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Since its inception ADEPT approach has been widely
2021-01-22
Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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Sensory gating describes a filter mechanism
2021-01-22
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits tenofovir price to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Au
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Since the aggregation of neurotoxic forms of A plays a
2021-01-22
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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Data from immunohistochemical detection of
2021-01-22
Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the
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Results are expressed as mean
2021-01-22
Results are expressed as mean±s.e.m. Paired or unpaired Student's t test was used for comparisons between 2 groups and one-way ANOVA followed by Bonferroni's post-test for more groups. Statistical significance was assigned if p Results and discussion Variations in [Ca2+]i in cardiomyocytes loaded
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URMC-099 receptor Immunomodulation effects of certain oxyste
2021-01-22
Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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Modulating protein stability specifically inhibiting ubiquit
2021-01-22
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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E is encoded by the
2021-01-22
E1 is encoded by the largest and most conserved open-reading frame (ORF) of the PV genome. The protein ranges in size from 600 to 650 amino acids, depending on the PV type. Overall, the protein can be divided into three functional segments: an N-terminal regulatory region that is essential for optim
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To ascertain separation of the distinct enzymatic activities
2021-01-22
To ascertain separation of the distinct enzymatic activities found in this protein preparation following separation on the HAP column, a rigorous quantitative analysis was conducted on the nickel–agarose elution and HAP FT pools of protein. For these analyses, each pool of protein was dialyzed in th
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br Acknowledgements These studies were supported by a
2021-01-21
Acknowledgements These studies were supported by a research grant from the NIH (R01 AR065594) to C. Putterman. Introduction Macrophages integrate and adapt to their locally encountered cytokine and chemokine milieu. In tumors characterized by an unresolving inflammation, the tumor cell-killin
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In the present study we investigated the effect of morphine
2021-01-21
In the present study we investigated the effect of morphine withdrawal on G-protein coupling to opioid and ET receptors in neonatal rats. Morphine-induced G-protein activation was significantly higher in neonatal rats undergoing morphine withdrawal; suggesting enhanced coupling of the receptors to G
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Replacement of the saturated propoxy group in compound with
2021-01-21
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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The importance of EBI for
2021-01-21
The importance of EBI2 for B cell function was first suggested by the dramatic upregulation of this receptor in EBV-transformed B cells and further inferred from its regulation in activated and GC B cells (Birkenbach et al., 1993, Glynne et al., 2000, Shaffer et al., 2000). An involvement of EBI2 in
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br Multi subunit RINGs There are
2021-01-21
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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SIRT has deacetylated regulation on numerous nonhistone prot
2021-01-21
SIRT1 has deacetylated regulation on numerous nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016) to play a key role in protecting against cell stress. Therefore, the role of SIRT1 in fluorine-induced oxidative stress was explored. The results revea
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