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We report here the first study
2023-11-23

We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR b
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Most clinically approved antiangiogenic drugs are aimed at b
2023-11-23

Most clinically approved antiangiogenic drugs are aimed at blocking the action of vascular endothelial growth factor, or VEGF, which is accepted to be the most important tumor-derived angiogenic factor, stimulating proliferation and migration of endothelial cells, as well as branching of vessels (Fe
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2768 br Conclusion br Acknowledgement This study was
2023-11-23

Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the gene
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Heat shock protein Hsp is a molecular chaperone that
2023-11-23

Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p
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As one of emerging high
2023-11-23

As one of emerging high-throughout methods, metabolomics detects metabolites which are ultimate response of biological systems to environmental changes [14]. Metabolomics uncovers metabolic alteration at the systems level. Comparison of global metabolic profiling reflects some unidentified biologica
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Further evidence for action mechanism was provided
2023-11-23

Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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br Discussion With recently improved understanding of the ro
2023-11-23

Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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Rising depolarization was observed during and decaying
2023-11-23

Rising depolarization was observed during and decaying depolarization after the photostimulation (Fig. 1D). The slow decrease of the firing rate after photostimulation is also a remarkable characteristic of the striatal neuron (Figs. 1E, 2 and 3), since the cortex pyramidal neurons (data not shown)
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The gene SRD A encodes the reductase enzyme
2023-11-22

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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In humans the major LOs are subdivided by their positional
2023-11-22

In humans, the major LOs are subdivided by their positional specificity into 5-(ALOX5), 12-(ALOX12) and 15-LO (ALOX15) (Kuhn et al., 2015). 5-LO is the key enzyme for LT biosynthesis and mainly found in mature cells from myeloid origin, including neutrophil, eosinophil and basophil granulocytes, mon
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mtor inhibitors In summary the role of HT and
2023-11-22

In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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br Perspective AA LA and other PUFAs and their lipid
2023-11-22

Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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In this review we will present
2023-11-22

In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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br Acknowledgements We would like to thank Dr Thomas Blanpie
2023-11-22

Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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In summary this report demonstrates another
2023-11-22

In summary, this report demonstrates another successful application of gene editing in iPSCs. Despite the lack of efficient metabolic functional repair after transplantation, the application of gene correction into HLCs might still be a realistic goal for ex vivo gene therapy of liver diseases with
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