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Next we designed substituents of the position Edge to
2022-06-20
Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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BCCA occlusion followed by reperfusion injury significantly
2022-06-20
BCCA occlusion, followed by reperfusion injury, significantly increased the brain AT1 and AT2 receptor expression in mice. Reports have demonstrated elevation of AT1 receptor expression in the cerebral 4EGI-1 during ischemia [34,35]. The gene expression of brain AT2 receptor is increased in both in
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Introduction Adaptations in the metabolism
2022-06-20
Introduction Adaptations in the metabolism of cancers contribute to tumor survival and growth and present opportunities to develop novel therapeutic strategies (Kelloff et al., 2005, Som et al., 1980). In particular, glutamine metabolism plays such an important role in cancer growth that a phenomen
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In patients with type diabetes glucagon receptor antagonism
2022-06-18
In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be
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Discrepancies in the reported results and conclusions from
2022-06-18
Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately
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Galanin mediates its activity by binding to
2022-06-18
Galanin mediates its activity by binding to three G-protein coupled receptor subtypes (designated GAL1-GAL3). Since GAL3 mRNA is found mainly in regions of the mesolimbic dopamine system, such as the ventral tegmental area, dorsal raphe nucleus, LC, amygdala, hippocampus, thalamus, hypothalamus, NAc
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Serotonin hydroxytryptamine HT is a monoamine with dual func
2022-06-18
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the GS-4997 as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Condron, 201
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br Funding Our work in this field was supported by
2022-06-18
Funding Our work in this field was supported by CNRSLIA528, Agence Nationale de la Recherche 06-Neuro, Agence Nationale de la Recherche MNMP 2009. Introduction GABA and the GI motility The role of GABA in the modulation of GI motility is quite complex and not fully understood, since GABA-i
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We hypothesize that HBO increases GABA activity at
2022-06-18
We hypothesize that HBO2 increases GABA activity at the GABAA receptor via a nitric oxide dependent mechanism. Blotting for the phosphorylated β3 subunit of the GABAA receptor should theoretically be increased when there is more GABA activity at the receptor (McDonald et al., 1998). We expected that
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Following these discoveries the term ferroptosis
2022-06-18
Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de
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Sperm capacitation was negatively r p related
2022-06-18
Sperm capacitation was negatively (r = −0.68; p ive but not significant (r = 0.22). No significant relationship was observed between the expression levels of either CB1 receptor or FAAH and any of the sperm quality parameters studied. The scatter plot distribution of spermatozoa expression of CB1 an
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In an effort to more fully
2022-06-18
In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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br Introduction Regulation of transcription is
2022-06-18
Introduction Regulation of transcription is a critical event of the embryonic development and epigenetic mechanisms such as histone modifications and DNA methylation appear important in mediating temporal changes, and differences among cells/tissues, of temporary stabilized transcriptomes (Mas et
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br STAR Methods br Author
2022-06-18
STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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In this study we also
2022-06-18
In this study, we also investigated the role of GST SBI-0206965 synthesis in relation to ASD. In univariable analyses, where the role of each GST gene (i.e., GSTM1, GSTT1, GSTP1) was individually assessed, we did not observe any significant associations between the GST genotypes and ASD. In contras
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