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Compounds and administered orally to fasted Harlan Sprague D
2021-02-26
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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Cytochromes P CYP are a superfamily of hemoproteins containi
2021-02-26
Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xen
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Although the findings detailed above provide ample evidence
2021-02-26
Although the findings detailed above provide ample evidence that the activity of the CRF1 receptor in the amygdala plays a role in the acute and chronic effects of alcohol exposure, several important areas of investigation remain understudied. The majority of the work on CRF1-alcohol interactions ha
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To the best of our
2021-02-26
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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br Method br Results br Discussion In
2021-02-26
Method Results Discussion In this cross-sectional study, we investigated the relationship between the COMT ValMet polymorphism and age on regional cortical thickness in healthy adults across the lifespan. The mesocortical pathway was of primary interest because of its projections from the v
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br Discussion Of the age related differences in
2021-02-26
Discussion Of the age-related differences in serum non-cholesterol sterols, we first deal with the cholesterol precursors. After birth, the markedly elevated serum desmosterol values decreased during the first year of life, and after 1 year of age they were similar between the other age groups. S
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Several CHK inhibitors have been reported in the
2021-02-26
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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Amphiphilic compounds lower interfacial tension and its biol
2021-02-26
Amphiphilic compounds lower interfacial tension and its biological production often results in a competitive environmental advantage (Darvishi et al., 2011). The reduction of interfacial tension can increase the biologically available surface areas resulting in increased metabolism of insoluble comp
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The transcription factor CREB has been extensively
2021-02-26
The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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It is well established that a number
2021-02-26
It is well established that a number of intracellular signaling pathways mediate sensitization of sensory neurons (Gold and Gebhart, 2010, Richardson and Vasko, 2002). This redundancy could be advantageous since it provides diversity in initiating and maintaining hypersensitivity in response to inju
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The nitrophenols b d were prepared
2021-02-26
The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric L-NMMA citrate gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration
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Our results showed that in elastase induced AAA TGF
2021-02-26
Our results showed that in elastase-induced AAA, TGF-β neutralization finely tunes macrophage phenotype. Note that several studies have already addressed the role of M1 markers, such as IL-6 and IL-1β, or M2 markers, including IL-10 and TGF-β.4, 9, 10, 11 The expression and the role of ARG1 in AAA h
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The AURA trial was a phase
2021-02-26
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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Introduction Activation of epidermal growth factor receptor
2021-02-26
Introduction Activation of epidermal growth factor receptor (EGFR)-receptor tyrosine kinases (RTKs) is a key factor in the progression of non-small cell lung cancer (NSCLC). EGFR-RTKs cause proliferation, invasion, metastasis, and angiogenesis, as well as suppress apoptosis, in lung adenocarcinoma
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DMH-1 In this study we generated mice in
2021-02-26
In this study we generated mice in which the native Bcl6 locus was engineered to produce a form of Bcl6 containing a mutant RD2 domain that disrupts its repressor function. We found that RD2 domain is essential for pre-GC B cell differentiation and clustering into nascent GC within follicles, in par
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