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Haj Yahya et al applied
2020-09-21

Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur ru listings resu
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DNA damage represents a persistent threat to genomic stabili
2020-09-21

DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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Indeed the alkyl group is not
2020-09-21

Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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DDR upregulation in patients with kidney diseases such
2020-09-21

DDR1 upregulation in patients with kidney diseases such as lupus nephritis and Goodpasture\'s syndrome [8] as well as in animal models of kidney injury [7], [8], [18] suggests that DDR1 plays an important role in kidney disease. Studies in various mouse models of kidney injury indicate that DDR1 del
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br Acknowledgements This work was supported by
2020-09-21

Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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The use of inhibitors clearly has its caveats
2020-09-19

The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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Dryocrassin ABBA The detection of galactomannan GM a polysac
2020-09-19

The detection of galactomannan (GM), a polysaccharide that is released during Aspergillus growth, is a useful and reliable non-invasive diagnostic test for screening and management of aspergillosis and is often more sensitive than culture (Schelenz et al., 2015, Fisher et al., 2013). The level of ga
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With regards to what might represent a typical baseline
2020-09-19

With regards to what might represent a typical “baseline” ChE (or AChE) activity in Saccostrea sp., it glucagon receptor should be remembered that the observed enzyme responses were obtained in laboratory exposures, over a narrow experimental window (96h), with specimens collected over the course o
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Nociceptive and hyperalgesic actions of ET are
2020-09-19

Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that
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Although further experiments are needed to determine definit
2020-09-19

Although further experiments are needed to determine definitively whether D–ETB receptor heterodimers exist, for example, by using fluorescence resonance rad51 transfer analysis or co-immunoprecipitation of receptors, the results of the study by Zeng and colleagues appear to indicate that D–ETB rec
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In summary we have identified
2020-09-19

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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ROS generation is crucial for NETs release
2020-09-19

ROS generation is crucial for NETs release upon both physiological or pathogenic stimuli [16,30]. In our study, we further verified this conclusion by demonstrating that SRA stimulation by Poly I enhanced intracellular ROS levels while scavenging of ROS by anti-oxidant agents effectively abolished t
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As proof of principle the effect of selective blockade
2020-09-19

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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In this review we present compelling
2020-09-18

In this review, we present compelling evidence in support of DHODH as an essential enzyme for the survival of cancer cells. DHODH, and its relationship to de novo pyrimidine metabolism, will be discussed along with factors that influence its regulation and expression. We will show evidence of DHODH\
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Studies of LRRK tagged with
2020-09-18

Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the LB42708 of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines its functio
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