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As mentioned above variation of the A ring was undertaken
2024-03-15
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to STA-4783 synthesis (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having compa
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Silodosin br Author contributions br Conflict of
2024-03-15
Author contributions Conflict of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81502276), Major Projects of Science and Technology of Health and Family Planning Commission of Hunan Province (A2017013), the Natural Science Foundation o
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In addition to the data provided by the Ki treatment
2024-03-15
In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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HCC aetiology is multifactorial and the disease is often
2024-03-15
HCC aetiology is multifactorial and the disease is often preceded by other conditions including liver fibrosis and cirrhosis that are associated with HCV, HBV, alcoholic and non-alcoholic hepatitis. The discovery of new therapeutic targets will require a greater understanding of the pathogenic mecha
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There are two major isoforms of LO
2024-03-15
There are two major isoforms of 12/15-LO in mammalian, 12 and 15- LO, with different cellular distributions. To determine the relative contributions of these isoforms towards glucose-induced monocyte-endothelial interactions, the distribution of these isoforms in the two cell types involved in leuko
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br Conflict of interest br Acknowledgements br Introduction
2024-03-15
Conflict of interest Acknowledgements Introduction The mitogen-activated protein kinase (MAPK) pathway is an important intracellular signaling system that regulates diverse cellular functions, such as proliferation, differentiation, and apoptosis [1]. Apoptosis signal-regulating kinase 1 (A
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Molecular docking quantitative structure activity relationsh
2024-03-15
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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The neural circuitry involved in the production of the EOD
2024-03-15
The neural circuitry involved in the production of the EOD, its modulations, and in the sensory processing of communication signals has been well characterized (Bell and Maler, 2005; Chacron et al., 2011; Krahe and Maler, 2014; reviewed in Metzner, 1999). Pacemaker cells located in the pacemaker nuc
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br COPD As in asthma also in COPD increased
2024-03-15
COPD As in asthma, also in COPD, increased expression of arginase has been reported, and tobacco smoke may increase expression of arginase in human subjects [46, 47]. Increased ADMA levels have also been reported in COPD, and both the increased expression of arginase and ADMA contribute to remode
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To introduce in a simple way
2024-03-15
To introduce in a simple way the variability in the concentration of the proteins involved in the process, and to consider possible stochastic effects due to possible finite sizes of the populations involved in the problem, the dynamics of each cell is studied using the Gillespie’s algorithm (Gilles
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As with most G protein coupled
2024-03-15
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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In glucose stimulated pancreatic cells B Raf
2024-03-15
In glucose-stimulated pancreatic β-cells, B-Raf activity is increased, while Raf-1 activity is under the detection limit (Duan and Cobb, 2010). Thus, B-Raf is the primary protein kinase involved in the rapid activation of ERK1/2 in glucose-treated pancreatic β-cells. Expression of a dominant-negativ
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Introduction Heterotrimeric G proteins mediate signal transd
2024-03-14
Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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In humans the superior safety profile of lipid associated
2024-03-14
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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Kuda et al reported that
2024-03-14
Kuda et al. (1997) reported that the activity of aminopeptidase A (ApA) but not aminopeptidase B (ApB) nor aminopeptidase N (ApN) was decreased in plasma from patients with Alzheimer's disease (AD). More recently Puertas et al. (2013) reported that the activities of plasma ApA, ApB, ApN and IRAP wer
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