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Since artemisinin shows low solubility and poor oral bioavai
2024-09-11
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Recently the FDA approved the first blood based
2024-09-11
Recently, the FDA approved the first blood-based test for the detection of EGFR mutations in non-small cell lung cancer patients (http://www.fda.gov) (Voelker, 2016). This allows detection of specific, recurrent mutations, which can help the selection of the patients that could benefit from Erlotini
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Initially DPP DPP and prolyl tripeptidyl
2024-09-11
Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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A characteristic of iron present in brain fluids is
2024-09-11
A characteristic of iron present in brain fluids is considerable differences between measured values of ferritin and transferrin and the total iron content value (Table 1). Variation of the latter is compatible with differences in individual metabolisms. However differences between total iron conten
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Imatinib was first approved for the treatment of Philadelphi
2024-09-11
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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br AHR expression in cancer Perhaps the
2024-09-11
AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug
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Vortioxetine is a multimodal antidepressant that acts as an
2024-09-11
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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The hypothalamic pituitary adrenal HPA axis is a
2024-09-11
The hypothalamic-pituitary-adrenal (HPA) axis is a neuroendocrine system that is central to regulating responses to stress (Palazidou, 2012). In older persons, a high dysfunction of the HPA axis is observed (Otte et al., 2005) which may be enhanced by stimulatory effects of genes involved in the axi
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Derivatives of M that possess either an alkyne or
2024-09-10
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these sphingosine to maintain 5-HTR antagonist properties as (+)-M100907 was demonstra
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NVP-BGJ398 phosphate Moreover our present work suggests that
2024-09-10
Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in NVP-BGJ398 phosphate activated with AXL receptor ligand. A role
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The transcription factor activator protein AP is a
2024-09-10
The transcription factor activator protein-1 (AP-1) is a redox-sensitive transcription factor whose activity is controlled by agents that perturb intracellular thiol concentrations [10,11]. AP-1 is mainly composed of Jun, Fos, and ATF protein dimers [12,13]. AP-1 mediates the regulation of numerous
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br Conclusion We present here the first comprehensive analys
2024-09-10
Conclusion We present here the first comprehensive analysis of B-Raf-induced transcriptional activation in insulinoma cells. The B-Raf-induced signaling cascade targets the c-Fos and the c-Jun genes. Both gene products are constituents of the AP-1 transcription factor. The phosphatases MKP-1 and
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Enhancers are short regions of DNA
2024-09-10
Enhancers are short regions of DNA that are bound by DNA-binding proteins (TFs) to increase the likelihood of a particular gene to be expressed. Importantly, enhancers can be identified, and classified, by their patterns of chromatin accessibility and of enrichment in certain histone modifications.
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Fig shows a possible scheme of the generation
2024-09-10
Fig. 8 shows a possible scheme of the generation of AP(+)-exosomes based on this study. In response to inflammatory stimuli, ERAP1 is secreted from ER into the extracellular milieu through the conventional secretion pathway. On the other hand, exosomes are derived from the endosomal pathway, and are
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BH3I-1 mg A characteristic of iron present in brain fluids i
2024-09-10
A characteristic of iron present in brain fluids is considerable differences between measured values of ferritin and transferrin and the total iron content value (Table 1). Variation of the latter is compatible with differences in individual metabolisms. However differences between total iron conten
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