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We started our investigation by evaluating the impact
2022-01-17

We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition
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Compared to previously reported atypical N glycosites that w
2022-01-17

Compared to previously reported atypical N-glycosites that were identified based on the deamidation of asparagine residues after PNGase F treatment [106], [107], these two studies further validated the identified atypical motif glycosites by directly identifying their intact glycopeptides. Since the
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Glial cells have emerged as important
2022-01-17

Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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Interestingly mGlu and mGlu receptors differ
2022-01-17

Interestingly, mGlu2 and mGlu3 receptors differ notably by their cellular distribution. Whereas mGlu2 receptors are mostly neuronal, mGlu3 receptors are expressed both in glia and in neurons. In neurons, mGlu3 receptors are present at the post-synapse and in presynaptic elements (Tamaru et al., 2001
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br Materials and Methods br Results br Discussion A model
2022-01-17

Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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Recent studies suggested that non coding RNAs participate
2022-01-17

Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 antifungal [38]. Theref
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br Acknowledgements This work was supported by a fellowship
2022-01-17

Acknowledgements This work was supported by a fellowship to C.H. under the ‘100 Foreign Expert’ scheme of the Shanxi province government(R100456). Conflict of interest: Dr. Holscher is a named inventor on a patent submitted by Lancaster University on the use of dual GLP-1/GIP analogues in neurode
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br Conclusions There are a number of factors that affect
2022-01-17

Conclusions There are a number of factors that affect the transit of solutes through gap junction channels. Fig. 4 provides a simplified illustration of those factors. First is the cytoplasmic vestibule through which all permeable solutes must pass to gain access to the pore. In an equivalent cir
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The expression and localization of Cx Cx and Cx in
2022-01-17

The expression and localization of Cx43, Cx46 and Cx50 in the anterior pituitary vary with physiological activities and with various conditions associated with both natural and pathological changes in hormone secretion. Anterior pituitary Cx43 and Cx50 levels increase and exhibit a more widespread d
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br Results br Discussion Previous studies have shown that
2022-01-15

Results Discussion Previous studies have shown that all the components of ET system are expressed by various neuronal and non-neuronal structures throughout the CNS (McCumber et al., 1990; Giaid et al., 1991). In effect, endothelin-converting enzyme activity, mRNA, ET-1 and ET-3 immunoreactivi
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As an inflammatory mediator histamine plays a pivotal
2022-01-15

As an inflammatory mediator, histamine plays a pivotal role in nociceptive processes in both the central and peripheral nervous systems (Gemkow et al., 2009; Hough & Rice, 2011; Tiligada et al., 2009). In this respect, the participation of H3Rs in modulating pain, especially neuropathic pain, has at
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a cool way to improve br Background To treat chronic
2022-01-15

Background To treat chronic HCV genotype (GT) 1-infected patients, telaprevir (TLP) or boceprevir (BOC), first generation protease inhibitors (PIs), were used in combination with pegylated-interferon (PEG-IFN) and ribavirin (RBV) triple therapy [1], [2]. The main weaknesses of the first-generatio
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The hypothesis that genes involved in type diabetes evolved
2022-01-15

The hypothesis that genes involved in type 2 diabetes evolved under changing selective pressures and may carry the signature of natural selection motivated us to describe patterns of sequence variation at CAPN10 and GPR35 in human populations. An initial population genetics study reported an unusual
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Finally we investigated increasing basicity as a
2022-01-15

Finally, we investigated increasing basicity as a way to improve solubility. We expected that conversion of the ether linkage of to an -methyl group could improve solubility. More than expected, c-myc inhibitor demonstrated significant improvement of values of solubility for the two media, especi
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br Methods br Results br Discussion br Conclusion The in
2022-01-15

Methods Results Discussion Conclusion The in vivo pEC50 for NEFA release in the rat was derived for 12 GPR81/GPR109A agonists, including the historically well-known nicotinic acid. By integrating in vitro cell assay potency data for both receptors, these in vivo pEC50 values could be rea
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