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Unfortunately the approved drugs suffer from failure in many
2022-03-18
Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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Acknowledgements We appreciated the contributions of
2022-03-18
Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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br Rho family GTPases are molecular switches most
2022-03-18
Rho-family GTPases are molecular switches; most which cycle from an ‘on’ GTP bound state to an ‘off’ GDP bound state, driven by GEFs (guanine nucleotide exchange factors) and GAPs (GTPase-activating proteins) respectively. Association with lipid membranes through a lipid (farnesyl or geranylgerany
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The absolute requirement for substrate prephosphorylation ra
2022-03-18
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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br Next we explored the SAR around the aryl ring
2022-03-18
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 Bicalutamide sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo di
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Limited efforts were made to exploit the naturally occurring
2022-03-18
Limited efforts were made to exploit the naturally-occurring antigen-specific Treg for ex vivo expansion. This study sets up a reproducible protocol for the expansion of insulin-specific Treg isolated from NOD mice. These BMS 777607 exhibited higher suppressive capacity compared to the polyclonal T
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Rapid action of E on GnRH neurons has been
2022-03-18
Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor
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Compared to previously reported atypical
2022-03-18
Compared to previously reported atypical N-glycosites that were identified based on the deamidation of asparagine residues after PNGase F treatment [106], [107], these two studies further validated the identified atypical motif glycosites by directly identifying their intact glycopeptides. Since the
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The effects of these steroids namely the decrease
2022-03-18
The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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Excessive extracellular glutamate may induce excitotoxic
2022-03-18
Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much
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Results indicated that superfusion of orexin alone
2022-03-18
Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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Tianeptine sodium synthesis The progression of HIV varies fr
2022-03-17
The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these
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Thus far it is reported that the
2022-03-17
Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7
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TASIN-1 australia Several studies have also shown that
2022-03-17
Several studies have also shown that HK2 may be an important downstream TASIN-1 australia of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with HK2 expression in primary colon cancer
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Our data indicate that curcumin reduced MDA and LOOH formati
2022-03-16
Our data indicate that curcumin reduced MDA and LOOH formation in plasma and kidney induced by gentamicin treatment. The results demonstrate the protective effect of this compound against oxidative damage to these membranes. Moreover, the ability of curcumin to reduce the formation of LOOH induced b
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