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Recently two distinct small molecule inhibitors of
2024-08-30
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer nor-NOHA acetate with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the
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Here we have used transcriptome
2024-08-30
Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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The disease stimulatory effects of hyperadiponectinemia in
2024-08-30
The disease-stimulatory effects of hyperadiponectinemia in patients contradict a previous view based on studies of preclinical models showing that APN might be beneficial for AD [8]. Indeed, despite the action of APN as a risk factor in patients with AD, APN is protective against oxidative stress-in
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We also demonstrate that PACAP
2024-08-30
We also demonstrate that PACAP treatment dose-dependently disrupts performance in the 5CSRTT, suggestive of attentional deficits, another core feature of mood and anxiety disorders. Treatment with PACAP (.5–1.0 µg) decreased the percentage of correct responses, increased the percentage of trials in
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The results also showed that the A receptor http www
2024-08-30
The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 Eeyarestatin I stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transection model
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Silk which is a mixture of mainly SF
2024-08-30
Silk, which is a mixture of mainly SF and sericin, has an extensive history in clinical application as a suture material. Unwanted immune reactions to silk sutures observed early on in their application were assigned to the presence of sericin. However, in vitro and in vivo evaluations of pure SF fi
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The AChR is composed of five homologous membrane spanning su
2024-08-30
The AChR is composed of five homologous, membrane-spanning subunits. AChRs containing two α, one β, one δ and one γ subunit (AChRγ) predominate during embryonic development and mice lacking AChRγ die at birth (Takahashi et al., 2002). After birth, the AChRγs are replaced during the first 2 postnatal
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PF also a dual Aurora A and Aurora B inhibitor
2024-08-30
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly cappung for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was defined
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Although TP status has been shown to play
2024-08-29
Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient p2x7 antago
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In Rainey et al published the
2024-08-29
In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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Among steroid saponins ginsenosides are the
2024-08-29
Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid
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For the derivatives a c another likely
2024-08-29
For the derivatives 3a–3c, another likely explanation for antifungal properties is that polymers bearing primary amine groups and secondary phosphoryl groups formed, enhancing complexation with the phosphate groups, and the complexes are amphiphilic (Palermo, Lee, Ramamoorthy, & Kuroda, 2011). The a
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The association of male gender with increased atherosclerosi
2024-08-29
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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The first and the best
2024-08-29
The first and the best-characterized mechanism of receptor-dependent internalization of Aβ is mediated via the α7-nicotinic ABT-869 synthesis receptor [82]. Lipoprotein receptor protein represents the second best-studied route that facilitates the uptake of Aβ by neurons, involving additional molec
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A unique finding in this study is that LO influences
2024-08-29
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic A-443654 mg for substrate, can regulate CREB phosphoryation in the context of Alzheimer
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