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Oxidative stress has recently been reported
2023-12-16
Oxidative stress has recently been reported as one of the important mechanisms of toxic effect of Cd2+[43]. The mechanism of Cd2+-induced oxidative stress involves an imbalance between generation and removal of ROS in tissues and cellular components, causing damage to membranes, DNA, and proteins [4
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In conclusion we have demonstrated that diaryl pyrazolo pyri
2023-12-16
In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi
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To understand the kinase selectivity profile of this series
2023-12-16
To understand the kinase selectivity profile of this series, melanocortin 1 receptor , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift assa
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During years research efforts at
2023-12-16
During 2002–2004years research efforts at Los Alamos National Laboratory (LANL) focused on constructing a quantum computer based on regular arrays build from neutral radical molecules possessing one single unpaired LXR-623 spin. The idea was built on the ability to manipulate individual electron sp
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We found that several anticancer
2023-12-16
We found that several anticancer drugs inhibit 5-HT3 trans-isomer synthesis current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is
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Here we show that the co activation
2023-12-16
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC TG003 mg and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005
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Thirty six of the analogs synthesized showed ATX inhibition
2023-12-16
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Aurora A or B selective and pan aurora inhibitors have
2023-12-16
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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As shown in B the recombinant human LOX nM showed
2023-12-16
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic PCI32765 and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disappeare
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A positive correlation between nasopharyngeal
2023-12-16
A positive correlation between nasopharyngeal CCL3 and CCL5 [16] concentrations and illness severity was shown in evaluating patients with RSV bronchiolitis [17]. CCL5 and CCL3 are important for monocyte and lymphocyte recruitment to the lung during RSV infection [7], [16], [18]. Despite the signifi
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br Introduction Hepatocellular carcinoma HCC is an aggressiv
2023-12-16
Introduction Hepatocellular carcinoma (HCC) is an aggressive and malignant cancer detected in clinical practice, as it is the third key reason of tumor-related deaths worldwide, with > 800, 000 mortalities every year (Torre et al., 2015). Current treatments for HCC are surgical therapy, liver tra
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Introduction Hepatocellular carcinoma HCC is one of the most
2023-12-16
Introduction Hepatocellular carcinoma (HCC) is one of the most difficult cancers to treat, and it threatens human health severely [1]. Although various interventions, including surgical operation, radiofrequency ablation, and chemotherapy, have been endorsed, the prognosis of HCC patients remains p
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The reasons why antibiotic treatment may be detrimental
2023-12-16
The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga
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GSK180 br Results br Discussion Cardiac dysfunction common c
2023-12-15
Results Discussion Cardiac dysfunction, common complication of severe sepsis, is one cause of death in intensive care units. Accumulated evidence revealed the regulatory effect of autophagy on sepsis-induced cardiac dysfunction [15], [22], although the mechanisms in young and aging are not elu
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Differentiation of skeletal myoblasts is a
2023-12-15
Differentiation of skeletal myoblasts is a tightly orchestrated process that involves myoblast proliferation, multidrug resistance transporter withdrawal, expression of muscle-specific genes, and fusion into multinucleated myofibers (Horsley and Pavlath, 2004; Krauss, 2010). The maintenance of musc
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