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Search sphere This sphere includes the
2023-07-27
Search sphere 1: This sphere includes the Ellipticine binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the channel pore of the two subun
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In conclusion we have produced
2023-07-27
In conclusion, we have produced some highly potent inhibitors of P450 in comparison to the standard yutopar KTZ. Also, due to the limited specificity of these compounds against lyase in comparison to the 17α-OHase component, these compounds would be expected to have a major impact on corticosteroid
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Receptor tyrosine kinase Axl is a member of
2023-07-27
Receptor tyrosine kinase Axl is a member of the TAM (Tyro3/Axl/Mer) family, and has reported been associated with a spectrum of human cancers [8]. Numerous studies have revealed that the oncogenic potential of Axl is attributed to the anti-apoptotic and proliferative signaling pathways triggered by
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Physiological total plasma LPA levels are normally less than
2023-07-27
Physiological total plasma LPA levels are normally less than 1μM in healthy subjects. LPA levels have been reported to be increased in malignant effusions or plasma in cancer patients [20]. In addition, increasing ATX activity detected in healthy pregnant women in the third trimester of pregnancy ex
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Having taken a step back from
2023-07-27
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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Thus phosphorylation of p was used to measure the
2023-07-27
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc 6-Chloromelatonin expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]
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br Author contribution br Acknowledgement br Introduction Si
2023-07-27
Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of
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br Conclusions br Funding This work
2023-07-27
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in
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br Introduction Sustained over activation of neurohormonal s
2023-07-27
Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin Solithromycin system (RAAS) constitute cornerstones of pharmacotherapy for H
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In receptor binding terminology both receptor and acceptor c
2023-07-27
In receptor binding terminology, both receptor and acceptor contain a receptive site for the ligand, although only the receptor induces a biological function. Moreover, the acceptor lacks an endogenous ligand. Many proteins have been described as receptors for toxic Aβ assemblies, implying a designe
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Here we provide evidence that NO contributes
2023-07-27
Here, we provide evidence that NO contributes to changes in synaptic strength, but also offer an explanation as to why previous attempts to link NO to LTP have often failed. Our results describe a model by which cycling AMPARs, held in intracellular pools, are rapidly delivered to the membrane surfa
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br Concluding Remarks and Future
2023-07-27
Concluding Remarks and Future Perspectives While postmortem human TCS 2002 material is relatively sparse and has inherent limitations as discussed above, additional investigations could benefit from analysis of in vitro cellular models to corroborate findings in patient material. Generation of ne
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idarubicin In summary we identified a
2023-07-27
In summary, we identified a novel MLPH-ALK fusion in AST with discordant results of ALK IHC. In order not to overlook ALK-rearranged AST with rare fusion partners on IHC screening, a sensitive IHC method is preferable. Introduction Lung cancer remains the leading cause of cancer related deaths w
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Ambient levels of ppm ozone were recorded
2023-07-27
Ambient levels of 0.2ppm ozone were recorded during a recent 2017 weather event in Texas, United States (EPA, 2007). This concentration or higher levels have been used in several human clinical studies during intermittent exercise (Miller et al., 2016c). Although ozone concentration of 0.8ppm used i
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br Methods br Results br Discussion Adiponectin is naturally
2023-07-27
Methods Results Discussion Adiponectin is naturally expressed and secreted exclusively from adipocytes, and adiponectin levels and its isoforms in circulation have recently been reported to highly associate with human coronary artery disease (CAD) [46], [47], [48], [49], these studies clear
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