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Several lines of evidence suggest that thermosensation in AF
2022-06-07

Several lines of evidence suggest that thermosensation in AFD is unlikely to be mediated by thermosensitive ion channels. AFD exhibits a steep temperature dependence with a reported Q of >1015 for temperature-evoked current, implying a strong amplification step in the thermotransduction process (Ram
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br Ketone body metabolism and neuronal excitability One of t
2022-06-07

Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona
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br Material and methods br
2022-06-07

Material and methods Results The search for proteins selectively expressed in pancreatic islet 84 9 in the Human Protein Atlas (HPA) yielded 27 hits, including well-known islet cell markers such as insulin, glucagon and pancreatic polypeptide (Table 1). The search algorithm excluded islet cell
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Firstly the impact on activity
2022-06-07

Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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In summary we have developed an efficient synthetic route to
2022-06-06

In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ-
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d-cycloserine sale br Acknowledgments This work was supporte
2022-06-06

Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE010200
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Interestingly mGlu and mGlu receptors differ notably by thei
2022-06-06

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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We recently reported the first cyclopropene analog of
2022-06-06

We recently reported the first cyclopropene-analog of the amino Trigonelline receptor neurotransmitter glutamate (Fig. 2A) [27]. This first-generation cyclopropene-glutamate expanded the only other documented report of a cyclopropene-neurotransmitter (cyclopropene-GABA analog by Reissig and coworke
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br Conflicts of interest br Funding This
2022-06-06

Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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br Materials and Methods br Results br Discussion A
2022-06-06

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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br Experimental Procedures br Acknowledgments This work
2022-06-06

Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI) R00 HG006922 and NIH/NHGRI R01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research rep
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The focused set of additional pyrazole
2022-06-06

The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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br Structures of human secretase Before
2022-06-06

Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a dl 473 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specula
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Gal is a amino acid residue peptide
2022-06-06

Gal is a 29-amino Sitafloxacin Hydrate residue peptide, comprising 30 amino acids in humans, isolated from the porcine intestine 30 years ago (Tatemoto et al., 1983). It has been shown to be involved in the regulation of numerous processes, including neuroendocrine control of systems such as the hyp
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cetp inhibitors On the contrary the benzhydrol series showed
2022-06-06

On the contrary, the benzhydrol series showed modest activity with EC of two digit micromole. The bulkiness of the cetp inhibitors tail may be the reason for the low activity. Interestingly, introduction of H-bonding groups, such as OMe in and CF in , slightly improved the activity compared to the
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