen, USA) on a flow cytometer (FACSCalibur, Becton–Dickinson, USA). Briefly, 1
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In the present study we investigated the effect of morphine
2019-11-21
In the present study we investigated the effect of morphine withdrawal on G-protein coupling to opioid and ET receptors in neonatal rats. Morphine-induced G-protein activation was significantly higher in neonatal rats undergoing morphine withdrawal; suggesting enhanced coupling of the receptors to G
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Similarly in the EAE model Chalmin et
2019-11-21
Similarly in the EAE model, Chalmin et al. previously demonstrated that EBI2 and CH25H might be responsible for the efficient egress of differentiated Th17 cells from the draining lymph nodes [31]. As discussed above, in active EAE we did not find differences in EAE development and only the transfer
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br Acknowledgements br This work
2019-11-21
Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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ARA metabolites which are produced through cytochrome P
2019-11-21
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic Flurbiprofen (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney [14].
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One strategy which is different from the above is
2019-11-21
One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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Previous studies have shown the harmful
2019-11-21
Previous studies have shown the harmful effects of NEFA on ovarian functionality, such as inhibition of bovine granulosa cell survival and proliferation, steroidogenesis, and follicular development and alteration in oocyte development [36,45,46]. Therefore, the higher levels of NEFA found in the fol
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Abdominal aortic aneurysm AAA is
2019-11-20
Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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Another critical finding in this study is that
2019-11-20
Another critical finding in this study is that the level of αSyn oligomers in the SN of σ1R−/− mice was progressively increased with age, whereas the levels of αSyn monomers and αSyn messenger RNA (data not shown) were not altered compared to WT mice. A number of studies reported that soluble αSyn m
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Proof of concept studies with disulfiram suggest the potenti
2019-11-20
Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d
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dexamethasone acetate br Conclusions In this paper
2019-11-20
Conclusions In this paper we describe the recombinant expression and characterization of ParI, a C5-DNA-MTase from P. arcticus 273–4. To our knowledge, this is the first characterization of an orphan C5-DNA-MTase from a psychrophilic bacterium. The C5-DNA-MTase could not be expressed in regular E
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