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The aims of the present
2022-05-10

The aims of the present study were to further investigate the localisation of glycine and GABAA receptors on individual neurons and how closely these two receptor types were associated with each other by carrying out double immunofluorescent labelling and imaged using confocal laser scanning microsc
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br Recent insights into EAAT structure
2022-05-10

Recent insights into EAAT structure/function aspects The EAATs are secondary-active transporters coupling the movement of one Glu with the symport of three Na+ and one proton and the counter-transport of one K+ [3, 4]. The transporters are trimeric assemblies of protomers that function independen
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Glucose uptake a critical metabolic
2022-05-10

Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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The MeO CFO phen yl group was
2022-05-09

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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Despite potent biological actions the native hormone undergo
2022-05-09

Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene
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br Discussion RBCs possess a much simpler composition and st
2022-05-09

Discussion RBCs possess a much simpler composition and structure than other eukaryotic resazurin and can therefore serve as a convenient system on which to study how cell functioning relates to the molecular and supramolecular properties of its constituents. The model developed in this work is a
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Inhibitors of the G rdos effect include the
2022-05-09

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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Clobetasol propionate Retinal GAL receptor distribution sugg
2022-05-09

Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret
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Seizures in turn selectively modulate the expression of GalR
2022-05-09

Seizures, in turn, selectively modulate the hundreds of people of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could have
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The present in vitro experiments confirm
2022-05-09

The present in vitro experiments confirm previous suppositions (Ciosek, Gałecka, 2011, Izdebska, Ciosek, 2010) that Gal modulates AVP and OT release by acting at every level of the hypothalamo-neurohypophysial system. In fact, both 10−10 M and 10−8 M Gal diminished basal release of AVP and OT from t
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Since we were able to reach low micromolar to sub
2022-05-09

Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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The subcellular redistribution of some
2022-05-09

The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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3,3',5'-Triiodo-L-thyronine br Acknowledgement The a
2022-05-09

Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru
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Here we show that Jmjd a zebrafish
2022-05-09

Here, we show that Jmjd3, a zebrafish JmjC domain-containing protein, possesses H3K27 histone demethylase activity in vivo, and down-regulation of jmjd3 leads to significant reduction of primitive and definitive myelopoiesis. Importantly, we have demonstrated that jmjd3 directly upregulates spi1 exp
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br Acknowledgements br Introduction Pregnancy brings
2022-05-09

Acknowledgements Introduction Pregnancy brings forth significant metabolic reprogramming that induces a number of metabolic changes to ensure that the nutrient requirements of the mother and fetus are met [[1], [2], [3]]. These adaptations change radically over the period of pregnancy dependin
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