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In conclusion we have discovered two new derivatives and tha
2021-04-29
In conclusion, we have discovered two new derivatives ( and ) that are potent inhibitors of DHODH. H and C NMR spectroscopic data revealed that these compounds undergo ready isomerisation at room temperature in -DMSO, but the docking studies indicate that there is neither conformation nor configurat
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br Introduction Noncanonical nucleoside triphosphates NTPs s
2021-04-29
Introduction Noncanonical nucleoside triphosphates (NTPs; such as deoxyinosine triphosphate (dITP), deoxyxanthosine triphosphate (dXTP), 8-oxo-deoxyguanosine triphosphate, and 2-oxo-deoxyadenosine triphosphate are produced from oxidation, deamination, or other modifications of canonical nucleotid
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Atg cleaves Atg at the peptide
2021-04-29
Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated At
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We have previously disclosed the
2021-04-29
We have previously disclosed the discovery of a 7-azaindole-3-acetic Entinostat CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work,
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In the cytoplasm the ternary CRM cargo RanGTP complex
2021-04-29
In the cytoplasm, the ternary CRM1–cargo–RanGTP complex is disassembled by the action of Ran-binding proteins RanBP1/2 and RanGAP. A recent kinetic study showed that the Ran-binding domains (RanBDs) of the cytoplasmic proteins RanBP1 and RanBP2, but not RanGAP, accelerate dissociation of NES from CR
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Previous studies from our laboratory in CD
2021-04-29
Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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br Author contribution br Acknowledgements QNRF grant number
2021-04-29
Author contribution Acknowledgements QNRF grant number NPRP6-065-3-012, Qatar National Research Fund, Doha Qatar for funding this work with grant number NPRP No.: NPRP6-065-3-012. Introduction Preeclampsia (PE) affects 3–5 % of pregnancies worldwide and is one of the leading causes of mate
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In humans the ER is encoded by the gene
2021-04-28
In humans, the ERα is encoded by the gene ESR1, located on chromosome 6, locus 6q25.1 (Gosden, Middleton, & Rout, 1986). In addition to the full-length ERα isoform (66kDa), several shorter isoforms (36kDa, 46kDa) have been identified as a result of the presence of alternate start codons, or as produ
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br Materials and methods br Results br
2021-04-28
Materials and methods Results Discussion This study demonstrates that various progestogens combined with E2 had different effects on breast cell growth. These effects had an inverse correlation with the changes of the PRA/PRB ratio. E2's antiapoptotic effects on MCF-7 α-Bungarotoxin may be
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br Role of ERK signaling in preventive and therapeutic poten
2021-04-28
Role of ERK signaling in preventive and therapeutic potential of flavonoids in neurodegenerative diseases ERK is one of the main pharmacological targets of natural phenolic compounds and contributes to several therapeutic approaches including anti-atherogenic, anti-cancer, anti-colitis, anti-arth
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We continued to investigate the
2021-04-28
We continued to investigate the contribution of the EP1 Erteberel to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed maximum sen
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The aim of this paper is
2021-04-28
The aim of this paper is to study the long-term socioeconomic impacts of local heat entrepreneurship from 2000 to 2016. The analysis focuses on impacts of the biomass-based district heat production on employment and income in a small peripheral community, called Eno, located in North Karelia, Finlan
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br Results and discussion The effects of hypoxia a combinati
2021-04-28
Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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In a larger study of patients
2021-04-28
In a larger study of 22 patients with nondiabetic proteinuric chronic kidney disease, BQ-123 produced significant natriuresis, resulting from increased renal blood flow. In addition, ETA antagonism reduced blood pressure and proteinuria, and, a new finding, decreased arterial stiffness. However, in
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The molecular mechanisms regulating the differentiation of
2021-04-28
The molecular mechanisms regulating the differentiation of Th1 versus Tfh lorlatinib from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cells to express
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