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The most potent compounds within the current
2024-06-20
The most potent compounds within the current series of compounds were therefore , , , , and , with 8-Methoxypsoralen synthesis possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM aga
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The synthesis and secretion of adrenal androgens
2024-06-20
The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s
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Our previous studies found that some steroid mimetic
2024-06-20
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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br Acknowledgements We thank Dr Stefan Schulte Merker and
2024-06-20
Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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Inactivation of the proton pump comes with luminal alkaliniz
2024-06-20
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 Cyclo(RGDyK) such as methylamine or chloroquine which accumulates in its protonated, non
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A large number of studies have shown
2024-06-20
A large number of studies have shown that oxidative stress is involved in the pathophysiological process of ventricular remodeling and is associated with left ventricular dysfunction (Hori and Nishida, 2009, Lord et al., 2010). The generation of reactive oxygen species (ROS) that exceeds anti-oxidat
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The mitogen activated protein kinase
2024-06-20
The mitogen-activated protein kinase (MAPK) plays an important role in a variety of cell processes by controlling transcriptional or translational regulation [14]. There are three major MAPK family members that have been well characterized: extracellular signal-regulated kinase (ERK), c-Jun N-termin
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br Material and methods br Results
2024-06-20
Material and methods Results Discussion Asparagine, arginine, leucine, methionine, and glutamine are the essential N1-Methyl-ATP for cancer cells and intensively investigated for the development of selective targeted therapeutics. Among them, asparagine depleting bacterial enzyme asparagina
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The results of our in vivo experiments provide promising
2024-06-19
The results of our in vivo experiments provide promising evidence that the apelin/APLNR axis is implicated in CCA growth and that targeting this axis with a receptor specific antagonist may help develop effective, tumor directed therapies. Not only do we show decreased proliferation and angiogenesis
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The regulation of gene expression
2024-06-19
The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m
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In this study we have
2024-06-19
In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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br AR mediated actions in cells
2024-06-19
AR-mediated actions in ritanserin mg of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discussed e
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br Available treatment modalities for individuals with NAFLD
2024-06-19
Available treatment modalities for individuals with NAFLD There are several treatment modalities currently used or in clinical trials for individuals with NAFLD. The most widely recommended treatment is a lifestyle modification plan. As little as 5% weight loss has been shown to improve NASH hist
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Introduction Increasing environmental pollution caused
2024-06-19
Introduction Increasing environmental pollution caused by heavy metals, originating mainly from industrial processes and urban activities, as well as the widespread application of pesticides, fertilizers, manure and sewage sludge, has posed a serious problem for safe food production and become a po
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COPD is almost unheard of in individuals less
2024-06-19
COPD is almost unheard of in individuals less than 40 years of age (even among heavy smokers), 1 in 10 lifetime never-smokers and 1 in 3 develop COPD by age 75 [26], unquestionably, COPD is an age-related disorder. This notion of accelerated ageing of COPD is supported by animal models, which demons
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