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Ryoichi et al modified potent clinical candidate VX with
2024-07-11

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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Aurora A or B selective
2024-07-11

Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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br Materials and methods br
2024-07-11

Materials and methods Results Discussion In the present study, we found that SSTR2, SSTR5, and DA2R proteins are expressed in ACTH-positive artesunate receptor in healthy canine pituitary glands, with particularly high positive cell ratios in the intermediate lobes. Somatostatin has been re
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It has been reported that Daxx an
2024-07-11

It has been reported that Daxx, an interacting partner of MCRS2/MSP58, promotes ASK1 activation following direct interaction with ASK1 [10], [11]. However, it has not been determined whether MCRS2 is involved in ASK1 signalling. In this study, we identified the direct interaction between MCRS2 and
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Human hepatocyte transplantation resulted in some animals wi
2024-07-11

Human hepatocyte transplantation resulted in some animals with relatively sparse repopulation while others had >90% of their liver containing human hepatocytes. The presence of circulating human albumin varied based on the amount of repopulation as the degree of humanization is reported to correlate
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Previous research showed that combination of chitosan and
2024-07-11

Previous research showed that combination of chitosan and 324 4 nanocrystals (CNCs) can produce coating films with superior properties (Naseri, Mathew, Girandon, Fröhlich, & Oksman, 2015). CNCs are crystalline nanometer sized rod-like particles. It has been demonstrated that antimicrobial activity
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Previous studies demonstrate that chiral biointerface
2024-07-11

Previous studies demonstrate that chiral biointerface has great influence on cells adhesion and proteins adsorption [39], [40], [41], [42], [43], which inspired us to further develop antimicrobial materials or surfaces by taking advantage of the “chiral taste” of microbes. L-borneol is a hydrophobic
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Pathological angiogenesis occurs when an imbalance of endoge
2024-07-11

Pathological angiogenesis occurs when an imbalance of endogenous proangiogenic and antiangiogenic factors occurs. Although the focus of angiogenesis-related drug development has been geared to the discovery of antiangiogenic compounds for use in pathologies where excessive angiogenesis occurs (cance
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Intracellular Signaling Cascades From ligand sensitization t
2024-07-11

Intracellular Signaling Cascades. From ligand sensitization to translation of genes, all cellular processes are dependent on the intracellular levels and activity of partners involved in the signaling pathway. These signaling events lead to critical post-translational modifications including phosph
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The number of times an animal reared was the only
2024-07-11

The number of times an animal reared was the only emotional behavior that was significantly higher in the young mice than in the middle-aged group. This may be explained by diminished curiosity or augmented ambulation with aging (Lalonde and Strazielle, 2008). A recent study showed that middle-aged
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In vitro studies with soman
2024-07-10

In vitro studies with soman-inhibited, non-aged AChE revealed a species dependent reactivating potency of HI-6 and MMB-4. With guinea pig AChE second order reactivation rate constants of 0.051 and 0.038mM−1min−1 were determined for HI-6 and MMB-4, respectively (Luo et al., 2007). Corresponding value
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Using constant potential amperometry and electrochemical enz
2024-07-10

Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of ack1 inhibitor release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured simultane
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Concerning asthma in a study evaluating the effect
2024-07-10

Concerning asthma, in a study evaluating the effect of tiotropium in severe asthma, the sputum eosinophil count and exhaled nitric oxide were also assessed. However, evaluation of the anti-inflammatory effect of tiotropium was difficult because these markers were low at baseline and thereafter. In a
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The presence of different LO splice variants
2024-07-10

The presence of different 5-LO splice variants was first demonstrated in human Vatalanib tumour cells and in dimethyl sulfoxide-differentiated HL-60 cells [40] and a correlation between the 5-LO splicing pattern and the malignancy of the brain tumours was found. Later, other splice variants were ide
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Notably our preliminary results confirmed that fluoxetine SS
2024-07-10

Notably, our preliminary results confirmed that fluoxetine (SSRIs, 5–10 mg/kg) and duloxetine (SNRIs, 5–10 mg/kg) could not enhance memory function in the novel object recognition or step-down passive avoidance tasks (data not shown). In the present study, we also found that vilazodone showed had no
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