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br Conflict of interest br Acknowledgments Dr Hauger
2020-01-21
Conflict of interest Acknowledgments Dr. Hauger was supported by a BLR&D Merit Review grant from the Department of Veterans Affairs, Veterans Health Administration, Office of Research and Development. Dr. Hauger also received support from the VA Center of Excellence for Stress and Mental Healt
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Therapeutic options targeting intrahepatic resistance
2020-01-21
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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ERR and ERR share high sequence
2020-01-21
ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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Our previous high throughput screening HTS
2020-01-21
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based mi2 mg assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23], [
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br Materials and methods br Results discussion br Conclusion
2020-01-21
Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro
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To study the effect of DDR inhibition by imatinib
2020-01-21
To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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Compression The L vertebral body
2020-01-21
Compression: The L4 vertebral body was tested in compression with loads applied along the craniocaudal axis using an Instron 8800 device at a rate of 3mm/min. Load displacement data were captured using Bluehill software. The ultimate load, yield load, stiffness, ultimate stress, yield stress and You
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arginase inhibitor br GPCRs form heterotetramers In
2020-01-21
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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br Competing interests br Acknowledgements br
2020-01-21
Competing interests Acknowledgements Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) in biomembranes to produce phosphatidic survivin (baculoviral IAP repeat-containing protein 5) (21-28) (PA) [1], [2], [3], [4], [5], [6]. To date, ten mammalian DGK isozymes (α,
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2580 receptor Dgat mice however had less
2020-01-21
Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e
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Steady state mRNA levels of CYP A
2020-01-21
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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br Conflicts of interest br Acknowledgements br Lung cancer
2020-01-21
Conflicts of interest Acknowledgements Lung cancer continues to be the leading cause of cancer deaths in the US and worldwide., Non–small-cell lung cancer (NSCLC) remains the predominant form of lung cancer (approximately 85%)., With some improvements in surgical techniques and combined ther
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Based on both the observational and theoretical data generat
2020-01-21
Based on both the observational and theoretical data generated in this study, it appears that the mechanism(s) underlying lower IFM CPT1 activity is complex. Modeling enzyme activity versus alterations in catalytic efficiency (Fig. 3A) suggests that the observed age-associated changes in Km and Vmax
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MdHCLB channels expressed in Xenopus oocytes produced curren
2020-01-21
MdHCLB channels expressed in Xenopus oocytes produced currents in response to HA and GABA (Fig. 1, Fig. 3). This is in agreement with the findings with Drosophila HCLB channels (Gisselmann et al., 2004). In the HA concentration-response curves, the effects of GABA were additive to those of HA only i
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Although the analysis described above goes far to explain
2020-01-21
Although the analysis described above goes far to explain the mechanism of NS 11021 perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and PI3K-AKT pat
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