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Over the past decade extensive research
2025-02-01
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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According to the present observations the Ampk isoform promo
2025-01-31
According to the present observations, the Ampkα1 isoform promotes AP-1 transcriptional activity and thereby fosters Methscopolamine of AP-1 target genes in cardiomyocytes via activation of Pkcζ. The transcription factor AP-1 plays a decisive role during cardiac remodeling [24], [25], [26], [37]. A
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Over expression of the inflammatory cytokines MMPs and COX a
2025-01-31
Over expression of the inflammatory cytokines, MMPs and COX-2 act as an important inducer of chronic inflammation. COX-2 catalyzes the biosynthesis of prostaglandins (PGs), and induced expression was observed in retinoic acid receptor stimulated with pro-inflammatory cytokines or bacterial lipopoly
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Methods We conducted a secondary analysis of
2025-01-31
Methods We conducted a secondary analysis of an extant cohort of 580 infants hylaxis, premature rupture of membranes, chorioamnionitis, and to prolong pregnancy (latency). Maternal antibiotic exposure did not include Combretastatin A4 given after the time of delivery or antibiotic initiated by sur
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Prostate cell growth and prostate carcinogenesis are not onl
2025-01-31
Prostate cell growth and prostate carcinogenesis are not only mediated by androgens, they are also dependent on functional insulin receptor (IR) and insulin-like growth factor-1 (IGF-1) receptor (IGF1R) signaling. Previous studies addressed this issue and reported a correlation between high insulin
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Detailed analysis of the dose dependence of A effects
2025-01-31
Detailed analysis of the dose dependence of Aβ effects revealed that at low amounts, Aβ can also act as a positive regulator of presynaptic activity, enhancing the neurotransmitter release probability and increasing the neuronal excitability [2]. The facilitator effects of low Aβ dose on excitatory
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First investigation of numerous membered ether
2025-01-31
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindin
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To further demonstrate the significance of Nrf activation in
2025-01-31
To further demonstrate the significance of Nrf2 activation in the prevention of EGF-induced CRC growth by AR inhibitor, we examined the effect of fidarestat on EGF-induced cell viability in Nrf2-ablated cells. Our results suggest that AR inhibitor prevented the EGF-induced cell viability in control
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Signaling through Axl can lead to activation of
2025-01-27
Signaling through Axl can lead to activation of the PI3K/Akt and Ras/MAPK pathways which promote cellular phenotypes (e.g., transformation, migration) consistent with pro-survival and pro-metastatic effects., , Inhibition of Axl activity by a variety of approaches (including pharmacologic, dominant
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An AXL decoy receptor with enhanced
2025-01-27
An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer estradiol vaginal cream and a murine breast cancer cell line in grafting
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Pompe disease is accompanied by the
2025-01-27
Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the akt inhibitor unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results in th
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The relative stereochemistry of both the major and
2025-01-27
The relative stereochemistry of both the major and minor diastereoisomer of (±)-2-(hydroxymethyl)blebbistatin (±)- (and thus (±)-2-(allyloxymethyl)blebbistatin (±)-) was determined with 1D-NOESY experiments (), as crystallization efforts failed. These experiments revealed an interaction between H an
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Acknowledgments br Introduction Prostate cancer is the
2025-01-27
Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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We subsequently performed immunohistochemistry on sections o
2025-01-27
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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MADS box proteins are combinatorial transcription factors in
2025-01-27
MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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