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Pharmacologic approaches of inhibiting GSNOR activity have
2022-03-12
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Canine HGF / Hepatocyte Growth Factor Protein The recently
2022-03-12
The recently de-orphaned G-protein coupled receptor (GPCR), GPR55, is activated endogenously by L-α-lysophosphatidylinositol (LPI), a lipid signaling molecule, as well as N-arachidonoyl glycine (NAGly) and numerous endo, phyto, and synthetic cannabinoids (Oka et al., 2007, Henstridge et al., 2010, H
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Molecular dynamics studies have proved an effective
2022-03-12
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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Due to the requirement of high end methods such as
2022-03-12
Due to the requirement of high-end methods such as total internal reflection fluorescence (TIRF) microscopy to visualize lipid rafts, isolation procedures are employed to study the protein content of lipid rafts [29]. The different methods utilized to isolated lipid rafts and other low density micro
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In an immunohistochemical analysis of gastric cancer samples
2022-03-12
In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial p-nitro-C
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Although NCT undergoes complex glycosylation processing for
2022-03-12
Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st
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The focused set of additional pyrazole analogs
2022-03-12
The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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In the course of our ongoing
2022-03-12
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric PF-01367338 type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the proc
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azd6244 Chemotherapeutic approaches to glioblastoma which
2022-03-12
Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this
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Macrophage populations are prominent in active IBD Strober a
2022-03-12
Macrophage populations are prominent in active IBD (Strober and James, 1986) as compared to healthy donors. Further, percentages of macrophages are increased in DSS-induced colitis (Grose et al., 2001, Ogawa et al., 2004). IBD is also linked to an influx of neutrophils and depletion of neutrophils b
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Materials and methods br Results and discussions
2022-03-11
Materials and methods Results and discussions Conclusions In this study, we identified 7 histone acetyltransferases and 12 histone deacetylases in Marchantia polymorpha. The present phylogenetic analysis of MpHATs and MpHDACs provide the insight into the evolutionary relationships of these tw
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Evidence indicates that astrocytes play a role in the
2022-03-11
Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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br Hydroxamic acids br Inhibitors
2022-03-11
Hydroxamic acids Inhibitors with reporting modalities Dual or more HDAC inhibitors Conclusion Finally, non-human HDAC such as Schistosoma mansoni HDAC8 are targeted for parasitic diseases and recent work highlight the interest of HDACs in viral infections. Despite their discovery in the
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Organisms can adapt to increasing ROS
2022-03-11
Organisms can adapt to increasing ROS production by up-regulating antioxidant defences, such as the activities of antioxidant enzymes (Livingstone, 2003). Failure of antioxidant defences to detoxify excess ROS production can lead to significant oxidative damage including enzyme inactivation, protein
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In an attempt to gain
2022-03-11
In an attempt to gain increased molecular insights into in vivo transmigration of neutrophils, we applied an aseptic inflammatory skin chamber model. In this model, recruitment of neutrophils is typically associated with phenotypic changes of many plasma membrane localized adhesion receptors in peri
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