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Overall the evidence and the results
2020-05-15
Overall, the evidence and the results from in vivo studies clearly indicate that cyclosporine biotransformation can be induced by dasatinib co-administration through induction of CYP3A expression. However, further studies are needed to explore the role of P-gp modulation in DDIs. Conclusion In v
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A set of small molecule
2020-05-15
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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CRF and urocortin produce marked effects on the cardiovascul
2020-05-15
CRF and urocortin 1 produce marked effects on the U-73122 when administered both i.v. or directly into the CNS (Parkes et al., 2001). Systemic i.v administration of CRF and urocortin 1 cause a marked and long-lasting reduction in mean arterial blood pressure in rats Briscoe et al., 2000, Lawrence et
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The mechanism by which these HIV PIs
2020-05-15
The mechanism by which these HIV-PIs impair skeletal muscle palmitate transport and oxidation has been partially elucidated. CD36 (also referred to as fatty 4-ap synthesis translocase; FAT) is a transmembrane protein involved in the transport of long-chain fatty acids (LCFA) across cellular membran
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4 aminopyridine In order to further evaluate cpt a function
2020-05-15
In order to further evaluate cpt1a function, we determined its tissue distribution in large yellow croaker. The mRNA levels of cpt1a were detected in all the tested tissues, but at varying levels. cpt1a mRNA expression was the highest in liver among different tissues, similar to reports in other fis
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br Next let s recall some definitions and
2020-05-15
Next, let\'s recall some definitions and notations from [14] which are necessary to obtain the proof of Theorem 1. Let denote the CMV matrix whose Verblunsky coefficients replaced by , that is The corresponding extended CMV matrix is Recall the definition of in the proof of Theorem 2, replace
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Accumulated evidence indicates that apelin plays a protectiv
2020-05-15
Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 Berberine syn
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Otherwise ES cells express high level of
2020-05-15
Otherwise, ES trabectedin express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under the condition of
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The potential off target activity of against other ATP
2020-05-14
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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Targeting both PARP and DHODH for anti cancer
2020-05-14
Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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Compound was advanced to a chronic efficacy study in db
2020-05-14
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Glycyrrhizic acid 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured
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br Methods br Results br Discussion MEN is a potent
2020-05-14
Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3
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Fatty acid oxidation plays a crucial role in maintaining bod
2020-05-14
Fatty mct inhibitor β-oxidation plays a crucial role in maintaining body energy homoeostasis mainly during catabolic states. It mainly occurs in mitochondria and involves a cyclical series of reactions that result in the shortening of fatty acids. Fatty acids comprise an efficient source of energy
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br Methods br Results br Discussion On the other hand
2020-05-14
Methods Results Discussion On the other hand, surgical patients have to some extent stress during pre- and/or post-operative period. It is well known that CRF/CRF1 receptor is involved in the activation of HPA during acute and chronic stress (Papadimitriou and Priftis, 2009, Zelena et al.,
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br Acknowledgements br The oxygenation level has an impact
2020-05-14
Acknowledgements The oxygenation level has an impact on various aspects of skin physiology, but mechanisms of these effects, including the role of hypoxia in epidermal differentiation, are still poorly understood. The main components of the hypoxia pathway are short-lived transcription factor H
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