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In this scenario the receptor
2024-05-17
In this scenario, the receptor tyrosine kinase inhibitors (TKI), sunitinib, an anti-angiogenic agent, was tested in phase III trial, leading to a longer progressing free survival when compared to interferon (median: 11 vs. 5mo, respectively, hazard ratio (HR) = 0.42; 95% CI: 0.32–0.54; Pvandetanib
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At the outset of targeting the
2024-05-16
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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Crystal structures were obtained of sulfonamide and amide as
2024-05-16
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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br Current limitations and future directions There
2024-05-16
Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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Non steroidal anti inflammatory drugs which include
2024-05-16
Non-steroidal anti-inflammatory drugs, which include aspirin and ibuprofen, target COX-2 activity to inhibit inflammation. It has been shown that daily use of a nonsteroidal anti-inflammatory drugs is associated with reduced ER-positive breast cancer recurrence in obese and overweight women. More pr
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br Author contribution br Acknowledgement br Introduction Si
2024-05-16
Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of
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Coincident with APJ receptor several
2024-05-16
Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu
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Dual acting RAAS blockade and neprilysin inhibition
2024-05-16
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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It has been well established that shortly after systemic
2024-05-16
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the microcystin lr and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADPH o
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The control group participants of the current study
2024-05-16
The control group participants of the current study were very similar in age to those of Puertas et al. There was no significant correlation between age and enzyme activity over the short age span studied although age-related changes in the activity of ApA and aspartyl aminopeptidase, typically incr
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br Materials and methods br Results
2024-05-16
Materials and methods Results Table 1 presents the metabolic phenotype of obese minipigs. After 60 d of HFHS feeding, minipigs not only showed an increased body weight (+45%), but also a perturbed GS1101 homeostasis, with higher insulin levels (about +2-fold), HOMA-IR (+5.5-fold), and HOMA-%B
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br Concluding remarks The past
2024-05-16
Concluding remarks The past decade has seen rapid advances in our understanding of the metabolic reprogramming that occurs during tumorigenesis. Strategies to target specific nodes of cancer cell amino Niflumic acid metabolism have progressed from preclinical studies to clinical trials, and are
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Recent genome wide association studies have indicated SORL a
2024-05-16
Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its express
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In conclusion we show that HBP is phosphorylated on three
2024-05-16
In conclusion, we show that HBP1 is phosphorylated on three sites, which control HBP1 transcriptional activity and glioblastoma cell proliferation. This phosphorylation largely depends on AKT, although other kinases may also be involved. In a previous study, we had shown that the PI3K-AKT pathway re
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br Parkinson s Disease and
2024-05-16
Parkinson’s Disease and the immune system Parkinson’s Disease (PD) is the second most common neurodegenerative disorder, after Alzheimer’s, which affects 10 million people globally and is characterized by rigidity, bradykinesia, tremors, and gait instability (O’sullivan et al., 2007). The patholo
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