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Another milestone in the field is the de novo
2020-01-09
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of Phenacetin , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and b
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Herein in continuation of our interest
2020-01-09
Herein, in continuation of our interest in designing new DNA photocleavage agents [18], we report the synthesis, characterization and DNA binding and cleaving properties of a novel compound: trans-N,N-dimethyl-10,11-di(pyridin-4-ium)-10,11-dihydro-9,12-dioxobenzo[e]phenanthrene tetrafluoroborate (1)
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Studies of Jelski and Szmitkowski show that differences of
2020-01-09
Studies of Jelski and Szmitkowski show that differences of alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activity between cftr channel of many cancers and healthy tissue may be one of the factors intensifying carcinogenesis [7]. Moreover, changes of ADH and ALDH activity in cancer ce
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Aspergillus nigerA niger is another
2020-01-09
Aspergillus nigerA. niger is another filamentous fungus, in which alternative dehydrogenases have been described. Filamentous fungi are a very important group of microorganisms that are used in industry (O’Donnell et al. 2011). Biotechnological production processes using these organisms are often hi
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The discoidin domain receptors DDR and DDR
2020-01-09
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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Findings from this study also indicate that
2020-01-09
Findings from this study also indicate that DAPK regulated BimEL expression during OGD as DAPK shRNA transfection inhibited OGD-induced increase of BimEL. A previous study shows that Bim is found in ER compartment in stressed HO-3867 but not in normal cells, indicating translocation of Bim during E
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Since free testosterone diffuses into
2020-01-09
Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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Indeed some cancers may even be defined by
2020-01-09
Indeed, some cancers may even be defined by dysregulated cyclin and thus CDK activity: mantle cell lymphoma, an uncommon lymphoma of mature B cells, is defined by the presence of overexpressed cyclin D1, usually as a result of a translocation between chromosomes 11 and 14 with the net result that cy
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br Results and discussion br Conclusion In this investigatio
2020-01-09
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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Despite the significant increase in Bdnf mRNA levels
2020-01-09
Despite the significant increase in Bdnf1 mRNA levels after DNMT inhibition, the expression of Bdnf4 and Bdnf9 was unaltered. It is particularly surprising that Bdnf4 is not affected by the DNMT inhibitor, as the promoter of the Bdnf4 exon is known to be susceptible to epigenetic changes (Kotera et
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In patients with CTEPH ET levels are raised
2020-01-09
In patients with CTEPH, ET-1 levels are raised and have been shown to fall after PEA surgery [24]. After an acute pulmonary embolism there is obstruction of the pulmonary 5003 by acute thrombus and elevated levels of ET-1 [28], [30]. Elevated levels of ET-1 have also been observed in air embolus in
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Finally we demonstrated for the first time that the
2020-01-09
Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph
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Considering these reports and with the aim of
2020-01-09
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on
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In rodents Wang et al Wang and
2020-01-09
In rodents (Wang et al., 2003, Wang and Tsirka, 2005b, Zhu et al., 2012) and humans (Wang et al., 2011), the major forms of cell death after ICH are necrosis and apoptosis. In the perihematomal region of rodents, the number of necrotic and apoptotic cells peaks at 72h post-ICH (Matsushita et al., 20
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PF-562271 To provide a brief critical
2020-01-09
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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