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Potential break through technology poised to overcome
2020-07-10
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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The instructive precedent for galectin phosphorylation is hu
2020-07-09
The instructive precedent for galectin phosphorylation is human galectin-3 (hGal-3). Its serine modification by protein kinase CK1 in the N-terminal tail is relevant for nuclear export during the course of apoptosis regulation and contact formation with the neural cell adhesion molecule L1 , , , . T
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For most enolases fluoride acts as
2020-07-09
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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The majority of APC C subunits form a giant
2020-07-09
The majority of APC/C subunits form a giant scaffold, which was originally named the arc lamp, based on its shape when viewing APC/C from one side (Figure 1 and Box 1) [24]. The scaffold consists of two modules: the TPR lobe resembles the curved post and lamp, and the platform resembles the CP 31398
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br RING type E s and their
2020-07-09
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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The potential off target activity of against
2020-07-09
The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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We initially identified four putative Egr binding sites and
2020-07-09
We initially identified four putative Egr1 Heparin sodium (−39/−36, −105/−102, −107/−104, and −227/−224) on the DBH proximal promoter. The deletion and mutagenesis experiments indicate that the motif at −227/−224 is required for Egr1-elicited reduction in DBH promoter activity. It remains to be det
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br Conflict of Interest br Acknowledgements Marques
2020-07-09
Conflict of Interest Acknowledgements Marques F. was supported by the Foundation for Science and Technology (FCT), Portugal, Grant UMINHO/BI/35/2012. This work was supported by FCT by the Project PTDC/AGR-AAM/70418/2006. Introduction β-methylamino-l-alanine (BMAA) exposure has long been as
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As for antiviral activity eight out of synthesized
2020-07-09
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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br Four active site residues of
2020-07-09
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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L-Kynurenine br Authors contributions br Acknowledgements br
2020-07-09
Authors’ contributions Acknowledgements Introduction Retinoic L-Kynurenine is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation of
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Recently Schenck et al identified an active
2020-07-09
Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat
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Multiple protein species are known to naturally exist for
2020-07-09
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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In vitro study indicated the cell death of hippocampal
2020-07-09
In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i
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br Materials and methods br
2020-07-09
Materials and methods Results Discussion Our study assessed the cytokine and chemokine changes associated with first onset PP as compared to HP and HNP groups. In the monocytes/ macrophages/ dendritic biotin-LC-LC-tyramide panel, IL-6 levels were found to be significantly elevated in both
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