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The GABA A receptors containing the
2022-07-27

The GABA-A receptors containing the δ subunit are crucial for the mediation of non-synaptic inhibition in the dentate gyrus; thus, the decreased expression of the δ subunit may suggest a decrease in the inhibitory tone and an increase in the neuronal excitability. Moreover, the GABA-A receptors cont
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At present many methods have been applied for
2022-07-27

At present, many methods have been applied for multiple detection. For example, BOP reagent [[9], [10], [11]] is frequently used to detect multiple targets because of its exquisite sensitivity and specificity, but it is difficult to design experiments to test short-length oligonucleotides. Electroc
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br Acknowledgement We like to thank
2022-07-27

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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Tetrazole is one of the most
2022-07-27

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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So what makes a FFAR agonist different
2022-07-27

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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Results of studies on fish FBPase are
2022-07-27

Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv
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8-Azido-ATP The Rho family of GTPases is composed of many sm
2022-07-26

The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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(S)-AMPA The ETB receptor has been shown
2022-07-26

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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WZ811 All these recent results show the interconnection
2022-07-26

All these recent results show the interconnection between the Hippo pathway as a tumor-suppressor on the one hand and its function as regulator of metabolic homeostasis on the other. Disruption of the Hippo pathway leads to cancer growth, which is often associated with pathological disturbances in t
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In contrast to RhoA Rac and Rap which are
2022-07-26

In contrast to RhoA, Rac1 and Rap1 which are stimulated by platelet activators and inhibited by NO/PKG, the GTPase ADP-ribosylation factor 6 (Arf6) is regulated in the reverse way. Platelet agonists like thrombin, collagen, or ADP, reduce Arf6-GTP levels, whereas NO and PGI2 oppose this reduction [1
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Considering its role in regulating
2022-07-26

Considering its role in regulating cytoskeletal dynamics, the Rho kinase effector ROCK has been particularly implicated in tumor metastasis. The ROCK inhibitors Y27632 and fasudil have been extensively studied in cancer and beneficial effects have been observed in many types of cancers (Kale et al.,
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In the H NMR spectrum
2022-07-26

In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be
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Finally our data found that the
2022-07-26

Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist
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Compound was synthesized in a racemic fashion
2022-07-26

Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (
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To investigate if such an effect is observed in native
2022-07-26

To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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