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A considerable body of evidence
2022-01-13
A considerable body of evidence suggests that alcohols, volatile anesthetics and inhaled drugs of abuse act at discrete sites on glycine and GABAA receptors, specifically within circumscribed protein pockets (Mascia et al., 2000, Mihic et al., 1997, Beckstead et al., 2000). An amino Cell Cycle Compo
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The aims of the present study were to
2022-01-13
The aims of the present study were to further investigate the localisation of glycine and GABAA receptors on individual neurons and how closely these two receptor types were associated with each other by carrying out double immunofluorescent labelling and imaged using confocal laser scanning microsc
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The in vivo biological activity
2022-01-12
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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The GAL also modified HT
2022-01-12
The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B SB408124 (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragmen
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The present study demonstrates that SNAP exhibits a
2022-01-12
The present study demonstrates that SNAP 37889 exhibits a toxic effect to these specific cell types, which is independent of endogenous expression of GAL receptor subtypes and leads to apoptosis. This conclusion is based on our findings that, although HMCB, HL-60 and SH-SY5Y cell lines differ in GAL
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am 580 Sumoylation is involved in regulating protein protein
2022-01-12
Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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The current lack of effective
2022-01-12
The current lack of effective treatments for primary or metastatic UM leaves a large therapeutic gap for patients and clinicians underscoring an urgent need for the identification of additional pharmacological targets for therapeutic intervention. As YAP-targeting strategies have remained elusive th
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Among the HER mutations reported in this study the JMD
2022-01-12
Among the HER2 mutations reported in this study, the JMD mutant R678Q is the third most recurrent HER2 mutation. Basic residues (such as arginine) play an important role in anchoring TMD helices of single transmembrane proteins to the bilayer (Gleason et al., 2013, Hristova and Wimley, 2011, Kim et
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In the course of studies leading to the
2022-01-12
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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The Rab to Rab switch
2022-01-12
The Rab5 to Rab7 switch on endosomes co-occurs with the release of the Rab5 GEF Rabex5 from endosomes, which prevents further Rab5 activation [5]. In addition, the Rab5 GAP is recruited to inactivate remaining Rab5 [67]. Recent data suggest that another GAP, TBC1D5, which binds the retromer complex,
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Sal 003 br Conclusion GST expression was detected in
2022-01-12
Conclusion GST expression was detected in the Hemicornea construct and the commonly used animal cornea models at both the protein and functional levels. The results are summarized in Table 1. However, the construct exhibited lower levels of activity of GST, a marker of phase II enzymatic activity
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br Introduction The replacement of a regular
2022-01-12
Introduction The replacement of a regular intake of healthy oils and fibres for a diet based substantially on high fat- and high sugar-content foods has had profound consequences for public health. These changes in the way that the populations of high income, particularly Western countries, manag
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It has been found that WHI P a JAK
2022-01-12
It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T Metabolism Compound Library australia (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proap
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Autophagy as an important cellular
2022-01-12
Autophagy as an important cellular process has drawn attentions to its role in cardiovascular systems [16]. Autophagy is a self-digestion and degradation process that recycles the contents of the cytosol, including macromolecules and cellular organelles, resulting in self-repair and conservation for
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diacerein mg Although glycine receptors predominate in the b
2022-01-11
Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including
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