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Tacrine amino tetrahydroacridine I Fig was
2019-08-05
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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Recent data obtained with etifoxine
2019-08-02
Recent data obtained with etifoxine suggest that facilitation of GABAergic inhibition may be also associated with an indirect mechanism implying activation of the peripheral benzodiazepine receptor with a subsequent increase in neurosteroid production (Schlichter et al., 2000, Verleye et al., 2005).
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Oleandrin where The present study has shown that additional
2019-08-02
The present study has shown that additional protein stability can be achieved (Fig. 6). The 0.6 to 1.0 °C increases that were observed were not large compared, for example, to the ∼5 °C increase that has been reported using sequence modifications [22]. This may reflect that the Hyp enters both the X
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Nociceptive and hyperalgesic actions of ET
2019-08-02
Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that
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Prenylation may turn a flavonoid from an
2019-08-02
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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br Results br Discussion Adaptive drug resistance
2019-08-02
Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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br Acknowledgements We thank Joseph Granger and
2019-08-02
Acknowledgements We thank Joseph Granger and Bryan Neumann for careful reading of this manuscript. This work is supported by NIH grants AG37609 and HL 60306 to TYC and CCYC. Introduction Eleven million tonnes of waste are produced yearly by the European pulp and paper industry (Monte et al.,
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Given its high frequency it is not surprising
2019-08-02
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant Dequalinium Chloride to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have
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Methylation of histone tails is important in regulating chro
2019-08-02
Methylation of histone tails is important in regulating Golgicide A structure and transcription. Methylation occurs at arginine and at mono-, di- or tri-methylated lysine residues. The reversibility of histone methylation was recently revealed by the identification of two histone demethylases, LSD1
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DGK is also involved in cell differentiation Previously
2019-08-02
DGKδ is also involved in cell differentiation. Previously, to investigate the physiological roles of DGKδ, DGKδ-deficient mice have been generated. On the basis of the analysis of DGKδ-deficient mice, Crotty et al. reported that DGKδ regulates the epidermal growth factor receptor (EGFR) pathway by a
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br Materials and methods br Results br Discussion
2019-08-02
Materials and methods Results Discussion Our previous investigation demonstrated that some genes in the latex that were involved in rubber biosynthesis were regulated by exogenous JA, and Hbvp1 is one of the JA-responsive genes in the latex of rubber trees [23]. In this study, the Hbvp1 enc
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In the PTEN loss mouse
2019-08-02
In the PTEN loss mouse model, deletion of ATG7 gene not only caused an autophagy-deficient phenotype, but also postponed the progression of inoculated prostate tumor [22]. On the basis of these experimental facts, these ATG7 and PTEN related genes were then compared with the 3020 BCR-associated gene
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Betamethasone br Lymphoplasmacytic lymphoma Waldenstrom macr
2019-08-01
Lymphoplasmacytic lymphoma/Waldenstrom macroglobulinemia Lymphoplasmacytic lymphoma (LPL) and its subgroup Waldenstrom macroglobulinemia (WM) are rare and indolent lymphomas that arise from fully differentiated B cells. The only family of GPCRs that has been well studied in LPL/WM is the chemokin
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Here we were able to show for
2019-08-01
Here, we were able to show for the first time that stimulation of VSMCs with two different growth factors resulted in a dramatic decrease in gp130mRNA expression occurring four to six hours after stimulation with Ang II and PDGF-BB. The mRNA level remained extremely low within 12 hours after stimula
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br The modulation of ER from
2019-08-01
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective Gemcitabine solubility receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high aff
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