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Currently much effort has been made
2019-07-31

Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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br Author Contributions br Acknowledgments br Introduction M
2019-07-31

Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.
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Previous studies from our lab
2019-07-31

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to iden
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br Four active site residues of
2019-07-31

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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Prednisolone It has been reported that CysLT receptors
2019-07-31

It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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Some of the psychoactive actions
2019-07-31

Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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Soon after the discovery of
2019-07-31

Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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Another clinical study indicated the daily consumption
2019-07-31

Another clinical study indicated the daily consumption of green tea with low concentrations of theanine and catechin would improve cognitive function (Ide et al., 2014). Further, in a double blind randomized clinical study involving 102 patients, the Hypericum extract was examined in terms of effica
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The pseudo DUBs KIAA and Abraxas are required for the
2019-07-31

The pseudo DUBs KIAA0157 and Abraxas are required for the catalytic function of BRCC36. Comparison of the BRCC36–KIAA0157 heterodimer structure with an inactive BRCC36 homodimer structure provides a model for understanding how this functional interplay is achieved. As shown in schematic form in Figu
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br Materials and methods br Results br Discussion
2019-07-31

Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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Apart from its high affinity
2019-07-30

Apart from its high affinity, the selection of GW2580 as 11-dUTP lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensive
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br Conclusion In this study we investigated
2019-07-30

Conclusion In this study, we investigated functional alterations of ECs following exposure to mechanical and/or physicochemical stimuli. Specifically, hypoxia induced phosphorylation with significant increases after 30 min and the maximum increase was after 180 min. Our data show that a combinati
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Studies have shown that endothelial cells damaged by
2019-07-30

Studies have shown that endothelial cells damaged by SAH can release a large amount of ET-1, thus its plasma level is elevated and is positively correlated with the symptoms of SAH (Lei et al., 2015, Masaoka et al., 1989). Our data obtained from SAH-along rabbits were consistent with these findings.
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The effect of ET activity on the development of
2019-07-30

The effect of ET-1 activity on the development of experimental pulmonary fibrosis has also been examined by other investigators. One study found that repeated administration of Bosentan, an ERA used to treat pulmonary arterial hypertension (PAH), significantly decreased bleomycin-induced pulmonary f
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Introduction Excessive exposure to ultraviolet
2019-07-30

Introduction Excessive exposure to ultraviolet (UV) irradiation from the sun injures human skin, which might lead to premature aging and skin pathologies [1], [2]. Chronic exposure to UV (especially ultraviolet-B, UVB) irradiation could profoundly affect the skin epidermis, interfering with the ker
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