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exemplifies three of the compounds investigated
2025-02-18
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC (56nM) was more extensively investigated. Although it is a strong inhibitor of several human cytochrome P450’s, particularly 2C9 and 2C19, this was not considered a showstopper.
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To evaluate the ability of both sets of
2025-02-18
To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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The analysis of the profile
2025-02-18
The analysis of the profile of protein phosphorylation in MMS-treated parp apoptosis pathway confirmed that both the ATM and ATR pathways were activated in S-phase blocked cells. Interestingly, phosphorylation of Chk1 was observed 24h after MMS-treatment both in AT- and ATM-inhibited cells, whilst i
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er alpha Significant reductions in GYN cancer patient
2025-02-18
Significant reductions in GYN cancer patient mortality and morbidity rates require treatments that proactively prevent and reverse resistance to chemotherapy and radiation. Combining chemotherapy and radiation with inhibitors of key DDR proteins targets is likely to enhance the ability of genotoxic
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br Interaction between ASK and TRX Thioredoxins are small kD
2025-02-18
Interaction between ASK1 and TRX Thioredoxins are small (∼12kDa) dithiol oxidoreductases ubiquitously expressed in species ranging from plants to archaea and mammals. They perform various biological functions, such as reducing protein disulfide bonds, supplying reducing equivalents to redox glyco
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Obesity is associated with chronic low grade inflammation re
2025-02-18
Obesity is associated with chronic low-grade 4-Methylhistamine dihydrochloride synthesis resulting from increased M1 macrophage infiltration into adipose tissue, which can subsequently lead to the development of insulin resistance. Previously, we reported that LFE and FSB both reduced body weight g
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br Materials and methods br Results br
2025-02-18
Materials and methods Results Discussion Pulmonary fibrosis is a progressive and chronic lung disease and its typical features include Conessine proliferation, epithelial injury, chronic interstitial inflammation, increased extracellular matrix (ECM) production, and collapse of alveoli, al
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In addition to peroxyl radicals the most found radical
2025-02-18
In addition to peroxyl radicals, the most found radical forms in biological systems, some of assays took into account other free radicals such as superoxide anion, hydroxyl, hydrogen peroxide, singlet oxygen and peroxynitrite. ORAC procedure was also modified using different radical sources such as
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Sustained release property is also associated with side effe
2025-02-18
Sustained release property is also associated with side effects reduction [16] that could be confirmed by histopathological analyzes. Massive infiltrating inflammatory cells, hyperproliferation of skin layers and keratin pearls, caused by DMBA and croton oil application [32] are attenuated in Imq-lo
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Maynard et al demonstrated that serum levels of sFlt
2025-02-18
Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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Through an extensive SAR optimization campaign
2025-02-18
Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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br Hypothesis The hypothesis is that AhR in skin diseases
2025-02-17
Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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br Hyperadiponectinemia in disease conditions
2025-02-17
Hyperadiponectinemia in disease conditions Other evidence indicates that hyperadiponectinemia does not necessarily always imply a healthy outcome. Indeed, a recent study suggested that hyperadiponectinemia occurs in various diseases. Given that the risk for AD and vascular dementia is increased i
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In another study authors found
2025-02-17
In another study, authors found that ADORA1 were present on the intrinsically photosensitive retinal ganglion olda (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 ipRGCs are a
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Macrophage polarization is linked to activation of the ligan
2025-02-17
Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic Aura
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