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Of all ES cases approximately
2020-12-22
Of all ES cases, approximately 26–28% are metastatic diseases at diagnosis with the remainder being localized disease [14]. Instituting a systemic chemotherapy regimen in combination with surgery and/or radiotherapy has significantly increased the survival of patients with localized disease. The 5-y
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Given the potency enhancing effect of the
2020-12-22
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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Altered brain insulin signaling and
2020-12-22
Altered Apoptosis Inhibitor insulin signaling and CNS hypometabolism are also associated with pathogenesis of neurodegeneration. Insulin receptors are mostly located in the cerebral cortex, hippocampus, cerebellum, hypothalamus and olfactory bulb, possess an effective role in the regulation of cent
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The ADME profile of AAT was very promising
2020-12-22
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in . A
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Leflunomide In the present study it was particularly of inte
2020-12-22
In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including Leflunomide pai
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Quantum dots QDs which exhibit excellent fluorescence quantu
2020-12-22
Quantum dots (QDs), which exhibit excellent fluorescence quantum yields (QYs), high extinction coefficients and size-tunable narrow emission have highly attracted great interest in various applications such as in solar cells, sensors, and bioimaging [16], [17], [18], [19], [20]. However, QDs suffere
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Dual inhibition of ACE and NEP as a
2020-12-22
Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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The AURA trial was a phase I II study
2020-12-22
The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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Interestingly we observed that T D islet cells have lower
2020-12-21
Interestingly, we observed that T2D islet Flurbiprofen have lower DPP-4 expression, as compared to ND cells (Fig. 1, Fig. 2). Previously, a reduced activity of this peptidase was observed in human T2D islet lysates (Omar et al., 2014). As mentioned above, GLP-1 is also produced by islet cells (alph
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In conclusion our work led
2020-12-21
In conclusion, our work led to the characterization of some signalling events of the CysLT1 receptor variants, at several levels, and showed that a punctual serine mutation could alter the response of receptors to cysLTs. Although atopy is a complex phenotype implicating different cell types, media
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The corticotropin releasing factor CRF also referred
2020-12-21
The corticotropin-releasing factor (CRF) also referred to as corticotropin-releasing hormone, is a key mediator of mammalian endocrine, behavioral, autonomic, and immune responses to stress (Vale et al., 1981, Owens and Nemeroff, 1991, Bale and Vale, 2004). Within the hypothalamic–pituitary–adrenal
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To the best of our knowledge this study was the
2020-12-21
To the best of our knowledge, this study was the first to demonstrate in vitro and in vivo that the lipolytic effect of kinsenoside results from coordination between PKA and AMPK pathways. We validated the lipolytic effect of kinsenoside in vivo and the effect of PKA activation on the modulating AMP
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Under conditions of energy scarcity or nutritional
2020-12-21
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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Additionally of outmost important is
2020-12-21
Additionally, of outmost important is the location of the different CpG islands in relation to the transcription starting site (TSS) of the promoter as well as their interaction with transcription activators or repressors. It has been shown that methylation at the downstream region of the TSS in the
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Octreotide acetate br Results and discussion br Conclusion I
2020-12-21
Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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