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br Application of TIRFM to visualizing
2022-04-19
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin protease inhibitors hiv (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of
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AGK7 br Discussion Considering cardiovascular risk factors t
2022-04-19
Discussion Considering cardiovascular risk factors, there was a significant difference in prevalence of dyslipidemia in both groups, 57.5% in HIV-infected stroke patients compared to 8.9% in the HIV-uninfected patients. These results are similar to that of Chow et al. who found a dyslipidemia pre
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br Introduction Histamine stored in mast cells and basophils
2022-04-19
Introduction Histamine stored in mast cells and basophils has been recognized as one of the most critical mediators in allergic reactions and plays an important role in eliciting the nasal symptoms of allergic rhinitis, such as sneezing, nasal itch, pain, rhinorrhea, and congestion [1], [2]. It i
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Studies have demonstrated the paradoxical role of HO
2022-04-19
Studies have demonstrated the paradoxical role of HO-1 in tumorigenesis. At initial stages of carcinogenesis, it protects DNA by lowering the ROS-mediated mutational rate, but later, HO-1 promotes cancer cell survival and proliferation. One PDAC therapeutic strategy is to increase ROS production and
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G protein coupled receptors GPCRs constitute a large family
2022-04-18
G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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Beside its role in NF
2022-04-18
Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr
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Several studies have found that GPR possesses a distinct
2022-04-18
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Deferiprone expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (
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To apply the recently developed GPR
2022-04-18
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the baicalein australia and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this
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Starting from commercially available dioxaspiro
2022-04-18
Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an Oseltamivir phosphate catalyzed deprotection efficiently gave . A - enriched mixture of (
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As part of their ongoing
2022-04-18
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile RSVA 405 derivatives as TGR
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Previously we have shown that the natural flavonoid
2022-04-18
Previously, we have shown that the natural flavonoid compounds that possess C-4 ketone group and C-5 hydroxy group, such as baicalein, luteolin, myricetin and quercetin, effectively inhibit human GLO I. Considering our interest in inhibitors of GLO I and based on the rationale mentioned above, struc
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By contrast pentameric glycine receptors
2022-04-18
By contrast, pentameric glycine receptors (GlyR) in humans have four functional subunits, α1− α3 and β (Lynch, 2004) whereas the retina of other mammals have an additional α4 subunit (Harvey et al., 2000), and in humans the α4 subunit is considered a pseudogene as it lacks the 4th transmembrane doma
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br Conclusion In summary a series
2022-04-18
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Fluconazole motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing poten
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Although EAAT may not be involved in
2022-04-18
Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few
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Accordingly a bioassay guided approach was
2022-04-18
Accordingly, a bioassay-guided approach was been used to study the bioactive compounds in VAS contribute to the α-glucosidase inhibitory and antioxidant activity. The 95% ethanol extraction of VAS was successively partitioned with petroleum ether, ethyl acetate and n-butanol. Ethyl acetate fraction
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