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From the general synthetic route we
2020-09-27
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Another novel finding of our study was that
2020-09-27
Another novel finding of our study was that the global 5 hmC was down-regulated and was associated with a substantial reduction of TET expression in the PE placentas compared with the controls. The decreased global 5 hmC level was consistent with the increased global 5 mC level in the preeclamptic p
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Our approach relied on measurement
2020-09-27
Our approach relied on measurement of bulk solute diffusivity in the three tissue types of interest. Our diffusivity values (Table 3) are on the order of 10−6 cm2/s and are comparable to the PG diffusion coefficient in water at infinite dilution, which is about 10−5 cm2/s at room temperature, as wel
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Several studies have already shown that mPR activation can s
2020-09-25
Several studies have already shown that mPR activation can significantly reduce intracellular cAMP levels in different kind of cells, such as GT1-7 neuronal cells [32], MDA-MB-468 breast cancer cells [55] and primary vascular endothelial cells [56]. The experiments performed with PTXa and 8-Br-cAMP
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br Conflicts of interest br Acknowledgements This
2020-09-25
Conflicts of interest Acknowledgements This work was supported, in part or in whole, by the grants from the National Natural Science Foundation of China (11802056, 11772088), the China Postdoctoral Science Foundation (2018M640904), and the Fundamental Research Funds for the Central Universitie
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br Disclosure statement br Acknowledgements This
2020-09-25
Disclosure statement Acknowledgements This research was supported by grants from the National Institutes of Health, NS046400 and AG022971 (SD), and a fellowship from the Korea Research Foundation, KRF-2007-357-E00016 (YTK). The authors thank Dr. Barbara Crain for assistance with the immunologi
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aminoisobutyric acid BAIBA is a
2020-09-25
β-aminoisobutyric x04 (BAIBA) is a natural catabolite of the branched-chain amino acid thymine. BAIBA was recently found to reduce inflammation in skeletal muscle via the AMP-activated protein kinase (AMPK)-peroxisome proliferator-activated receptor (PPAR)δ signaling pathway. BAIBA reportedly enhanc
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In the present study we used
2020-09-25
In the present study, we used linagliptin, one of the commercially available DPP-4 inhibitors, because it has more long-lasting inhibition of DPP-4 activity than other drugs of this class. We hypothesized that linagliptin may interact with intercellular components, not only with DPP-4 on the plasma
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The three dimensional crystal structure of
2020-09-24
The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo
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br Acknowledgement This research was supported by a grant fr
2020-09-24
Acknowledgement This research was supported by a grant from the National Research Foundation of Korea (NRF-2013R1A1A2011238) funded to Young-Mi Lee. Introduction Stroke is considered a serious disease with high morbidity and high mortality. More than 6 million deaths are reported each year wo
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In the livers mefenamic acid ibuprofen and meloxicam
2020-09-24
In the livers, mefenamic acid, ibuprofen, and meloxicam significantly reduced expression of both 20-HETE and EETs synthesizing cyp450 genes (ANOVA, p value 0.05, Fig. 6). Control group: The lobular architecture and zonal accentuation in the liver of the control group were well preserved and kept i
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br Genotype phenotype correlations Genotype phenotype correl
2020-09-24
Genotype-phenotype correlations Genotype-phenotype correlations are limited. Compared with individuals with truncating variants, those with pathogenic missense variants in the adenosine triphosphate binding site had a milder disorder, some with ability to walk unaided, better hand use, and less r
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The Czech Republic is a country with
2020-09-24
The Czech Republic is a country with increasing CDI incidence (1.1 cases per 10,000 patient bed-days in 2008–4.4 cases in 2011–2012 and 6.2 cases per 10,000 patient bed-days in 2012–2013) (Bauer et al., 2011, Davies et al., 2014) and relatively high rates of antibiotic resistant C. difficile strains
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The CYP D inferred metabolizer phenotype describes only one
2020-09-24
The CYP2D6-inferred metabolizer phenotype describes only one phase of the tramadol (T) ADME (absorption, distribution, metabolism, and excretion) and response process and does not explain all genotypic contribution of an individual’s phenotypic expression [11]. Numerous polymorphisms in the downstre
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br Acknowledgements We are grateful to the National Natural
2020-09-24
Acknowledgements We are grateful to the National Natural Science Foundation of China (Grant Nos. 21571033 and 81503099) and the New Drug Creation Project of the National Science and Technology Major Foundation of China (Grant No. 2015ZX09101032) for financial aids to this work. The research was a
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