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Nevertheless because of the preclinical work and the interfe
2020-07-11
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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In summary we have identified a series of
2020-07-11
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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br Acknowledgments br Significance The mechanisms
2020-07-11
Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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gsk3 inhibitor br Sources of funding br Disclosures
2020-07-11
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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The MOF system described by Farha and coworkers
2020-07-11
The MOF system described by Farha and coworkers combines rational design of the support and good experimental results regarding activity and stability. However, a further increase in the speed of enzyme loading into the MOF and a decrease in leaching are still required. How can the design rules prop
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The cytoplasmic domain of classical cadherins is highly
2020-07-11
The cytoplasmic domain of classical cadherins is highly conserved and can interact with different cytosolic proteins. Typically this domain is associated with catenin family members, including p120 catenin, β-catenin, and α-catenin, which form a cadherin-catenin complex (Fig. 1). The catenin family
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While oxysterols were most extensively studied for its poten
2020-07-11
While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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Typical examples of CO utilization
2020-07-10
Typical examples of CO2 utilization and reduction technologies are catalytic reduction of CO2 to C1 compounds such as CO, formic acid, methanol and so on [[3], [4], [5], [6], [7], [8], [9], [10]], and catalytic organic synthesis using CO2 as a feedstock [[11], [12], [13], [14], [15], [16], [17], [18
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Overexpression of EP and DDR has been sporadically
2020-07-10
Overexpression of EP300 and DDR1 has been sporadically reported in the pathogenesis of pulmonary fibrosis and other fibrotic diseases. Zeng et al. reported that EP300 was increased in TGF-β1 treated lung fibroblasts and mediated decreases of SIRT1 expression. Bhattacharyya et al. found that both EP3
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2-D08 In vivo study showed that the CYP A activity was
2020-07-10
In vivo study showed that the CYP3A activity was increased, when morroniside (10, 30 and 90 mg/kg, i.g.) was daily for seven consecutive days. Further, RT-PCR analysis showed that the induction of mRNA 2-D08 by morroniside (10, 30 and 90 mg/kg, i.g.) was 1.13-, 1.43- and 1.79-fold higher, respectiv
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By live imaging of GUL GFP we
2020-07-10
By live imaging of GUL-1-GFP, we observed the kinetics of aggregate movement within the cell. One of the marked characteristics of GUL-1-GFP cytosolic (but not nuclear-associated) aggregate motion was a “comet-like” movement that was found to be dependent on the presence of properly polymerized micr
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Cx platin could improve the level of
2020-07-10
Cx-platin could improve the level of cellular uptake and DNA platination, hence triggering distinct DNA damage repair pathways. The data (Fig. 3B, C and D) demonstrated that Cx-platin could increase the foci number of γH2AX in cancer cells, preventing the efficient DSBs repair. This gives a good exp
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Yu et al also reported that extracting consortium of
2020-07-10
Yu et al. [24] also reported that extracting consortium of hydrolytic enzymes from sludge flocs performs better than costly single purified commercial enzyme. Thus, it is concluded from the above cited literature analysis that only few studies have been reported on extraction of enzymes from waste s
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br Results br Discussion Fetal development occurs under cond
2020-07-09
Results Discussion Fetal development occurs under conditions of low oxygen tension and steady maternal glucose such that physiologic systems including the pancreas are functionally poised in the prenatal state. Postnatally, oxidative metabolism becomes dominant and intermittent feeding exposes
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EC barrier dysfunction triggered by inflammatory mediators i
2020-07-09
EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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