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To study systemic potential of the
2020-09-15

To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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As a support chitosan presents interesting
2020-09-15

As a support, chitosan presents interesting characteristics that reinforce its great potential for enzyme immobilization [18,19]. Firstly, it is produced from renewable natural sources in addition to being biodegradable and water insoluble [20,21]. Also, the main peculiarity in the chitosan structur
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br Conclusions Nanoparticles can be used
2020-09-15

Conclusions Nanoparticles can be used to modulate the catalytic activity of various industrially and clinically useful enzymes, as well as pH, temperature and storage stabilities, which will enable the process to occur more efficiently and less costly. The interaction between an enzyme and nanopa
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br Materials and Methods br Acknowledgements br Introduction
2020-09-15

Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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The best characterized APC C
2020-09-14

The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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br Chemistry A total of new
2020-09-14

Chemistry A total of 35 new ThDP analogs in the series of 7, 12, 15, and 19 were designed and synthesized (Scheme 1). The synthetic route is simple and convenient. In this synthetic route, 4-amino-2-methylpyrimidine-5-carbaldehyde 3 is a key intermediate for the synthesis of title compounds 7, 1
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Together the protein engineering approaches employed by Teyr
2020-09-14

Together, the protein engineering approaches employed by Teyra et al., (2019) demonstrate the effectiveness of affinity maturation for improving the affinity of UbVs, but this comes at a cost in terms of specificity. Indeed, the most effective UbV was the dimeric construct generated from UbVs isolat
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Consistent with a clear separation of biological
2020-09-14

Consistent with a clear separation of biological function between ARISC and BRISC in cells, mutations in BRCC36 and Abraxas are prevalent in cancer genomes whereas mutations in KIAA0157 are rare. A survey of the Catalogue of Somatic Mutations in Cancer (COSMIC) consortium, revealed that to date, 37
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Because stimulation and blockade of dopamine D receptor all
2020-09-14

Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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The kinase activity of DNA PKcs is
2020-09-14

The kinase activity of DNA-PKcs is essential for NHEJ, but the exact role of the enzymatic activity of DNA-PKcs plays in NHEJ is not fully understood [57]. In vitro, DNA-PKcs can phosphorylate each of the canonical NHEJ factors including Ku70/80 [58], [59], XRCC4 [60], [61], Chloramphenicol receptor
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br Mammalian DGKs current knowledge Despite our understandin
2020-09-14

Mammalian DGKs: current knowledge Despite our understanding of prokaryotic DGKs, our limited understanding of the structure of mammalian DGKs is a major gap in our knowledge. Importantly, major differences exist between prokaryotic and mammalian enzymes often revealing the fact that structural fe
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br Conclusions In Summary a
2020-09-14

Conclusions In Summary, a multilayer screening of xanthones of natural origin (Xanthone-NPs) was undertaken against Pf-DHFR. The Re-rank score of screened compounds was size normalized and interaction profile was generated using experimentally known inhibitors. Three compounds X5, X113A and X164B
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In this study using REMD
2020-09-14

In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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br Other Alterations in Triglyceride Metabolism in DGAT Defi
2020-09-14

Other Alterations in Triglyceride Metabolism in DGAT-Deficient Mice Consistent with the enzyme\'s ubiquitous expression pattern, DGAT deficiency also altered triglyceride metabolism in other tissues. For example, postpartum Dgat−/− female mice were unable to nurse their young owing to an absence
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Calcium dependence of CaM target interaction was analyzed us
2020-09-14

Calcium dependence of CaM/target interaction was analyzed using a titration matrix in which both Ca2+ and CaM concentrations were changed. This gave us access to different parameters characterizing the interaction and namely to the number of bound Ca2+ required for the interaction to occur. Our app
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