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At the outset of targeting the two Gln
2025-01-31
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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br Results Four HT esters butyrate
2025-01-31
Results Four HT esters (butyrate, caprylate, laurate and stearate esters) were chosen as representative compounds of increasing lipophilicity (Fig. 1). We will refer to them as C4HT, C8HT, C12HT and C18HT, respectively. They have been synthesized, purified and characterized according to our previ
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Earlier studies with SERMs identified that distinct
2025-01-31
Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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The rescue of the behavioral deficit was associated with
2025-01-31
The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the Thymidine of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming prev
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The mechanism of transformation into SCLC is unclear
2025-01-31
The mechanism of transformation into SCLC is unclear but the loss of retinoblastoma gene (RB) seems important and constitutes an initial event in the tumorigenic process. Some reports revealed the role of the RB gene loss in EGFR mutated NSCLC who transformed into SCLC [15]. In NGS we retrieved mut
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br Materials and methods br Results br Discussion Several ma
2025-01-31
Materials and methods Results Discussion Several major signaling and developmental pathways (e.g. EGFR, ALK, KRAS, TGFβ, Notch and Wnt/β-catenin) have been shown to be involved in lung carcinogenesis and they are being exploited as targets of the non-small cell lung cancer therapy (for revi
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br Increased blood ATX and LPA in liver
2025-01-27
Increased blood ATX and LPA in liver fibrosis Although previous in vitro findings have suggested a link between LPA and liver fibrosis in vivo, whether LPA plays a primary role in the pathogenesis of liver fibrosis has remained uncertain. No phenotypic changes in livers of LPA receptor-deficient
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Starting with commercially available or
2025-01-27
Starting with commercially available 4- or 5-nitropyrazole-3-carboxylic acid, anilides containing nitro, amino or methylsulfonamido were synthesized. Here, manipulation of the substituents on the pyrazole ring was conducted after the anilide formation (). The ATRA of the nitro group was performed wi
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Suramin hexasodium salt PGR regulation of epithelium stroma
2025-01-27
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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br Materials and methods br Results br Discussion Fluoride c
2025-01-27
Materials and methods Results Discussion Fluoride can readily penetrate cellular membranes and seriously damage the structure and physiological function of cells (Zhou et al., 2015). Several studies have shown that excessive fluoride can decrease the viability of cells and that the growth o
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To investigate if WP increased
2025-01-27
To investigate if WP increased CAT activity in cells, C2C12 muscle Ryuvidine were treated with 0.1 to 0.4 mg/mL of WP (80.05% protein) for 24 h and then stressed with 0.75 mM H2O2 for 1 h (Xu et al., 2011). The CAT activity was significantly enhanced from 15.1 ± 0.7 to 23.7 ± 1.3 U/mg of total cell
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In an effort to increase
2025-01-27
In an effort to increase antioxidant properties of peptides from WP, Le Maux et al. (2016) altered the hydrolysis conditions (pH, enzyme type, reaction time, and temperature). Hydrolysis of WP (81% protein) test samples with papain (EC 3.4.22.2) at a constant pH of 7.0 gave significantly higher ORAC
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Despite the absence of disulfide bonds in its linear structu
2025-01-27
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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Plant defensins are cysteine rich
2025-01-27
Plant defensins are cysteine-rich cationic peptides of 5–8 kDa whose mature domain comprises 45 to 54 amino EGFR exon 19 deletion residues, with an isoelectric point around 9. The global fold of plant defensins consists of a cysteine-stabilized motif (CSα/β) made up of an α-helix and a triple-strand
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br Materials and methods br Conflict
2025-01-27
Materials and methods Conflict of interest Acknowledgments We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R01GM115366, R01CA160417, and R01CA
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