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Increasing age among middle aged subjects years old was asso
2020-06-20

Increasing age among middle-aged subjects (30–59years old) was associated with higher levels of cholesterol synthesis markers (although without statistical significance) and also of cholesterol nadph oxidase inhibitor markers (with statistical significance for campesterol and sitosterol); this findi
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Not all of the biological activities exhibited by progestoge
2020-06-20

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the RAS2410 sale is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respon
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Little information is available regarding the expression of
2020-06-20

Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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Repulsive interactions towards undesirable substrates are ar
2020-06-20

Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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Metal ions are known not to be
2020-06-20

Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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br Rationale and hypothesis To discover an allosteric inhibi
2020-06-20

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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Because of the important role of the DDB CUL
2020-06-20

Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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Of the acidic hydroxyazoles involved
2020-06-20

Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Previous synthetic lethal screening efforts Cox et
2020-06-20

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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Although PQQ has nutritional importance and pharmacological
2020-06-20

Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov
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Widely expressed mammalian adhesion receptors for fibrillar
2020-06-20

Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.
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In conclusion our data demonstrated that montelukast
2020-06-20

In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va
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br Conflicts of interest br Acknowledgments This research wa
2020-06-19

Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest
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The first transcription factor TF known to interact with
2020-06-19

The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone Tenovin-1 receptor of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed dev
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Acknowledgements This work was supported in
2020-06-19

Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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