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br Regulation of Glu transporters The pivotal role of
2021-11-04

Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino mu-opioid agonist 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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Acarbose and voglibose the classic glucosidase inhibitors
2021-11-04

Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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So far several methods have been used to
2021-11-04

So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute ampk inhibitors slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” experim
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In addition at the spinal level results
2021-11-04

In addition, at the spinal level, results from colocalization experiments demonstrate that GABA-C receptors are present in the substantia gelatinosa and that they are presynaptically located. Neurons located in the substantia gelatinosa are differentially activated by afferent noxious and non-noxiou
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br FPRs regulate anti microbial responses The classic
2021-11-04

FPRs regulate anti-microbial responses The classic evidence supporting FPR as an anti-microbial receptor is that bacteria are the major biological source of chemotactic formyl peptides, fMLF binds to FPR and fMLF activates chemotactic and anti-microbial responses in neutrophils 2., 3.. Recently,
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Thirteen multiparous German Holstein cows in their second to
2021-11-04

Thirteen multiparous German Holstein cows, in their second to fourth lactation, were selected from a previous study (Schäff et al., 2012) based on their individual peak in plasma BHB concentrations in wk 2 or 3 postpartum: high BHB (H-BHB; 1.05 to 2.57 mmol/L, mean 1.59 mmol/L; n = 8) and low BHB (L
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A pyrimidine class of compounds is of enormous interest
2021-11-04

A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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In addition to indoles two additional structural variants we
2021-11-04

In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic Protease Inhibitor Library sale side chain to prepare compound (). The extensi
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Syringin br Results br Discussion br STAR Methods br Acknowl
2021-11-04

Results Discussion STAR★Methods Acknowledgments The authors thank Drs. Michael Wegner, Ron Waclaw, and Ed Hurlock for critical comments. We thank Drs. Lihui Tsai and Jiang Wu for CHD8 and ASH2L-expressing vectors, respectively, Dr. Yueh-Chiang Hu for generating transgenic lines, and Jing
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Materials and methods br Results and discussion br Acknowled
2021-11-04

Materials and methods Results and discussion Acknowledgments This work was supported in part by the Japan Society for the Promotion of Science KAKENHI Grants JP21300174 and JP25282144 (H.K.). Introduction Epigenetic modifications of histones, such a lysine acetylation, play a key role in
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br Disclosures br Introduction The brown planthopper Nilapar
2021-11-03

Disclosures Introduction The brown planthopper, Nilaparvata lugens (Stål) (Hemiptera: Delphacidae), is a classic insecticide-induced resurgent pest throughout Asian rice-growing regions (Chelliah and Heinrichs, 1980). The resurgence of N. lugens induced by commonly used chemical agents has bee
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We are pursuing a hit to lead medicinal
2021-11-03

We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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br Substrate Interactions Outside of the
2021-11-03

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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Barasertib br Recent insights into EAAT structure function a
2021-11-03

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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Finally it is possible that the increase
2021-11-03

Finally, it is possible that the increase in the number of EAAT-3-labelled cells in the DG at PD 60, when compared with the control and experimental animals at PD 14, is associated with natural changes in the number of neurons present during the postnatal development of the hippocampus (41, 42) and,
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