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Foretinib br Conclusion The past few years have witnessed su
2019-08-07
Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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br Methods br Results br Discussion With this study we
2019-08-07
Methods Results Discussion With this study, we provided evidence that acriflavine can interfere with EMT and UPR, two well-described pathways associated with cancer aggressiveness. And, because drug resistance is also clearly associated with the mesenchymal state [36], blocking of the epith
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Boulares group has demonstrated that
2019-08-07
Boulares group [82] has demonstrated that the NF-κB1/p50 NF-κB, a family member of type I NF-κB, is an excellent substrate for DNA-PK, which-dependent phosphorylation of NF-κB1 at serine 20 appears to enhance its binding to DNA as either a homodimer or a heterodimer with p65 NF-κB and the ability of
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Given the excellent in vitro pharmacology profiles
2019-08-07
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic p-gp inhibitors functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT
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br The contribution of Interference RNA and
2019-08-07
The contribution of Interference RNA and epigenetic in OA attenuation Interference RNA, a cellular mechanism for post-transcriptional gene silencing that is associated with mRNA. The potential of RNAi has successfully silenced the wide range of protein coding genes. Its high specificity sanctions
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Published results have revealed relationships between serine
2019-08-07
Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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To better understand the mechanism of splicing in CLCN we
2019-08-07
To better understand the mechanism of splicing in CLCN1, we began by constructing a minigene spanning exons 5–7 of CLCN1, resulting in the synthetic CLCN1 (5–7) minigene. We also established a new assay using real-time reverse transcription (RT)-PCR, which can distinguish between splicing variants b
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Calcium dependence of CaM target
2019-08-07
Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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The all NTP pyrophosphatase and NUDIX families maintain the
2019-08-07
The all-α NTP pyrophosphatase and NUDIX families maintain the deoxynucleotide triphosphate (dNTP) pool balance, limit the incorporation of harmful nucleotides, and represent a promising therapeutic approach to develop anticancer and immunosuppressive agents., , , , Among these housekeeping enzymes
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We hypothesized that the atopic phenotype may be
2019-08-07
We hypothesized that the atopic phenotype may be partially influenced by an altered binding and/or signalling due to the amino-acid substitution in the receptor protein. The principal aim of this study was to investigate the signalling mechanisms of the variants CysLT1-G300S and CysLT1-I206S induced
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ARA metabolites which are produced through cytochrome P
2019-08-07
ARA metabolites, which are produced through cytochrome P450 (CYP450) enzymes influence cardiovascular homeostasis. Human CYP4A11 and CYP1A2 metabolize ARA to 20-hydroxyecostearonic ZD 7288 (20-HETE) [11], which is a vasoconstrictor [12], platelet activator [13] and naturetic in the kidney [14]. On t
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Telenzepine dihydrochloride br Conflicts of interest br Intr
2019-08-06
Conflicts of interest Introduction Diacylglycerols (DAGs) and phosphatidic Telenzepine dihydrochloride (PA) play fundamental roles in biology as basic components of membranes, intermediates in lipid metabolism, and secondary messengers in cellular signaling (Carrasco and Merida, 2007, Fang et
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br Acknowledgements The study was supported by
2019-08-06
Acknowledgements The study was supported by grant no. 501-003-11043 from the Institute of Psychiatry and Neurology in Warsaw. The authors thank Mrs. Ala Biegaj for the excellent technical assistance. Introduction In an effort to identify hIFN receptor molecules encoded by a gene(s) within hum
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In silico modelling studies might aid
2019-08-06
In silico modelling studies might aid our understanding of the functionality and potential biological activity of food and, in the long-term they might underpin the development of personalised diets to reduce health risks and help us to better understand pharmaceutical/food interactions. Acknowle
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br Discussion Nowadays data of uncommon EGFR
2019-08-06
Discussion Nowadays, data of uncommon EGFR mutations are limited, considering that patients carrying these rare alterations are usually excluded from clinical trials. Available survival data of activity of EGFR TKIs on this class of mutations, coming from a small number of usually retrospective s
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