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The optimization of the lead compound was initiated and
2021-05-18
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Isochlorogenic acid B moiety with other functional groups led to loss of functional activity against EP4
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br Iterative design approach overview An iterative design st
2021-05-18
Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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br Introduction Malaria remains a serious parasitic disease
2021-05-17
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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Interferon IFN induces formation of a heterotetrameric IFN
2021-05-17
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic TAPI-1 (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial growth factor (VEGF)-
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br Conflict of interest br Acknowledgements This work was su
2021-05-17
Conflict of interest Acknowledgements This work was supported by the Biotechnology Research Center, China Three Gorges University, Yichang, China (No. 2016KBC05), the National Natural Science Foundation of China (No. 31370600 and 31300508), the Zhejiang Science and Technology Major Program on
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br Genotype phenotype correlations Genotype phenotype correl
2021-05-17
Genotype-phenotype correlations Genotype-phenotype correlations are limited. Compared with individuals with truncating variants, those with pathogenic missense variants in the adenosine triphosphate binding site had a milder disorder, some with ability to walk unaided, better hand use, and less r
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Resveratrol is a phytoalexin that occurs in relatively
2021-05-17
Resveratrol is a phytoalexin that occurs in relatively large amounts in peanut, berries, grapes, and red wine (Soleas et al., 2001). A recent study showed that resveratrol prevents social deficit in an animal model of autism, indicating its potential for possible therapeutic use in children with aut
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Introduction Prolyl hydroxylation is a
2021-05-17
Introduction Prolyl hydroxylation is a widely observed post translational modification in collagen, an abundant animal protein. The high content (~13% per chain of the triple helical structure) of 4-hydroxyproline (Hyp,O) in collagen, togather with the natural abundance of collagen has led to the e
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Introduction br CK in the Regulation of Hh Pathway
2021-05-17
Introduction CK1 in the Regulation of Hh Pathway CK1 was initially identified as a negative regulator of Hh signaling at the level of transcription factor Ci by genetic studies in Drosophila and genome-wide RNAi screen in Drosophila cultured metalloproteinase (Jia et al., 2005, Lum et al., 2003
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Constitutive activity of Ras Raf MEK ERK pathway plays a
2021-05-17
Constitutive activity of Ras/Raf/MEK/ERK pathway plays a critical role on melanoma growth, thus inhibition of activity of Ras, Raf and MEK can reduce ERK activity, leading to a decrease in melanoma cell proliferation, survival and invasion (Burotto et al., 2014; Paluncic et al., 2016). Our results a
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Importantly our in vivo data fit to the
2021-05-17
Importantly, our in vivo data fit to the in vitro data, further confirming the synergistic effect of XJD and gefitinib on the inhibition of lung cancer and the regulation of SP1, HOTAIR, and EP4 flecainide acetate levels. The doses of XJD used were based on our previous in vivo study (Zhao et al., 2
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Treatment with AAV EP also improved aspects
2021-05-17
Treatment with AAV9-EP4 also improved aspects of adverse cardiac remodeling. The increased collagen deposition noted in the peri infarct and remote zone after MI was substantially attenuated by use of AAV9-EP4 and there were significant reductions in the number of macrophages and T Phos-tag Biotin
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In this paper we report the synthesis and microbiological ev
2021-05-17
In this paper, we report the synthesis and microbiological evaluation of a series of novel chromogenic sugar-based enzyme substrates based upon catechol, 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene 9 cores (Fig. 1).14, 15 2,3-Dihydroxynaphthalene is inexpensive and available in
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The role of ETB clearing receptors
2021-05-17
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous 5 alpha reductase of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all
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Recent reports revealed that CSE affects the endothelial cel
2021-05-17
Recent reports revealed that CSE affects the endothelial cells of various tissues like kidney, liver, heart including aspirin solubility [26,30]. The damage of brain endothelial cells enhances the progress of cognitive dysfunction due to the accumulation of toxic free bio-radicals and activation of
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