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The two competitive bivalent GlxI inhibitors polyBHG
2022-04-08
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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Previous studies have shown that zinc interacts with
2022-04-08
Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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PTMs have been shown to influence transporter kinetics
2022-04-08
PTMs have been shown to influence transporter kinetics, both directly and indirectly (Xu & You, 2017). They do not just regulate the innate structure-function relationship driven by a transporter's global architecture, but rather are also able to regulate this relationship down to the resolution of
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So far the functional significance of GluR A
2022-04-08
So far, the functional significance of GluR-A and GluR-B in synaptic plasticity has been best studied in the context of long-term potentiation of synaptic transmission in vitro in the hippocampus and the regulation of synaptic strength in paradigms underlying activity-dependent learning in vivo Taka
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br Results and discussion br Conclusion In conclusion
2022-04-08
Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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br Acknowledgements This research was
2022-04-08
Acknowledgements This research was funded by Ministry of Education Malaysia (MOE), and supported by the Department of Nutrition, Exercise & Sports, Department of Drug Design, University of Copenhagen, Denmark and Universiti Malaysia Pahang (UMP), Malaysia. HPLC equipment used for high-resolution
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fmoc-osu br Materials and methods br Results
2022-04-08
Materials and methods Results Discussion Our liver-specific Gck (−/−) mice and another line of liver-specific mice [13] exhibited impaired glucose tolerance. Furthermore, both knockout mice showed decreased hepatic glycogen content and reduced Pklr and Fas gene fmoc-osu in the liver [11].
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MRcKO mice showed a comparable degree
2022-04-08
MRcKO mice showed a comparable degree of cardiac remodeling compared to control (MRf/f) mice. Moreover, the worse cardiac remodeling in pressure-overloaded GRcKO mice is not due to compensatory activation of cardiomyocyte MR, because GRMRdcKO mice displayed cardiac remodeling to the same extent as G
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Olanzapine has been reported to attenuate insulin secretion
2022-04-08
Olanzapine has been reported to attenuate insulin secretion, cause insulin resistance (Chintoh et al., 2008) and reduce whole body carbohydrate oxidation (Klingerman et al., 2014). However, a blunting of these effects in Gcgr−/− mice would not appear to explain the protection against olanzapine-indu
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br Author contributions br Transparency document br Acknowle
2022-04-07
Author contributions Transparency document Acknowledgments The financial contributions of the Marie-Curie Action: BIOCONTROL, contract number MCRTN – 33439, the Agence Nationale de la Recherche (projects membraneDNP 12-BSV5-0012, MemPepSyn 14-CE34-0001-01, InMembrane 15-CE11-0017-01 and the
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Fibroblast growth factor receptors FGFRs play an essential r
2022-04-07
Fibroblast growth factor receptors (FGFRs) play an essential role in the regulation of cell survival, proliferation, migration and differentiation. FGFRs are a family of receptor tyrosine kinases (RTKs) exhibiting an extracellular immunoglobulin (Ig)-like ligand binding domain, a transmembrane domai
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The results of our analysis of Fas alleles Fas A
2022-04-07
The results of our analysis of Fas alleles, Fas 670 A>G, FasL alleles, and FasL IVS2nt 124 A>G for cases and controls are shown in Table 2. For Fas 670, we found statistically significant differences between the two groups regarding the AA Tioconazole (P=0.040) and GG/AG (P=0.040) as well as the A
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Our results on the other hand shows that there is
2022-04-07
Our results, on the other hand, shows that there is no upregulation of ETBR on the spinal cord after SCI, but there is a significant difference of mRNA on days 2, 7 and 28 on the SCI group on the spinal cord and no changes on the DRG, suggesting that the spinal cord injury may reduce the renovation
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Some SNPs have been identified for HRH
2022-04-07
Some SNPs have been identified for HRH in cancer (Table 4). Looking into breast cancer research, H4 receptor polymorphisms have been recently associated with the malignancy of the disease. This was evidenced upon the analysis of genotypes and haplotypes of a Chinese Han population; this study showed
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TCS PIM-1 1 The histamine H receptor H
2022-04-07
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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