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br G protein coupled receptor GPR also known
2022-04-01

G-protein coupled receptor 40 (GPR40), also known as a free fatty dpni receptor receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR40 agonis
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The physicochemical properties of the prodrugs provided impo
2022-04-01

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-al
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As for all DOACs measurement
2022-04-01

As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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Syt itself does not catalyze
2022-04-01

Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisel
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br Experimental br Results and discussion First
2022-03-31

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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Considering that TGF plays a pivotal
2022-03-31

Considering that TGF-β1 plays a pivotal role in inflammation, renal fibrosis, cell growth, differentiation, and apoptosis, it has been viewed as a vital mediator in kidney disease [49,50]. Studies have demonstrated that TGF-β1 is upregulated in both human and experimental kidney diseases [51,52]. TG
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Electrostatic potential along with measurement
2022-03-31

Electrostatic potential along with measurement and modeling of corresponding energies is vital for inferring protein properties, lone or complexed with ligands. DelPhi was used for solving Poisson Boltzmann equation, obtaining grid, total reaction and coulombic energies after solvating the proteins
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R R MNF is a unique bitopic agent
2022-03-31

(R,R′)-MNF is a unique bitopic agent with selective and potent β2AR agonistic and GPR55 inhibitory properties [10], [11] that are independently associated with the drug's anti-mitotic and anti-tumorigenic actions. In 1321N1, U118MG, and melanoma cell lines, (R,R′)-MNF activation of the β2AR decrease
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We tested this hypothesis with two experiments In the
2022-03-31

We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 PF 4800567 hydrochloride (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemica
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In previous work we showed that benzophenanthridines
2022-03-31

In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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In this study we provide biochemical and immunohistochemical
2022-03-31

In this study we provide biochemical and immunohistochemical evidence for the localization of the glycine transporter GLYT1 in synaptic vesicles. Previously, it was thought that GLYT1 was exclusively a glial protein (Zafra et al., 1995a). However, due to a partial discrepancy between mRNA and protei
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br Regulation of Glu transporters The pivotal
2022-03-31

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Sulfo-NHS-Biotin calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tra
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br Experimental section br Acknowledgments MIN cells were ki
2022-03-31

Experimental section Acknowledgments MIN6 2 deoxyglucose were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H06574 to T.U
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br Materials and methods br Results
2022-03-31

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 CU CPT 22 synthesis in the li
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br Conflict of interest br Acknowledgements br
2022-03-31

Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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