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Many PIM inhibitors have been reported to
2019-10-21
Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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Resistance to avermectins has been associated with point
2019-10-21
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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br The interaction network between the lncRNAs
2019-10-21
The interaction network between the lncRNAs which have been obtained from the previous steps, VDR and ESR was depicted using Cytoscape tool. Moreover, LncMAP tool (Li et al., 2018) was used to show transcriptional regulatory effects of two lncRNAs (MALAT1 and TBX5-AS1). The interaction network dep
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Fmoc-Arg(Pbf)-OH The same reservoir of genes
2019-10-21
The same reservoir of Fmoc-Arg(Pbf)-OH is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonable.
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Although several genomic technologies including the generati
2019-10-21
Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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Increased leukocyte trafficking and infiltration
2019-10-21
Increased leukocyte trafficking and infiltration of the vascular wall are thought to provide a key stimulus for SMC activation and subsequent neointima formation in response to vascular injury [19], [20]. The essential trigger regulating the accumulation of leukocytes in the vessel wall is the upreg
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Further modifications on the position of compound led
2019-10-21
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a pow
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The contribution of local ETA and ETB receptors towards
2019-10-21
The contribution of local ETA and ETB receptors towards heat hyperalgesia induced by inoculation of XC tumor PF-00562271 in the paw of mice has been demonstrated by Baamonde and colleagues (Baamonde et al., 2004). Furthermore, using neuropathic and inflammatory nociception models, several studies h
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br Materials and methods br Results
2019-10-21
Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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In the phase I AURA trial patients
2019-10-21
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for odm 201 19 deletions, 86% for L858R and
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br Discussion Nowadays data of uncommon EGFR mutations are
2019-10-21
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
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As mentioned above there are two major
2019-10-21
As mentioned above, there are two major pathways for the DSB repair in mammalian cells, NHEJ and HR/HDR (homology-directed repair) [13], [51]. NHEJ is active throughout the cell cycle, predominately during the G0 and G1 phases and is considered the major pathway for the DSB repair in human cells [52
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Acknowledgments We acknowledge the Danish Council for Indepe
2019-10-21
Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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Then we explored the MCLEIA methodology parameters including
2019-10-21
Then, we explored the MCLEIA methodology parameters including precision, accuracy and specificity. In the 0.5–128 ng/mL, the standard curve equation was = 0.5014 + 1.769 ( was log, was RLU/RLU with a correlation coefficient of 0.9907) (). On the one hand, same sample (0.5, 4.0, 32.0 ng/mL) detecte
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CYP enzymes have an important role in
2019-10-19
CYP450 MAFP have an important role in microsomal oxidase function across a broad range of taxa (Pakharukova et al., 2012). They are involved in metabolism and detoxification of both internally generated compounds and xenobiotics as the phase I metabolizing enzymes and play an important role in main
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