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Epac proteins consist of a
2019-07-09
Epac proteins consist of a carboxyl-terminal catalytic region and an amino-terminal regulatory region, which harbors one cAMP-binding domain in Epac1 and two in Epac2 [22], [32], [51]. In the absence of cAMP, the regulatory region covers the CDC25-homology domain and autoinhibits Epac\'s enzymatic a
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Since OH PGE is a moderately selective EP agonist which
2019-07-09
Since 1-OH-PGE2 is a moderately selective EP4 agonist which could bind to mouse EP3 and EP4 with a relatively similar affinity (Kiriyama et al., 1997), we have used a highly selective EP4 agonist CAY10580 to evaluate the involvement of EP4 activation in PGE2-facilitated EP4 internalization and recyc
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The Penicillium strain used in this work was isolated
2019-07-09
The Penicillium strain used in this work was isolated from Atlantic forest soil and previously screened as lipase producer (Tauk-Tornisielo et al., 2005). The immobilization was previously evaluated using hydrophobic supports, i.e. agarose based butyl-(But), phenyl-(Phe) and octyl-Sepharose (Oct), a
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In principle in vitro techniques for assessing enzyme
2019-07-09
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized 4-P-PDOT lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA en
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br Analytical improvements Since our review of Oxysterol Met
2019-07-09
Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana
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Downregulation of tumor suppressors is a major factor
2019-07-09
Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the porcine what of which is often downregulated or even absent in the majority of human cancers, functions as a phosphatase
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External factors such as protein partners can
2019-07-09
External factors, such as protein partners, can also activate DUBs by either reinforcing the stimulatory effects of intramolecular factors or by other means. The intramolecular activation of the USP7 CD by its HUBL domain is allosterically potentiated by external factor GMP synthase (GMPS), which co
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br Introduction Pattern separation is the
2019-07-09
Introduction Pattern separation is the ability to make distinct representations from highly overlapping information, a process which is important for memory encoding (Clelland et al., 2009). For correct pattern separation, old information needs to be retrieved and compared to new information. If
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br Chagas disease Chagas disease
2019-07-09
Chagas disease Chagas disease, an NTD caused by the protozoan Trypanosoma cruzi, affects 8–10 million people globally. More than 10,000 deaths are caused by the disease each year, and nearly 70 million people are susceptible to infection (Manne-Goehler, Umeh, Montgomery, & Wirtz, 2016). Chagas di
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Cell migration and invasion are central processes
2019-07-08
Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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Several in vivo human studies have produced conflicting
2019-07-08
Several in vivo human studies have produced conflicting results for evaluating the inhibition of OCs on the metabolism of CYP3A substrates. Balogh et al. [12] demonstrated an approximately 25% inhibition of CYP3A activities in vivo after the administration of an OC containing 30μg of ethinylestradio
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In conclusion we demonstrated phenoconversion of CYP A in st
2019-07-08
In conclusion, we demonstrated phenoconversion of CYP3A in stable kidney transplant recipients, and that higher plasma indoxyl sulfate concentrations in these subjects may be involved in the phenomenon. The present findings suggest that dose adjustment of drugs metabolized by CYP3A may be needed in
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br Conflicts of interest br
2019-07-08
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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Our previous high throughput screening
2019-07-08
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based AR-M 1896 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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hexokinase regulation We initially identified four putative
2019-07-08
We initially identified four putative Egr1 hexokinase regulation (−39/−36, −105/−102, −107/−104, and −227/−224) on the DBH proximal promoter. The deletion and mutagenesis experiments indicate that the motif at −227/−224 is required for Egr1-elicited reduction in DBH promoter activity. It remains to
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