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br Phosphorylation of P c Initial studies In addition
2023-11-20
Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor
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Thirty six of the analogs synthesized showed
2023-11-20
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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br Involvement of LPA receptors
2023-11-20
Involvement of LPA receptors in cancer LPA׳s effects are mediated by at least six different G protein-coupled receptors (LPA1–6). Human gastric and ovarian cancers overexpress the mRNA encoding LPA1 and LPA2 compared to healthy tissues [6], [11], [12]. Papillary and follicular thyroid cancers exh
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Imatinib is a well known anticancer
2023-11-20
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing Pleuromutilin (K562 ce
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Inactivation of the proton pump comes
2023-11-20
Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak comt inhibitors such as methylamine or chloroquine which accumulates in its protonated, n
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br Results br Discussion Control of chronic inflammation is
2023-11-20
Results Discussion Control of chronic inflammation is important in several inflammatory conditions like asthma, rheumatoid arthritis and fibrosis in lung diseases. The regulatory pathways that control chronic inflammation are complex and multi-factorial. Over expression of inflammatory mediato
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Most human diseases e g cancer diabetes and
2023-11-20
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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The current antifungal pipeline contains several categories
2023-11-20
The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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Regardless of the initial treatment
2023-11-20
Regardless of the initial treatment, most patients with advanced NSCLC experience relapse and disease progression [15]. A subpopulation of immediate concern and clinical need is patients who have advanced NSCLC that is especially aggressive, which is usually defined as disease that rapidly progresse
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Dual acting RAAS blockade and neprilysin inhibition has been
2023-11-20
Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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As noted above yeasts particularly
2023-11-18
As noted above, yeasts, particularly S. cerevisiae (Frey and Röhm 1978; Trumbly and Bradley 1983), produce APs, but these are intracellular enzymes located in the vacuolar compartment, with the exception of aminopeptidase II. About 40% of aminopeptidase II activity is detected as external enzyme, li
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br Perspective AA LA and
2023-11-18
Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path
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The mechanism of transformation into SCLC is unclear but the
2023-11-18
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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Acetaminophen N acetyl p aminophenol
2023-11-18
Acetaminophen (N-acetyl-p-aminophenol, AAP) (Fig. 1) is a medically important, low cost, readily available and commonly used over the counter analgesic and antipyretic drug [18,19]. Acetaminophen monotherapy is efficient and is safer than Aspirin and Ibuprofen [20]. The efficacy and tolerability in
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Rising depolarization was observed during and decaying depol
2023-11-18
Rising depolarization was observed during and decaying depolarization after the photostimulation (Fig. 1D). The slow decrease of the firing rate after photostimulation is also a remarkable characteristic of the striatal neuron (Figs. 1E, 2 and 3), since the cortex pyramidal neurons (data not shown)
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