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The activity of chromenones bearing heteroaryl
2019-10-07

The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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Interestingly all three lesions that
2019-10-07

Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of SC 79 residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleotides opposite AP-sites and bulky les
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Under conditions of energy scarcity or nutritional restricti
2019-10-07

Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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Resistance to avermectins has been associated with point mut
2019-10-07

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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The redox sensitive transcription factor NF B is reported to
2019-10-07

The redox sensitive transcription factor NF-κB is reported to play a crucial role in the COPD pathogenesis via up regulating the expression of several cytokines, chemokines, growth factors, and adhesion molecules [71]. Incidentally, we and others have shown that PARP-1 modulates the NF-κB activation
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ELUXA HM EMSI is an ongoing pivotal Phase
2019-10-07

ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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2-Deoxycytidine Our data furthermore suggest that Ch h induc
2019-10-07

Our data furthermore suggest that Ch25h-induced oxysterols could play an important role in modulating the immune cell migration. Mechanistically, we observed impaired trafficking of CD44+CD4+ T cells in mice deficient for Ch25h. CD44+CD4+ T cells lacking EBI2, the receptor of 7α-25OHC, were delayed
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The E enzyme is the apex for downstream enzymatic
2019-10-07

The E1 enzyme is the apex for downstream enzymatic cascades and signaling pathways mediated by Ub and Ub-like proteins (Ubls) (Pickart, 2001). Studying characteristics of E1 and its catalytic functions may throw light to the role of ubiquitination in cell development. All known eukaryotic E1 are mon
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Two isoforms of intracellular ER ER
2019-10-07

Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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In the present study we
2019-10-07

In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2019-10-05

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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Colony stimulating factor receptor CSF R or cFMS is a
2019-10-05

Colony stimulating factor-1 receptor (CSF-1R or cFMS) is a type III receptor tyrosine kinase. It is activated by binding with CSF-1 and IL-34, which stimulates differentiation, proliferation, survival and migration of monocyte-macrophage lineage cells., , , Also, macrophages produce inflammatory me
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This work started from the standard
2019-10-05

This work started from the standard version of the CPA model [17] and investigated its known weaknesses: 1) not meeting the defined critical temperature, 2) missing the temperature dependence of pure component saturated liquid densities, 3) using an α function in the cubic term that can provide unre
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Abbas et al studied the mitigation of
2019-10-05

Abbas et al. studied the mitigation of ASR in their corresponding study by incorporating RHA [1]. These researchers used Ordinary Portland Cement (OPC), four different percentages (i.e., 10%, 20%, 30% and 40% by weight of OPC) of RHA and reactive aggregate (sand from Dolomite-limestone rock) in thei
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The following are the supplementary data related to this art
2019-10-05

The following are the supplementary data related to this article. Acknowledgments Introduction Cyclooxygenases metabolize arachidonic PyBOP to five primary prostanoids, PGE2, PGF2, PGI2, TXA2 (TX), and PGD2. These lipid mediators interact with specific members of a family of distinct G-prote
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