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br Conclusion br Acknowledgment This study was supported
2022-03-12
Conclusion Acknowledgment This study was supported by grants from the Excellence Initiative of the German federal and state governments, the Else Kröner-Fresenius Foundation and the German Society for Cardiology (DGK) to F.K. and grants from the Deutsche Forschungsgemeinschaft (SFB TRR 219 M-0
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br Clinical trials testing GLP mimetics in
2022-03-12
Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino GSK2606414 incretin growth factor which activates pancreatic islets to enhance insulin sec
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With rare exceptions the biological
2022-03-12
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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hmg-coa reductase inhibitors A group of small molecule with
2022-03-12
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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To improve the preferential GalR binding we
2022-03-12
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Recently we indicated that cell motility was
2022-03-12
Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 Methimazole treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) which is a poten
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Interestingly the subcellular localization of FBPase in hepa
2022-03-12
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Tankyrase Inhibitors 49 reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our result
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In Kdm c germline and forebrain conditional knockout
2022-03-11
In Kdm5c germline and forebrain conditional knockout mice, RNA sequencing showed the upregulation of a large set of genes, suggesting that Kdm5c functions primarily as a transcriptional repressor [,]. While no changes in global H3K4me3 levels were observed in the knockout neurons, there were thousa
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As for hMOF inhibitor s study Dekker and Zheng
2022-03-11
As for hMOF inhibitor's study, Dekker and Zheng et al. synthesized MG149 (Fig. 1) as an inhibitor of Tip60 and MOF which has an IC50 value of 74 ± 20 μM and 47 ± 14 μM [31]. However, MG149 has no experimental data on hMOF in cell or in vivo. The lack of hMOF inhibitor limits the function study of hM
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With LML methyl oxo dihydropyridazin yl piperidin yl cyclobu
2022-03-11
With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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nmda A second feature of the Ras type
2022-03-11
A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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br Introduction Atherosclerosis is a chronic inflammatory di
2022-03-11
Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino cdc42 pathway derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown
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We also investigated fat depots in mesenteric and
2022-03-11
We also investigated fat depots in mesenteric and retroperitoneal adipose tissues as well as in the liver and verified a reduction in lipid droplets following exercise or exercise and FS oil treatments in the liver from obese mice. Potential molecular candidates in the modulation of adipose tissue b
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This evidence suggests that the human cochlea is equipped
2022-03-11
This evidence suggests that the human cochlea is equipped with antigen presenting macrophages as well as T lymphocytes that execute cytotoxic and immune mediation function. In an animal study, following acoustic overstimulation, Yang et al. (2015) found infiltration of macrophages into the region of
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Phenytoin sodium Originally identified as a GPCR upregulated
2022-03-11
Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated Phenytoin sodium to extrafollicular sites for early plasmablast respons
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