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br Conclusion In conclusion we discovered a
2022-04-01
Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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With rare exceptions the biological role
2022-04-01
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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Further research should indeed focus
2022-04-01
Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t
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It is considered that activations of
2022-04-01
It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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br Author contributions statement P
2022-04-01
Author contributions statement P.N.Y. designed the study, analyzed the data and prepared the draft of the manuscript. C.S performed the experiments, analyzed the data and generated Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5, Fig. 6, Fig. 7, Fig. 8. A.K. and S.D. made Supplementary Figs. S1 and S2. D.
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It has been reported that the pathway upstream
2022-04-01
It has been reported that the pathway upstream of YAP phosphorylation is operative in a tissue or context-specific manner. LPA or S1P bound to their corresponding membrane GPCRs and act through Rho GTPases to activate YAP/TAZ [11]. Consistently, another report showed that activation of PAR1 (a GPCR)
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Magtanong et al observed that caspase
2022-04-01
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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br Characterization of quantal exocytosis
2022-04-01
Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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br Materials and methods br Results br Discussion Several
2022-03-31
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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Surface enhanced Raman spectroscopy SERS is one
2022-03-31
Surface-enhanced Raman spectroscopy (SERS) is one of the most powerful and ultra-sensitive analytical tools, which has been widely applied to food security analysis and many other fields (Craig, Franca, & Irudayaraj, 2013; Gukowsky, Xie, Gao, Qu, & He, 2018; Qi et al., 2013; Zhang et al., 2015). For
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In vitro studies suggest that the increase in
2022-03-31
In vitro studies suggest that the increase in Hx activity seen in normal pregnancy may contribute to the down-regulation of the vascular expression of Angiotensin II receptor 1 thereby promoting a relaxed and dilated maternal vascular bed [25]. It has further been suggested that the decreased Hx act
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br Regulation of HO expression under conditions of ischemic
2022-03-31
Regulation of HO-1 expression under conditions of ischemic cardiac damage Heart is a vital organ with high metabolic demand, rich in mitochondria and it is very vulnerable to oxidative damage [85]. Disruption in coronary blood flow following MI leads to hypoxia (a reduction in the amount of avail
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We observed that the Toc
2022-03-31
We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate
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Concerning the molecular mechanisms underlying transcription
2022-03-31
Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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br Next we explored the SAR around the aryl ring
2022-03-31
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic Cholesterol sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did not
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