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Previous synthetic lethal screening efforts
2020-10-15

Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s
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Introduction Formate dehydrogenase enzymes FDHs are a
2020-10-15

Introduction Formate dehydrogenase enzymes (FDHs) are a group of heterogeneous proteins that catalyse the reversible formate () oxidation to carbon dioxide () (Eq. (1)). These enzymes are classified in two families, one gathering the enzymes that hold no redox-active centres and another that includ
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perifosine br Transparency document br Acknowledgements This
2020-10-15

Transparency document Acknowledgements This work was supported by research grant G092715N of the Research Foundation Flanders (FWO). The authors are indebted to Drs. V. Baekelandt and E. Lobbestael (Research Group for Neurobiology and Gene Therapy, KU Leuven) for stimulating discussions and he
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Introduction Tumor necrosis factor TNF is a pro inflammatory
2020-10-15

Introduction Tumor necrosis factor (TNF) is a pro-inflammatory mediator with the capacity to induce apoptosis (Benderska et al., 2012). Recent reports have shown that TNF might trigger cell death, at least in part, by directly affecting the reorganization of the gamma-Glu-Cys cytoskeleton (Campos
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Rivaroxaban Additionally of outmost important is the locatio
2020-10-14

Additionally, of outmost important is the location of the different CpG islands in relation to the transcription starting site (TSS) of the promoter as well as their interaction with transcription activators or repressors. It has been shown that methylation at the downstream region of the TSS in the
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There are some limitations to our study First the small
2020-10-14

There are some limitations to our study. First, the small sample size, even if comparable or higher than most studies, did not offer the possibility to consider other variables, such as frequency of use or age of onset. Second, since most subjects did not report current use, we could not analyze sep
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SPR was used to measure biomolecular
2020-10-14

SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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From the results of previous experiments with the purvalanol
2020-10-14

From the results of previous experiments with the purvalanol B affinity matrix, it is not clear whether the selective capture of parasite CK1 enzymes is a reflection of their high abundance or rather their affinity for the ligand compared with other kinases present in the lysates. Based on compariso
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Prostaglandins PGs in particular PGE and PGF play pivotal ro
2020-10-13

Prostaglandins (PGs), in particular PGE2 and PGF2α, play pivotal roles in human parturition by stimulating cervical ripening, myometrial contraction and fetal membrane rupture (Challis et al., 1997). In human pregnancy, the amnion is the principle source of PGE2 (Duchesne et al., 1978). In the amnio
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br The synthesis of these
2020-10-13

The synthesis of these antagonists relied heavily on Stille and Suzuki coupling reactions. The preparation of the required building blocks is presented in . Reduction of ethyl 6-bromo-2-pyridinecarboxylate with diisobutylaluminum hydride in tetrahydrofuran followed by treatment with triisopropylsi
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To develop antagonists selective for the mouse EP receptor w
2020-10-13

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Harmine mg () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde
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Covalent inhibitors are well suited for targeting the
2020-10-13

Covalent inhibitors are well suited for targeting the E1 MK-3207 HCl of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in cir
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Enolases are among the most abundantly expressed
2020-10-13

Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pro
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Another critical finding in this study is that the
2020-10-13

Another critical finding in this study is that the level of αSyn oligomers in the SN of σ1R−/− mice was progressively increased with age, whereas the levels of αSyn monomers and αSyn messenger RNA (data not shown) were not altered compared to WT mice. A number of studies reported that soluble αSyn m
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br EBV BILF A Virus Encoded TM Receptor with
2020-10-13

EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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