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Having taken a step back from
2023-11-08
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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Recent studies have indicated that V ATPase activity negativ
2023-11-08
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ perifosine have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah1Δ cells' a
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retinoic acid receptor The protective role of HMW HA in infl
2023-11-07
The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid
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A large number of studies have shown that oxidative
2023-11-07
A large number of studies have shown that oxidative stress is involved in the pathophysiological process of ventricular remodeling and is associated with left ventricular dysfunction (Hori and Nishida, 2009, Lord et al., 2010). The generation of reactive oxygen species (ROS) that exceeds anti-oxidat
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Consistent with the above prediction there are additional
2023-11-07
Consistent with the above prediction, there are additional reports in which HMGA proteins have been demonstrated to facilitate recruitment of chromatin remodeling complexes to gene regulatory regions containing positioned nucleosomes during the transcriptional activation process. One particularly il
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br Acknowledgments This work was supported by
2023-11-07
Acknowledgments This work was supported by Grant-in-aid for Scientific Research (S) (20229008) (to T.K.), Targeted Proteins Research Program (to T.K.), the Global COE Research Program (to T.K.) and Translational Systems Biology and Medicine Initiative (to T.K.) from the Ministry of Education, Cul
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Renal fibrosis is regarded as
2023-11-07
Renal fibrosis is regarded as the final common pathway for most forms of progressive renal disease, and mouse UUO is a widely accepted experimental model of renal injury leading to extreme fibrosis localized to the interstitial compartment. A-306989 attenuated the mRNA expression levels of several k
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Despite these efforts to prevent oxidative metabolic degrada
2023-11-07
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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The theoretical calculations of ADME parameters molecular we
2023-11-07
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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Macrophage polarization is linked to activation of the
2023-11-07
Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic Rose
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In humans the major LOs are subdivided by
2023-11-07
In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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In summary the role of HT and
2023-11-07
In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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NPPB The structural analysis of the ASK
2023-11-06
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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81 9 br Results br Discussion br Conclusions In summary
2023-11-06
Results Discussion Conclusions In summary, this study provides novel report of pericardial adipose aromatase expression – in both human and rodent. We show that aromatase expression is remarkably upregulated with aging (Fig. 1C), and that total aromatase 81 9 conversion capacity is signifi
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In the current study SA was assessed to
2023-11-06
In the current study, SA was assessed to confirm the safety of CS addition to erythrocytes SA as well as SA elicits antioxidant action. It has been reported that, ROS induced desialylation by depletion of SA content from cell surfaces (Pawluczyk et al., 2014, Harisa, 2015). Therefore, significant de
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