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Phenylbenzofurans are a very important
2019-07-22
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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To investigate the mechanism of action
2019-07-19
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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Besides the assessment of toxicological effects
2019-07-19
Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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To provide a brief critical evaluation of this technology
2019-07-19
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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br Acknowledgments Denise Fernandes acknowledges a postdoc f
2019-07-19
Acknowledgments Denise Fernandes acknowledges a postdoc fellowship (SFRH/BPD/34289/2006) from the Portuguese Fundação para a Ciência e Tecnologia (FCT) of the Ministry of Science and Technology of Portugal. This work was supported by the Spanish National Plan for Research (Project Ref. CGL2011-24
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From an industrial perspective the low turnover numbers and
2019-07-19
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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In Fig results of this experiment are shown as
2019-07-19
In Fig. 1 results of this experiment are shown as the contour plots of endopeptidase activity. Optimal for the enzyme production by this strain concentrations of peptone and inorganic phosphate were found to be 24 and 0.3g/l, respectively. For specific activity, the optima close to those for glutamy
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Although PKC in cancer cells is
2019-07-19
Although PKCδ in cancer SNX-2112 is known to promote antiapoptotic signaling, a cleaved form of PKCδ, δCF, has been reported to play a contrasting role in enhancing apoptosis (Reyland, 2007), and these complex functions appear to be cell-type dependent (Basu and Pal, 2010). In NSCLC, full-length PK
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Ubiquitin activating enzyme activates ubiquitin by a three s
2019-07-19
Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP product
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In addition to demonstrating the
2019-07-19
In addition to demonstrating the importance of DNMTs, we show that TGFβ1 differentially regulated DNMTs, and that TGFβ1 is both necessary and sufficient to induce lineage conversion of hepatocytes into MLCs with phenotypes and multipotency resembling MSCs. Upon withdrawal of TGFβ1 on day 28, we obse
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br Introduction Malaria remains a serious parasitic disease
2019-07-19
Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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It is well known that CysLTs exert potent contractile action
2019-07-19
It is well known that CysLTs exert potent contractile action on human bronchial smooth muscles through activation of CysLT1 receptors. Indeed, in vitro antigen-induced contraction of passively sensitized human bronchial tissue is markedly suppressed by a pre-treatment with CysLT1 receptor antagonist
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Previous studies reported that combined administration
2019-07-19
Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t
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br Acknowledgments Studies in the Tomkinson laboratory on DN
2019-07-18
Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as
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treat Recently naphthoquinone derivatives have shown promisi
2019-07-18
Recently, naphthoquinone derivatives have shown promising results as antiparasitic lead compounds [28]. Conjugated hybrid compounds could be an effective path to discovery of new drugs by associating two different pharmacophore groups with different mechanisms of action in a single molecule [29,30],
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