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The extent to which GPCR oligomerization is a
2023-07-05
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Since the introduction of zebrafish into the laboratory many
2023-07-05
Since the introduction of zebrafish into the laboratory, many milestones have been achieved that firmly establish this organism as a prominent genetic model for biology and medicine. Many features make this species an organism of easy maintenance in laboratory which provides advantages to understand
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Several studies have recently used optogenetics to selective
2023-07-05
Several studies have recently used optogenetics to selectively activate various cholinergic neurons (Jiang et al., 2014). However, most do not explicitly report direct release of GABA from cholinergic fibers, with the exception of our two studies described above (Saunders et al., 2015a, Saunders et
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Screening a selection of analogues from this library
2023-07-03
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to CHR2797 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrated >50%
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IGF signaling has been shown
2023-07-01
IGF-1 signaling has been shown to induce G007-LK changes via interacting with MKK-p38 signaling (Serra et al., 2007) and by perturbing Foxo3a signaling (Stitt et al., 2004), among other mechanisms. The current study demonstrates that the acetyl group itself may be limiting, since IGF-1/ACL/acetyl-C
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SAG While increased arginase levels has been
2023-06-30
While increased arginase levels has been shown in animal models and in humans with cardiovascular dysfunction [16], [22], [23], it is unknown whether plasma levels or activity of Arginase may predict ED risk. In addition, recent evidence suggests that plasma l-arginine hydrolysis by arginases limits
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br Conclusion We have identified three
2023-06-25
Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina
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It is noteworthy to mention the limitations of
2023-06-21
It is noteworthy to mention the limitations of this study like tPA plus LB1 treatment beyond 4 h after stroke was not investigated. Especially 6 or 8 h after stroke could be studied in future projects for translational purposes. Second drawback might be that we performed the experiments in different
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The synthetic adipoR agonists AdipoRon
2023-06-02
The synthetic adipoR agonists, AdipoRon (1) and 112254 (2), are both detectable in human plasma [18]. However, with increasing knowledge about their metabolism [19], a method for detection from human urine is conceivable and would be preferred given the easier accessibility and greater frequency of
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KNK437 Synthesis pharmacological evaluation for the
2023-06-01
Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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We also investigated the transmittance
2023-05-31
We also investigated the transmittance of actin polymerized with and without ABP. The presence of actin in the solution results in an increment in turbidity as other proteins provided Oxamic acid features [21], [32]. While G-actin showed a transmittance peak positioned at 241 nm, F-actin exhibited
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We also investigated the transmittance
2023-05-31
We also investigated the transmittance of actin polymerized with and without ABP. The presence of actin in the solution results in an increment in turbidity as other proteins provided Oxamic acid features [21], [32]. While G-actin showed a transmittance peak positioned at 241 nm, F-actin exhibited
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Recently several groups including ours have started to
2023-05-31
Recently, several groups, including ours, have started to use the C. elegans multi-dendritic PVD neurons as a model system to dissect the molecular mechanisms of dendrite development. During larval development, PVD elaborates complex and stereotyped dendritic arbors by sequentially adding primary (1
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HT modulates cortical and hippocampal pyramidal cell functio
2023-05-30
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Pyrene azide 3 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al
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br Aurora kinases br Wnt signaling pathway
2023-05-30
Aurora kinases Wnt signaling pathway The signal transduction pathway of Wnt/β-catenin signaling pathway plays an important role in embryogenesis to control cell differentiation and tumorigenesis [39]. A recent report indicates that 90% of colorectal cancer occur due to the activation of the Wn
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