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In order to increase the oral bioavailability abiraterone is
2024-12-25
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral survivin (baculoviral IAP repeat-containing protein 5) (21-28) synthesis of abiraterone acetate
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br Conclusion In summary screening a small compound library
2024-12-25
Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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PGR regulation of epithelium stroma crosstalk is proven by
2024-12-24
PGR regulation of epithelium–stroma crosstalk is proven by numerous studies that utilize genetically engineered mouse models. Before embryo implantation, epithelial PGR mediates the progesterone signal to transcriptionally increase the Ihh levels 13, 15. Epithelial IHH then activates the stromal hed
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AACOCF3 Introduction Preeclampsia a serious hypertensive dis
2024-12-24
Introduction Preeclampsia, a serious hypertensive disorder that can occur during pregnancy, is a pregnancy-related disease characterized by the onset of AACOCF3 and proteinuria after the 20 t h week of gestation, and it occurs in about 5% of all pregnancies [1]. If left untreated, preeclampsia can
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br ROS in AiP and regeneration Tissue wounding and inflammat
2024-12-24
ROS in AiP and regeneration Tissue wounding and inflammation are associated with production of ROS, and recent studies show that generation of ROS, especially during the initial stages of wounding and regeneration are essential for an efficient wound healing response. ROS, in particular H2O2 func
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Pathological angiogenesis occurs when an imbalance of endoge
2024-12-24
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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The loss of synaptic proteins such as synaptophysin
2024-12-24
The loss of synaptic proteins such as synaptophysin from the Phenazine methosulphate is indicative of synapse degeneration and provided a good correlate of the degree of dementia in AD [12], [13], [14]. Consequently, the loss of synaptic proteins from cultured primary neurons incubated with Aβ prov
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br Materials and methods br Results br Discussion
2024-12-24
Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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In the QFP rs T allele showed
2024-12-24
In the QFP, rs2269657-T allele showed a significant correlation with reduced plaque density in frontal cortices (Table 2), strengthening the association with amyloid pathology. The same Live/dead cell assay region was shown to exhibit a statistically significant reduction of SREBF2 mRNA levels in r
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With one exception all receptors for dopamine DA
2024-12-24
With one exception, all receptors for dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT), and norepinephrine are metabotropic receptors. The five metabotropic DA receptors (D1–D5) in the CNS are involved in motivation, pleasure, cognition, learning, memory, fine motor control, and modulate neuroen
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To reconstruct the amino acid sequence of an ancestral
2024-12-23
To reconstruct the amino n-acetyl-5-methoxytryptamine sequence of an ancestral β subunit a molecular phylogeny is required, which is inferred from a β subunit sequence alignment. To build this alignment we searched the NCBI database for proteins similar in sequence to the human muscle-type β subuni
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Search sphere This sphere includes the acetylcholine binding
2024-12-23
Search sphere 1: This sphere includes the hydrogel itaconic acid anti-inflammatory binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the c
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Several dehidropregnenolone derivatives functionalized at C
2024-12-23
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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NOXA a BH only protein is best
2024-12-23
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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NOS is classified into three isoforms endothelial
2024-12-23
NOS is classified into three isoforms: endothelial (eNOS), neuronal (nNOS), and inducible (iNOS), iNOS is expressed in macrophages (Eisenstein, Huang, Meissler Jr, & al-Ramadi, 1994) and osteoblast-like cells (Riancho et al., 1995) and is involved in the regulation of inflammatory reactions (Eisenst
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