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A highly attenuated B pertussis
2023-04-11
A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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Synthesis pharmacological evaluation for the binding at hA
2023-04-11
Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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Subsequently Palvimaki et al corroborated
2023-04-11
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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br Conclusion br Conflicts of interest
2023-04-11
Conclusion Conflicts of interest Introduction RNA interference is a specific post-transcriptional gene silencing mechanism within a cell via the transfection of microRNAs (miRNA), exogenous small interfering RNAs (siRNA) or small hairpin RNAs (shRNA) [1–3]. Transfection of shRNA can be done
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In order to increase the oral bioavailability abiraterone is
2023-04-11
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral prostaglandin synthase of abiraterone acetate (156), it is recommended that this drug should be
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The take home message here is that although
2023-04-11
The take-home message here is that, although Aurora A phosphorylated on T288 is the activated isoform of Aurora A, measuring the level of phosphorylation of T288 does not reflect Aurora A kinase activity (Figure 5). What would be the most appropriate readout for an in vivo Aurora A kinase activity
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Di ethylhexyl phthalate DEHP is one of the most
2023-04-10
Di-(2-ethylhexyl) phthalate (DEHP) is one of the most widely used environmental chemicals in the production of polyvinyl chloride. After myd88 inhibitor into human body, DEHP can be converted to the metabolite mono-ethylhexyl phthalate (MEHP), which has higher toxicity than DEHP and can influence r
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br Impact of global AHR deficiency on diet induced obesity
2023-04-10
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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AHR mediated MMP upregulation has been
2023-04-10
AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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We have expressed the ECDs of the
2023-04-10
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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Introduction Myasthenia gravis MG is an autoimmune disorder
2023-04-10
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic KU14R receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG. Experim
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While there is structural information on the
2023-04-10
While there is structural information on the core of the amyloid fibril, less is known about oligomer structure. There is evidence that the C-terminal of Aβ may form beta barrels in some oligomer species (Tay et al., 2013, Do et al., 2016), or may exist as loosely aggregated strands in other oligome
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In summary our data have shown that
2023-04-10
In summary, our data have shown that one mechanism by which glucose may mediate monocyte–endothelial cell interaction in the retinal endothelial cells is via the 12/15-LO pathway Furthermore, our current and previously published data [20,22] indicate a differential role of endothelial 12/15-LO versu
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br We approached the definition of
2023-04-08
We approached the definition of AD with the distinction between a syndrome and a disease in mind. Some will argue that a specific syndrome, that is, a multidomain amnestic dementia (after other potential etiologies have been excluded), should define AD in living people. Our position, however, is t
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We next considered the effect of alkyl chain
2023-04-08
We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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