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Based on the above we hypothesized that a PROTAC strategy
2019-07-03

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Over the past decade targeting DNA repair
2019-07-02

Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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Thus DGK active sites remain ill defined
2019-07-02

Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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Though the physiological roles of microglia derived elastase
2019-07-02

Though the physiological roles of microglia-derived elastases in the CNS are not well understood, their involvement in the metabolism of cholecystokinin [41] and in the processing of plasminogen to produce a low molecular weight plasminogen that enhances neurite outgrowth has been reported [38]. Exp
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For statistical analysis the Statistical
2019-07-02

For statistical analysis, the Statistical Package for Social Sciences (SPSS) was used (version 21.0; SPSSInc., Chicago, IL). Chi-square (x2) exact test was used for the comparison of categorical data, whereas Wilcoxon and Mann–Whitney U tests were used for the analysis of nonparametric variables bas
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Recently a method for in
2019-07-02

Recently, a method for in vivo photoactivation of semagacestat molecular expressing PA-GFP in precise microanatomical compartments was described (Victora et al., 2010), which makes it possible to optically mark Tfh cells and track them 20 hr later (Shulman et al., 2013). Unexpectedly, it was report
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First we synthesized inhibitor following the patent
2019-07-02

First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidine
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dpn The conventional medical therapy for IBD consists
2019-07-02

The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f
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In this study we observed alterations
2019-07-02

In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased parp inhibitors when the sensitization condition was established. Similarly, CRF2 receptor
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Recently we have observed that pharmacological PPAR
2019-07-02

Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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Similarly to other investigations the
2019-07-02

Similarly to other investigations, the present study found that ZEA in high concentrations decreases viability of both normal (Liu et al., 2018, Zheng et al., 2018a, Zheng et al., 2018b) and cancer ubiquitin e3 ligase (Khosrokhavar et al., 2009, Kowalska et al., 2017). The toxic effect of ZEA obser
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In this study we investigated the role
2019-07-02

In this study we investigated the role 17-phenyl tinor (pt)-PGE2 on endothelial barrier function and the underlying molecular mechanism in HMVEC-Ls as well as in a murine model of LPS-induced acute pulmonary inflammation. We found that 17-pt-PGE2 concentration-dependently enhanced endothelial barrie
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Previous research has suggested that
2019-07-01

Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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Rat pheochromocytoma PC cells have been widely
2019-07-01

Rat pheochromocytoma PC12 cells have been widely used as a cell system to study intracellular signaling leading to neurite outgrowth. The advantages of using PC12 cells in the CHK studies are the fact that they naturally express the rat form of CHK and the observation that down-regulation of CHK fun
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In conclusion through a series of experiments we showed
2019-07-01

In conclusion, through a series of experiments we showed that our antigen LALF32-51-E7 combined with alum adjuvant promotes a Th1 immune response and consequently an anti-tumor response in the TC-1 tumor model. Based on our results, we suggest not to underestimate the capacity of Al(OH)3 as adjuvant
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