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Our previous studies found that some steroid mimetic structu
2023-10-10
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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Having taken a step back from affinity to
2023-10-10
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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ASK belongs to the family of MAPKKK ASK mediated apoptosis
2023-10-10
ASK1 belongs to the family of MAPKKK. ASK1-mediated apoptosis is involved in the pathogenesis of several diseases such as I/R injury, infectious diseases and neurodegenerative disorders [33], [34], [35]. ASK1 can be activated through different mechanisms. One mechanism is that oxidative stress direc
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The radiographic correlate will be similarly
2023-10-10
The radiographic correlate will be similarly important for the success of other non-VEGF TKIs, such as those targeting the epidermal growth factor receptor expressed in 50% of high-grade primary kanamycin sulfate neoplasms. It has been reported that icotinib and gefitinib, epidermal growth factor re
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Sorafenib was the first small
2023-10-10
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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As an internal control this study validated many of the
2023-10-10
As an internal control, this study validated many of the known associations between GATA3 and predictive markers. GATA3 was shown to be associated with ER and PR, which are both well-known correlations. GATA3 was also negatively correlated with nuclear grade, which is consistent with our knowledge o
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Immunohistochemistry in tissue samples showed the expression
2023-10-10
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of Spectinomycin hydrochloride hydrate tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-ac
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It has been known for
2023-10-10
It has been known for a while that oxygenation (the addition of oxygen) of Aβ can inhibit the formation of amyloids and diminish their cytotoxicity. Photo-oxygenation of Aβ started with fullerenes almost a decade ago by Toshima and co-workers. Later, porphyrins and polyoxometalates were used as well
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br Material and methods br
2023-10-10
Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic Caspase-6, human recombinant protein to support cellular growth and survival. CCH influenc
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ALK fusion positive NSCLC is clinically actionable because
2023-10-10
ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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COPD is almost unheard of in individuals less than years
2023-10-10
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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Further examination of these vmat
2023-10-10
Further examination of these vmat-IR cells shows that they are also positive for vimentin (vim-IR) (Fig. 3A). However, within any one cell there may be a region of weaker vmat-IR, suggesting sub-cellular localization. As also shown in Fig. 3B and C not all vim-IR cells are vmat-IR suggesting that th
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However although in vitro studies in
2023-10-10
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Our in vitro data show that CyaA does not play
2023-10-10
Our in vitro data show that CyaA does not play a critical role in the bacterial adherence to mammalian cells. This observation is in contrast to previous studies that reported a role for CyaA in FHA-mediated adherence of B. pertussis bacteria to the respiratory epithelial ACA synthesis [37,38]. Thi
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In previous research we determined that
2023-10-10
In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and
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