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SPR was used to measure biomolecular
2019-10-18
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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br Conclusions and future perspectives It
2019-10-18
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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The authors then showed that Spt interacts directly with
2019-10-18
The authors then showed that Spt6 interacts directly with the PRC2 subunit Suz12. This interaction occurs in solution but not on chromatin, suggesting that Spt6 may prevent PRC2 recruitment by binding to Suz12. They then mapped the domains in both Spt6 and Suz12 that are involved in this interaction
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A major open question in the field of lipid
2019-10-18
A major open question in the field of lipid mediators is the molecular nature of the PLA2 enzyme involved in the release of DHA and related omega-3 fatty acids from phospholipids as a first committed step for the generation of SPMs. Although by analogy with AA it is often assumed that cPLA2α may ser
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br Introduction Hydrogen sulfide H S and nitric oxide NO
2019-10-18
Introduction Hydrogen sulfide (H2S) and nitric oxide (NO) are important gasotransmitters in the cardiovascular system and instrumental to the fine control of vascular tone [1] and cellular function [2]. NO is synthesized from l-arginine by calmodulin-dependent endothelial nitric oxide synthase (e
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We found that the postnatal absence of norepinephrine yields
2019-10-17
We found that the postnatal absence of norepinephrine yields differing effects depending on noradrenergic receptor type and 2750 region. The density of α1-AR, indicated by [3H]prazosin binding was similar between Dbh+/− and Dbh−/− mice except for a significant increase in hippocampus in Dbh−/− mice,
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In this study using REMD with the crystal environment
2019-10-17
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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The aniline R group was extensively explored
2019-10-17
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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br Cysteine proteases as molecular targets for trypanosomati
2019-10-17
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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flavin adenine dinucleotide Compounds and were outliers for
2019-10-17
Compounds and were outliers for this equation being the two most reactive compounds. The presence of outliers implies that other factors or specific mechanisms are involved in their chemical hydrolysis. Generally urea derivatives prove to be highly stable in aqueous solutions in vitro. Additional
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br Introduction The dopaminergic system and its projections
2019-10-17
Introduction The dopaminergic system and its projections including both the prefrontal PR-619 (PFC) and striatum are known as being crucial to synaptic plasticity, skill acquisition and higher order functions (e.g., working memory and cognitive control; Matsumoto et al., 2003). Variations in dop
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The applications of fungal enzymes in paper
2019-10-16
The applications of fungal enzymes in paper industry involve biobleaching of pulp, pulp de-inking, degradation of dissolved and suspended organic compounds in concentrated effluents of mills and enhanced fibrillation. Enzymes usage is encouraged in paper industry in order to reduce the use of chemic
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br Conflict of interest br Acknowledgments and funding
2019-10-16
Conflict of interest Acknowledgments and funding We thank Jaakko Matomäki, MSc, for the statistical analysis of the data. The study was supported by the Medical Research Council of the Academy of Finland, Decisions no. 250124 and 250114 (Centre of Excellence in Molecular Systems Immunology and
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br Results br Discussion In this paper we present
2019-10-16
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 UMI-77 via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhibitor
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Aldehyde dehydrogenase has been characterized as a cancer
2019-10-16
Aldehyde dehydrogenase has been characterized as a cancer stem cell marker, which plays a key role in various biological processes in tumor, including cell proliferation, invasiveness and chemoresistance. Recent data of Abourbih et al reported that ALDH1 expression did not correlate with primary tum
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