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TGR is a class A GPCR transducing signal through
2021-10-26
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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br Materials and methods br Results and
2021-10-26
Materials and methods Results and discussion We recently found that the GlyT1 N-terminal and C-terminal sequences could be modified by phophorylation, or partially lost under pathological conditions by calcium-dependent proteolysis (Baliova and Jursky, 2005, Baliova and Jursky, 2010). While re
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Introduction l Glutamate is a
2021-10-26
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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Azithromycin Dihydrate br Conclusion Discovery of an ideal o
2021-10-25
Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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Following the discovery of diketo compounds S and L as
2021-10-25
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent topotecan based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioas
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The measured ROcc values and
2021-10-25
The measured ROcc50 values (4.8 and 42 mg/kg, respectively) were lower than those estimated from the mouse free 4-IPP synthesis concentrations (0.4 and 9.3 mg/kg for the sigma-1 and histamine H3 receptor, respectively) or rat CSF levels (0.65 and 4.5 mg/kg, respectively). This discrepancy is almost
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PLP has been found to be effective inhibitor of
2021-10-25
PLP has been found to be effective inhibitor of many enzymes that have T7 High Yield Fluorescein RNA for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 defic
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Additionally molecular imaging has great potential for nonin
2021-10-25
Additionally, molecular imaging has great potential for noninvasive and quantitative imaging of pancreatic β-cells, but each single imaging modality has its own intrinsic strengths and limitations. Functional imaging modalities have high sensitivity (such as SPECT and PET) and anatomical imaging tec
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In summary we have designed and optimized
2021-10-25
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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The DNA cleavage activity assay in the present study also
2021-10-25
The DNA cleavage activity assay in the present study also demonstrated the DNA glycosylase activities of SMUG1, NEIL1, TDG, and NTHL1 for 5OHU paired with A. While our findings on the activities of SMUG1 and NEIL1 were consistent with the results reported from previous studies [25], [50], the activi
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Post translational ubiquitination has been shown to
2021-10-25
Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra
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Ca independent release of L C glutamate and GABA
2021-10-25
Ca2+-independent release of L-[14C]glutamate and [3Н]GABA that occurs via transporters working in the reverse mode also insignificantly increased in vitamin D3 deficiency despite decreased GAT-3 and EAAC-1 DL-α-Hydroxyglutaric acid disodium salt and neurotransmitter uptake efficacy Fig. 3, Fig. 6 A
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A main finding of this study was that the impact
2021-10-25
A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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In this study we investigated the contribution of GCK G
2021-10-25
In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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br Acknowledgement We like to
2021-10-23
Acknowledgement We like to thank the Austrian Federal Ministry of Science, Research and Economy for financial support (GZ402.000/00014-WF/V/6/2016 within the Sino-Austria project) as well as Andrea Szabo and Patricia Haiss for support regarding the drawing of figures and tables. Farnesoid X Re
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