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The original Aurora kinase was identified during
2024-05-06

The original Aurora kinase was identified during a phenotypic screen for defects in mitotic spindles in Drosophila mutants. Aurora mutants were so named because of the morphological defects at the mitotic spindle resembling the Aurora borealis, or the Northern light [4]. The structure of the Auroras
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br Introduction Lipoxygenases LOXs are a
2024-05-06

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 generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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br Acknowledgments This work was
2024-05-06

Acknowledgments This work was supported by grants from the “Agence Nationale de la Recherche” ANR-09-CESA-006 program, the Agence Nationale de Sécurité Sanitaire de l’Alimentation, de l’Environnement et du Travail (Anses, Project n° 2012-2-077) and the Interdisciplinary Program “Longévité et Viei
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Hepatic inflammation and fibrosis are hallmarks of
2024-05-06

Hepatic ABT-888 australia and fibrosis are hallmarks of the NASH phenotype and are thought to occur in a subset of patients with NAFLD. While it is hypothesized that therapeutic lowering of hepatic lipids will be sufficient to improve hepatic fibrosis and inflammation secondarily, this remains contr
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Overexpression of AR can lead to sorbitol accumulation leadi
2024-05-06

Overexpression of AR can lead to sorbitol accumulation, leading to diabetic complications (Ransohoff and Cardona, 2010). Therefore, AR is an important enzyme in the growth and development of organisms. With the aim of inhibiting the activity of AR in diabetic patients, screening for inhibitors and i
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MLN0128 In terms of the full
2024-05-06

In terms of the full-length proteins, it was noted early on that ACs have two cellular localizations: as integral proteins of the plasma membrane and as soluble proteins in the cytosol. Based on the distribution in mammalian sequences, it was initially proposed that subclass IIIa contains only membr
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Although the mechanisms of APP secretion are well characteri
2024-05-03

Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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A similar circuit between pyramidal
2024-05-03

A similar circuit between pyramidal neurons and SST interneurons is also prevalent in layers 2/3 of the cortex. The synapses onto SST interneurons, however, are functionally weak, raising questions about their computational power. In the first set of experiments, Urban-Ciecko et al. (2018) show that
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Molecular docking simulations were carried out for ligands i
2024-05-03

Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic IL
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br Conclusions Triptans are HT B D F receptors agonists
2024-05-03

Conclusions Triptans are 5-HT1B/1D/(1F) receptors agonists and are considered as the gold standard for acute migraine treatment that have been proven effective. Unfortunately, they are contraindicated in patients with cardiovascular diseases due to their vasoconstrictor (side) effects (MaassenVan
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In an effort to determine if one
2024-05-03

In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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fxr agonist To test the compounds metabolic
2024-05-03

To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structural i
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br Conclusion br Acknowledgements br
2024-05-03

Conclusion Acknowledgements Introduction Synapses are the fundamental elements of neuronal networks that enable the processing, encoding, and retrieval of information in the brain, and pathological disruptions in synapse structure are broadly held to underlie the development of neurologica
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br Conclusions br Acknowledgements We would like to
2024-05-03

Conclusions Acknowledgements We would like to thank the members of the Bergmann lab for fruitful discussions in the course of this work. This work was supported by the National Institute of General Medical Sciences (NIGMS) under award number R35 GM118330. The content is solely the responsibili
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The current antifungal pipeline contains several categories
2024-05-03

The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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