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Jesus et al discovered a new series of azaindole
2024-07-25
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified GSK1210151A 48 and 49 showed I
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br Aurora A Aurora B and
2024-07-25
Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br The role of LOX
2024-07-25
The role of 12/15-LOX plays in autophagy Autophagy is a process by which cellular material is delivered to lysosomal to degrade the damaged organelles and proteins to facilitate nutrient recycling (Towers and Thorburn, 2016). There has been characterized three types of autophagy-macroautophagy, m
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In vascular endothelial cells L arginine
2024-07-25
In vascular endothelial cells, L-arginine produces nitric oxide (NO) under the action of nitric oxide synthase (NOS), and nitric oxide can activate guanylate cyclase to produce a large amount of cGMP, thereby relaxing vascular smooth muscle and expanding blood vessels. Numerous studies have confirme
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To further address the mechanism of Didox s
2024-07-25
To further address the mechanism of Didox’s suppressive effects on mast cell activation, FceRI receptor Darunavir Ethanolate and downstream transcription factor induction were assessed. We found that Didox had no effect on FceRI surface expression, and thus concluded that Didox effects must be occu
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The AT hook motif is highly
2024-07-25
The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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br Introduction The development and
2024-07-25
Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo
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AZ505 ditrifluoroacetate Overexpression of AR can lead to so
2024-07-24
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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In this study using pure
2024-07-24
In this study, using pure enzyme preparations of human placental recombinant AR (hAR) and of AR isolated from bovine lens (bAR), which behave as Michaelis pituitary adenylate cyclase-activating peptide with glyceraldehyde as substrate, is shown that an apparent negative cooperativity action for glu
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Spectroscopic techniques are powerful biophysical tools used
2024-07-24
Spectroscopic techniques are powerful biophysical tools used in the study of biomolecular structures, including those of proteins. UV–Vis Kif15-IN-2 spectroscopy makes use of absorption property of the protein peptide backbone at around 218 nm, and aromatic amino acid residues primarily at around 28
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Previous reports indicate that the expression of AChRs and t
2024-07-24
Previous reports indicate that the expression of AChRs and their clustering on myotubes are critical factors required to induce contacts on muscle fibers in a natural biological system [14], [15], [16], [17], [18], [19]. For instance, in NMJ development in the mouse, AChRs are pre-patterned at sites
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Patients with AAG often respond
2024-07-24
Patients with AAG often respond to intravenous immunoglobulin or plasma exchange. If these therapies are inadequate, ongoing immune suppression with steroids, azathioprine, mycophenylate or rituximab have been shown to be effective in case reports. Our patient seemed initially resistant to steroid t
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br AD and COX LOX
2024-07-24
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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Evidences have suggested that impairment of CK activity cont
2024-07-24
Evidences have suggested that impairment of CK activity contributes to inhibition of Na+, K+-ATPase and H+-ATPase activities during infectious diseases, since these ATPases are dependent of ATP, as observed by Baldissera et al. [31] in fish experimentally infected by Aeromonas caviae. We observed th
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In humans the superior safety profile of lipid associated fo
2024-07-23
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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