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The effects of these steroids
2022-01-18

The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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In conclusion we demonstrated that the atypical high
2022-01-18

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 telomerase inhibitors results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts
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The effect of the selected compounds on NF
2022-01-18

The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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br Indirect GLI antagonists br Direct GLI
2022-01-18

Indirect GLI antagonists Direct GLI antagonists Concluding remarks Targeting GLI effectors represents a promising therapeutic strategy for cancer treatment. This is particularly relevant for certain tumors, such as MB, since, although classified into four distinct molecular groups (Hh- or W
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Further we examined the degradation of Cx Autophagy and the
2022-01-18

Further, we examined the degradation of Cx43. Autophagy and the proteasome system have previously been implicated in Cx43 degradation (Falk et al., 2014). DEX inhibited communication between PF-543 synthesis by promoting the degradation of Cx43 through autophagy in osteocytes (Gao et al., 2016). In
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In the present study we also found
2022-01-18

In the present study, we also found that specificity concerns persist for antibody-based tools, like ELISAs. Measuring the same human plasma sample with four different commercial galanin ELISA kits produced four widely different galanin concentrations. No recovery of synthetic galanin peptide added
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A way to identify what subunit interfaces
2022-01-18

A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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br FPRs regulate anti microbial responses The
2022-01-18

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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summarizes FAAH inhibition data for a series of benzofuran
2022-01-17

summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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In addition to the regulation of
2022-01-17

In addition to the regulation of SV exo- and euk 134 by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g. knockout of Munc1
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In terms of outcome measures statistically significant diffe
2022-01-17

In terms of outcome measures, statistically significant differences were only observed in need for invasive mechanical ventilation (23% vs 46%, p-value 0.005) and in-hospital mortality (13% vs 37%, p-value 0.002). Both these outcomes were still statistically significant following adjustment for conf
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Taken together this study provides the proof of concept
2022-01-17

Taken together, this study provides the proof of concept that our novel heterologous human/rat HER2-specific T cell vaccine HuRt-TEXO, which is capable of stimulating both humoral and CTL responses leading to potent antitumor immunity through the circumvention of HER2 tolerance in double transgenic
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br Materials and methods br Results br Discussion Recently w
2022-01-17

Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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To further investigate the relationship between the
2022-01-17

To further investigate the relationship between the pro-neurogenic and therapeutic actions, we analyzed the effect of VP2.51 in the presence of the antimitotic agent TMZ. No overt side effects were found at the time of testing as assessed by direct observation of the behavior of the animals in their
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N6-Cyclopentyladenosine br Acknowledgments br Free fatty aci
2022-01-17

Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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