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D appears to be important for receptor function
2021-10-18
D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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br Materials and methods br Results br
2021-10-16
Materials and methods Results Discussion Protein degradation plays a vital role in nearly all cellular processes, nearly 5% of genes are dedicated to the control of protein stability [31], [32]. The ubiquitin-proteasome system (UPS) represents the major way for degradation of proteins, whe
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br Role of funding source br
2021-10-16
Role of funding source Conflict of interest Acknowledgements We thank F. Blaskovits and P. Kesner for technical assistance. This project was supported by operating grants from the Canadian Institutes of Health Research (CIHR) to X. Zhang (MOP123249) and the National Natural Science Foundati
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While the binding of HK to
2021-10-16
While the binding of HK1 to VDAC1 is strong and continuous, the binding of HK2 to VDAC1 is much weaker, and alternates between a cytoplasmic and a mitochondrial-bound states (John et al., 2011). This dynamic process is regulated by the metabolic and energetic requirements of the NECA and provides t
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br Material and methods br Results br Discussion
2021-10-16
Material and methods Results Discussion Liver plays a key role in the metabolism and detoxification of DON (Peng et al., 2017). However, various DON investigations generated inconsistent results, with some showing hepatotoxicity of DON, while others not. For example, one report stated that
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br Conflict of interest br Funding This work was supported
2021-10-16
Conflict of interest Funding This work was supported by the National Institutes of Health MSK Cancer Center Support Grant/Core Grant [P30 CA008748]. The funding source had no involvement in the study design; in the collection, analysis and interpretation of data; in the writing of the report;
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pregnane x receptor Another interesting approach is to use p
2021-10-16
Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain
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Our observations with RBC in human platelets suggested a mor
2021-10-16
Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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Recent work by Que et
2021-10-16
Recent work by Que et al with mouse models implicates GSNOR in the cause of asthma. GSNOR is expressed in multiple cell types in the lung, including airway epithelial cells and infiltrating leukocytes. After exposure to ovalbumin, GSNOR activity increased in airway lining fluid, perhaps reflecting i
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Lactate induced GPR activation was confirmed with
2021-10-16
Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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Several studies have found that GPR possesses
2021-10-16
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected PND-1186 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rim
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Considering the fact that OCL induced depletion of
2021-10-16
Considering the fact that OCL induced depletion of T ikk inhibitor in non-stimulated cultures, the only possible explanation of this effect is the elevated mortality of these cells. It was found that OCL at the higher concentration induced the apoptosis of CD4+ and CD8+ T cells. These results stron
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br Materials and methods br Results br Discussion To the
2021-10-16
Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated sodium salt induced osteogenic effect via Wnt/β-catenin signaling. We found that dose–
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In conclusion we provided the first evidence of a
2021-10-16
In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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Immunohistochemistry using anti FFAR antibodies revealed imm
2021-10-15
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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