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Finally our work showed that HAART resulted
2021-11-15
Finally, our work showed that HAART resulted in significant inter-individual variability among DEGs, which reflected the Nifedipine in HIV-affected human gene expressions (Fig. 1, Fig. 2, Fig. 3, Fig. 4). These observations also highlighted the importance of determining common as well as personal s
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Our synthetic approach to GPR antagonists was designed
2021-11-15
Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic Tioconazole to 4-piperidone by first forming t
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br Competing interests br Introduction An
2021-11-15
Competing interests Introduction An effective vaccine against the Human immunodeficiency virus (HIV) is still to be created, even though many strategies have already been tried [1]. Antibodies against a vaccine antigen must be either neutralizing or inducing cellular cytotoxicity [1]. It is kn
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LbGlcK and the HsHxKIV d glucose complex PDB entry IDH
2021-11-15
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key GMX1778 binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK, such as K169 an
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The mechanism underlying the anorectic effect of OXM is
2021-11-15
The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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Despite a robust impact on learned social feeding behaviors
2021-11-15
Despite a robust impact on learned, social feeding behaviors, we observed no differences in body weight or food intake when the control or vHP GHSR-1A KD animals were maintained on either a normal chow diet or a Western diet high in fat and sugar. This is interesting in light of our previous work sh
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Activation of FXR or TGR inhibits inflammatory response via
2021-11-15
Activation of FXR or TGR5 inhibits inflammatory response via repressing NF-κB activity [1]. FXR is not expressed or expressed at a very low level in macrophages [45] (data not shown), but highly expressed in hepatocytes. In contrast, TGR5 is expressed in macrophages but not in hepatocytes. Our data
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Dual H H receptor antagonists developed
2021-11-15
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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HO acted as an intracellular defender against oxidative stre
2021-11-15
HO-1 acted as an intracellular defender against oxidative stress-induced cell damage. To elucidate the effects of HO-1 in ropivacaine-induced cytotoxicity in neuronal cells, HO-1 activity was inhibited using a specific HO-1 inhibitor zinc protoporphyrin, ZnPP. Our results indicate that ZnPP treatmen
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Stability of DBS over the day
2021-11-15
Stability of DBS over the 60-day time points was encouraging, with a maximum of 0.1 log10 IU/mL degradation from the day 1 value (Supplementary Fig. 1 and Supplementary Table 3). Discussion This study evaluated the sensitivity and specificity of the Aptima HCV Dx assay for HCV RNA detection from
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Importantly each conformational state in the SRP SR dimer
2021-11-15
Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon
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After ischemia expression of transcription factors including
2021-11-12
After ischemia, expression of transcription factors, including products of immediate early genes, stress proteins and neurotrophic factors are also altered in CA1 neurons78, 79. These proteins are potential candidates for downregulating of GluR2 expression by reducing mRNA transcription or stability
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br SMO antagonists pitfalls and limitations The first Hh inh
2021-11-12
SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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Many natural flavonoids have been identified as influencing
2021-11-12
Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la
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We next investigated whether pharmaceutical inhibition of
2021-11-12
We next investigated whether pharmaceutical inhibition of the PI3K pathway was synergistic with FGFR inhibition using BKM120, a pan-PI3K inhibitor with modest antitumor activity in cancer patients, as a single agent. We found that RT112 (- translocation) and JMSU1 ( amplification) were not significa
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