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The ER is responsible for calcium
2021-09-16
The ER is responsible for calcium storage, lipid and protein biosynthesis, and the folding, assembly, and maturation of proteins [23], and ER stress is one of the main causes in T2DM, which leads to β-cell apoptosis and dysfunction [[5], [6], [7]]. In this study, TG was used as an ER stress inducer.
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GnRH ant have been designed to obtain
2021-09-16
GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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It is known that hypercapnia
2021-09-16
It is known that hypercapnia, as well as hypoxia, can result in a decrease in body temperature, but the mechanisms involved are not very well known (Barros and Branco, 1998; Saiki and Mortola, 1996). One neutrophil elastase inhibitor is that when there is an acute hypercapnic exposure, acidosis pla
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In vitro studies have shown that some
2021-09-16
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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The findings in this study may represent an
2021-09-16
The findings in this study may represent an example of a more general phenomenon, namely that the exquisite specificity of the G protein-coupled receptors that mediate the physiological actions of the SBI-0206965 receptor family hormones in mammals may have arisen relatively late in evolution. In n
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In order to facilitate the
2021-09-15
In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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Galanin mediates its activity by binding to three G
2021-09-15
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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In summary the SAR of a series
2021-09-15
In summary, the SAR of a series of phenylpropanoic acid-free fatty c16 receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust efficacy in
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With the identification of small
2021-09-15
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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FPR ligands comprise structurally very diverse classes of co
2021-09-15
FPR ligands comprise structurally very diverse Hyper Assembly of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones, pyrid
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b-raf inhibitors As concerns TRPV assays benzylic amides and
2021-09-15
As concerns TRPV1 assays, benzylic amides and benzylic reverse amides exhibited an overall superiority over their aryl counterparts and , and ureas and . A reversed trend was however observed with the 4-chlorostyryl and 4--butylphenyl moieties (compare compounds and ; , , and ; and ). The EC a
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In Arabidopsis GCN containing protein complexes are found to
2021-09-15
In Arabidopsis, GCN5-containing protein complexes are found to be involved in cell differentiation, leaf and floral organogenesis [[8], [9], [10]]. AtHAC1 has involvement with root elongation, flowering, fertility and de novo shoot regeneration [11,12]. AtHAM1 and AtHAM2 control flowering time by ep
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br Experimental br Results and discussion
2021-09-15
Experimental Results and discussion First of all we had to choose suitable electrolyte´s system. We utilized advantageously the composition of the background electrolyte for biogenic amines separation published in our work [13] to which we adapted the leading and terminating electrolytes. With
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To date several studies have suggested that serum HER
2021-09-15
To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i
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It should be noted that one of
2021-09-15
It should be noted that one of the two phenyl groups of 15 is found in the main western pocket and the second phenyl group occupies the western secondary pocket (Ser53, Leu54, and Leu213). The nitrogen of the amide bond is involved in a hydrogen bonding interaction with Asp140. The alcoholic functio
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