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As proof of principle the effect of selective
2021-02-07
As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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The in vitro enantioselective metabolism of pesticides has b
2021-02-07
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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br Cytokines potent mediators of ILC function
2021-02-07
Cytokines – potent mediators of ILC function The different ILC players are portrayed in three categories, ILC1, ILC2 and ILC3, based on the cytokines they produce and transcription factors (TFs) that guide their differentiation [8] (Figure 1). Cytokines are the most extensively studied stimuli fo
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br Acknowledgments This work was supported by Grants from th
2021-02-07
Acknowledgments This work was supported by Grants from the National Research Foundation (2010-0000782) and the National Center for GM Crops (PJ008152) of the Next Generation BioGreen 21 Program funded by the Rural Development Administration, Republic of Korea, to W.T.K. Introduction Ubiquityl
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Intriguingly one E residue may serve as
2021-02-07
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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melanocortin receptor The nuclear receptor related protein N
2021-02-07
The nuclear receptor related-1 protein, Nurr1 (NR4A2), is a transcription factor that regulates the melanocortin receptor of genes critical for the development, maintenance, and survival of dopaminergic neurons (Alavian et al., 2014, Decressac et al., 2013, Dong et al., 2016, Jankovic et al., 2005,
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DNA methylation assay To test the biological activity of
2021-02-07
DNA methylation assay. To test the biological activity of purified A1S_0222, a methylation assay was performed using the Int1 DNA. As an alternative DNA substrate, Seq3 (located in gene A1S_0965 of A. baumannii ATCC 17978) was amplified from Acinetobacter baumannii 29D2 using the oligonucleotides Se
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The biological significance of DNA ligases is attributed to
2021-02-07
The biological significance of DNA ligases is attributed to their function in DNA replication, recombination and/or DNA repair [1], [2]. In vertebrates, three different DNA ligases I, III and IV are recognized. DNA ligase I is essential for the Okazaki fragments’ ligation during lagging-strand DNA s
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br Experimental methods br Results and
2021-02-07
Experimental methods Results and discussion Conclusion Rational design of highly selective fluorescent probes to detect G-quadruplexes is of profound importance for basic research. On this basis, we designed and synthesized a series of N-alkylated styrylquinolinium dyes Ls-1, Ls-2 and Ls-3.
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Some pyrimidine analogs are substrate based inhibitors that
2021-02-07
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHOD
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br Advantages of modified proteins over
2021-02-05
Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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The data correlations from Multiflash
2021-02-05
The data correlations from Multiflash™ [43] and DIPPR [44] were used for the liquid volume and heat of vaporization. For vapour pressure the curves were regressed from the experimental data present on both the DIPPR [44] and TRC [45] databases. As for liquid heat capacities both the latter databases
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CK enzymes belong to a
2021-02-05
CK1 enzymes belong to a conserved family of serine/threonine protein kinases that plays an important and diverse role in vesicular trafficking, DNA repair, Chlorpropamide progression and cytokinesis in organisms from yeast to humans [15]. In multicellular organisms CK1 enzymes also regulate develop
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br Effects of estradiol outside the
2021-02-05
Effects of estradiol outside the nucleus are often mediated by classical estrogen receptors Today, it is widely accepted that steroid hormones can signal in ways that do not rely on receptors acting in the nucleus, including activation of receptors localized to the cellular membrane. Rapid effect
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Hepatocyte proliferation is accompanied by changing
2021-02-05
Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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