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Initial investigations in the heart uncovered Epac
2019-10-08
Initial investigations in the heart uncovered Epac as a positive regulator of myocyte hypertrophy [8], [9]. Concomitantly, Epac has been shown to regulate cardiac Ca homeostasis [8], [10], [11], [12], [13]. Ca is an essential second messenger in the cardiac physiology because its rhythmic variations
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Malotilate Besides EGFR other tyrosine kinase
2019-10-08
Besides EGFR, other tyrosine kinase receptors are currently gaining attention as potential therapeutic targets. Included among these is the fibroblast growth factor receptor (FGFR) family, which is involved in the progression of a variety of cancers.7, 8, 9, 10, 11 In lung cancer, fibroblast growth
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Compound C mass Modulating protein stability specifically in
2019-10-08
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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To date many studies have reported significant aberrant
2019-10-08
To date, many studies have reported significant aberrant methylation patterns in TIMPs in various types of cancer 4EGI-1 and [[16], [17], [18]]. However, little has been reported on the events that lead to the methylation of TIMPs in the UV-irradiated human skin. Therefore, the objective of this st
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In neurodegenerative disorders neurons are
2019-10-08
In neurodegenerative disorders neurons are excited by enormous ionic flow which induces mitochondrial dysfunction and apoptosis. Glutamate as the main excitatory neurotransmitter, is released excessively in these diseases. Glutamate acts through N-methyl-d-aspartate (NMDA) receptor and α-amino-3-hyd
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In addition to the blockade of airway smooth
2019-10-08
In addition to the blockade of airway smooth muscle contractions, CysLT1 receptor antagonists also exerted a potent anti-inflammatory effect at this level. The oral administration of MEN91507, Pranlukast, Montelukast, and Zafirlukast also produced a long-lasting inhibition of leukotriene D4-induced
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Compounds were prepared via the routes shown
2019-10-08
Compounds were prepared via the routes shown in , varying the sequence of reactions to install the thiazole or the phenyl ring at the end of the synthesis (pyridyl examples were prepared using similar chemistry). The aminothiazole building blocks were prepared as shown in . 5-Aminothiazole was prep
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Considering all these facts in the
2019-10-08
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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Caspi et al first identified that the
2019-10-08
Caspi et al. (2005) first identified that the COMT polymorphism moderated the influence of adolescent cannabis use on developing adult psychosis (Caspi et al., 2005). In particular, compared to Met carriers, subjects with the Val/Val genotype were most likely to exhibit psychotic symptoms and to dev
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br Introduction The cys loop ligand gated ion channels LGICs
2019-10-08
Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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Introduction The physiological significance of hypoxia
2019-10-08
Introduction The physiological significance of hypoxia is undisputed, although largely over looked in the cancer therapeutics field focused on DNA-damage induced by ionizing radiation or drug treatment. Regions of hypoxia occur during a range of diverse biological situations including embryogenesis
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br Acknowledgment We thank Professor Yuh
2019-10-07
Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi
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In contrast crystal structures of the oxyester linked Ubc
2019-10-07
In contrast, crystal structures of the oxyester-linked Ubc13 and UbcH5b conjugates (Eddins et al., 2006, Sakata et al., 2010), and the NMR structure of the disulfide-linked UbcH8 conjugate (Serniwka & Shaw, 2009), revealed distinct open conformations (Fig. 10.3). In part, differences in the position
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In light of the overall loss of activity
2019-10-07
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Several reports have exploited the
2019-10-07
Several reports , , , , have exploited the application of HRM for detecting differentially methylated DNA. Even though DNA methylation analysis by HRM cannot determine the methylation status of individual CpGs, it does provide a robust and inexpensive method to differentiate DNA based on the overall
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