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The AURA trial was a
2021-03-15
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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In the absence of ligand RNA CARD of
2021-03-15
In the absence of ligand RNA, 2CARD of RIG-I is masked by the intramolecular interaction with the helicase domain, showing auto-repressed state [33], [34]. But upon viral RNA binding, 2CARD of RIG-I is exposed to interact with the CARD domain of MAVS (also known as Cardif, IPS-1 or VISA) on mitochon
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A prominent example of such enzyme is the
2021-03-15
A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as mu
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Main Text Post translational modifications by ubiquitin
2021-03-15
Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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Most enzymes involved in the addition and removal of ubiquit
2021-03-15
Most FMK involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligases (Ernst et al.
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Acknowledgments We acknowledge the Danish Council
2021-03-15
Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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Next the BE obtained for
2021-03-15
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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br Methods br Results br
2021-03-15
Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3
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In LPS treated BV cells we found
2021-03-15
In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial tyramide mg translocated to the nucleus in a ligand-independent manner afte
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Indeed some cancers may even be
2021-03-15
Indeed, some cancers may even be defined by dysregulated cyclin and thus CDK activity: mantle cell lymphoma, an uncommon lymphoma of mature B cells, is defined by the presence of overexpressed cyclin D1, usually as a result of a translocation between chromosomes 11 and 14 with the net result that cy
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Monastrol Previous studies have demonstrated the role of the
2021-03-13
Previous studies have demonstrated the role of the COMT Val158Met in response to positive and negative emotional stimuli (Bouhuys et al., 1999, Cohn et al., 2009), a fundamental process involved in well-being (Diener et al., 2009a, Diener et al., 1999, Gross and John, 2003). A handful of studies rep
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It would be very useful if unphosphorylated CK s
2021-03-13
It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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This review aims to examine the literature on chloride chann
2021-03-13
This review aims to examine the literature on chloride Thymidine in the context of transplacental transport. After a short overview of the general cellular functions of Cl− channels in epithelia and the molecular classifications of these channels, it will focus on the evidence for the presence of c
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The same reservoir of genes is involved
2021-03-13
The same reservoir of HET0016 is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonable. For insta
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Sennoside C Introduction Taenia solium is the causative agen
2021-03-13
Introduction Taenia solium is the causative agent of human taeniasis/cysticercosis and porcine cysticercosis, a major health problem and a veterinary economic challenge in developing countries of Latin America, Africa, and Asia. In Mexico, approximately 500 human neurocysticercosis cases were repor
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