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The acidification of endocytic compartments
2025-01-21

The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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In the nineties we knew that baclofen was
2025-01-20

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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Thus phosphorylation of p was used to measure the intracellu
2025-01-20

Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc Pinorubin expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Res
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Pyrimethamine synthesis Available data thus indicate that th
2025-01-20

Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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Tumor tissues often experience hypoxia owing
2025-01-20

Tumor tissues often experience hypoxia owing to accelerated growth rates of malignant cells, accumulation of metabolic products, disorganization of tumor blood vessels, and high interstitial fluid pressures (Makino et al., 2001). In response to AAD treatment, tumor vascular density often decreases t
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While there is structural information
2025-01-20

While there is structural information on the core of the amyloid fibril, less is known about oligomer structure. There is evidence that the C-terminal of Aβ may form beta barrels in some oligomer species (Tay et al., 2013, Do et al., 2016), or may exist as loosely aggregated strands in other oligome
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Introduction AMP activated protein kinase AMPK is mainly kno
2025-01-20

Introduction AMP-activated protein kinase (AMPK) is mainly known as a highly conserved and ubiquitously expressed energy sensor that is highly sensitive to changes in cellular energy levels (by sensing increases in AMP:ATP and ADP:ATP ratios) and makes appropriate adjustment to balance the consumpt
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Natural flavonoid br The lipoxygenase pathway and microvascu
2025-01-20

The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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The mechanism of transformation into SCLC is unclear but
2025-01-20

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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In this study high concentrations mM of
2025-01-20

In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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In another study authors found that
2025-01-20

In another study, authors found that ADORA1 were present on the intrinsically photosensitive retinal ganglion Aminoallyl-UTP (ipRGCs), and application of adenosine to rat retinas reduced light-evoked spiking of ipRGCs through suppression of a cAMP-mediated pathway (Sodhi and Hartwick, 2014). The ip
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Renal fibrosis is regarded as
2025-01-20

Renal fibrosis is regarded as the final common pathway for most forms of progressive renal disease, and mouse UUO is a widely accepted experimental model of renal injury leading to extreme fibrosis localized to the interstitial compartment. A-306989 attenuated the mRNA expression levels of several k
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punicalagin For the NSCLC patients with EGFR activating muta
2025-01-18

For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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Several dehidropregnenolone derivatives functionalized at C
2025-01-18

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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Axl which belongs to the Tyro Axl
2025-01-18

Axl, which belongs to the Tyro-Axl-Mer (TAM) family of RTKs, has been reported to regulate a variety of physiological processes including cell survival, proliferation, migration and adhesion, through the activation of the phosphoinositide 3-kinase (PI3K)/V-akt murine thymoma viral oncogene homolog (
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