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br Discussion The regulation of intracellular cholesterol le
2021-02-02

Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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ABH br Localization of D receptors in striatum One
2021-02-02

Localization of D2 receptors in striatum One characteristic of D2Rs that has complicated their study is their expression in multiple neuronal populations within striatum, both pre- and postsynaptically (Beaulieu and Gainetdinov, 2011). In addition to spiny projection neurons (SPNs), which are the
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The aniline R group was extensively explored and
2021-02-02

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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br Experimental procedures br Introduction
2021-02-02

Experimental procedures Introduction Protein kinases represent one of the largest enzyme YT Broth, 2X powder blend australia in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein
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Beside the previously reported Topo I inhibition time
2021-02-02

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Sixty eight male Sprague Dawley rats were acquired
2021-02-02

Sixty-eight male Sprague–Dawley rats were acquired from the University of South Dakota Laboratory Animal Services (Vermillion, SD, USA) and housed in pairs at 22°C (60% relative humidity) on reverse 12h light/dark CHIR-98014 australia (dark cycle started at 10:00a.m.) with food and water freely acce
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Experiment B CP during fear acquisition normalizes fear pote
2021-02-02

Experiment 4B: CP154,526 during fear acquisition normalizes fear-potentiated startle and prevents exacerbation of contextual conditioned fear in SERT−/− rats. As genotypes differed markedly in basal fear acquisition, drug effects could differ strongly between genotypes. Therefore, all effects in th
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Introduction Piperine is a pungent
2021-02-02

Introduction Piperine is a pungent alkaloid and accounts for 2–5% dry weight in black and white peppers (Butt et al., 2013). Physiological benefits of piperine have been a subject of extensive research in recent years. Piperine is an antioxidant with strong anti-inflammatory and antiangiogenic acti
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br Oxidoreductase like MEM for prodrug
2021-02-02

Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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br Materials and Methods br Acknowledgements br Introduction
2021-02-02

Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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CFSs are recognized as a driver of genome
2021-02-02

CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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br The contribution of Interference RNA and epigenetic in OA
2021-02-02

The contribution of Interference RNA and epigenetic in OA attenuation Interference RNA, a cellular mechanism for post-transcriptional gene silencing that is associated with mRNA. The potential of RNAi has successfully silenced the wide range of protein coding genes. Its high specificity sanctions
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Our recent discovery M P H
2021-02-02

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br Discussion In depression an activation of the
2021-02-01

Discussion In depression, an activation of the inflammation process and production of cytokines (including chemotactic cytokines – chemokines) and their receptors may occur due to the stimulation of the immune system. One of the earliest studied and described cytokines in depression is interleuki
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br Experimental procedures br Introduction Perfluorooctane
2021-02-01

Experimental procedures Introduction Perfluorooctane sulfonate (PFOS) is an anthropogenic compound with high thermal, chemical and biological stability, which makes it a perfect ingredient for many industrial applications (Kissa, 2001). Nevertheless, these characteristics also mean that PFOS i
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