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The pseudo DUBs KIAA and Abraxas
2021-04-16
The pseudo DUBs KIAA0157 and Abraxas are required for the catalytic function of BRCC36. Comparison of the BRCC36–KIAA0157 heterodimer structure with an inactive BRCC36 homodimer structure provides a model for understanding how this functional interplay is achieved. As shown in schematic form in Figu
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br Introduction As a strong analgesic
2021-04-16
Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft
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Contrary to the profuse dopaminergic innervation of
2021-04-16
Contrary to the profuse dopaminergic innervation of the thalamus found in human and non-human primates (Brown et al., 1979, Sanchez-Gonzalez et al., 2005), in rodents, the RTn is one the few thalamic nuclei that receives dopaminergic input (Anaya-Martinez et al., 2006, Garcia-Cabezas et al., 2007, G
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Sunitinib The following is the supplementary data related to
2021-04-16
The following is the supplementary data related to this article. Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) to produce phosphatidic Sunitinib (PA) (Baldanzi, 2014, Goto et al., 2006, Merida et al., 2008, Sakane et al., 2007, Topham and Epand, 2009). To date, ten
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br Acknowledgement br Introduction Human dihydroorotate dehy
2021-04-16
Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo BAY 87-2243 biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3]. Lefl
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ON-01910 mg br Materials and methods br Results br Discussio
2021-04-15
Materials and methods Results Discussion In this study, we developed a new CysLT1 and CysLT2 receptors-mediated ON-01910 mg guinea pig model for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. Unlike human CysLT2 receptors, which are equally stimulated by both LTC4 and LT
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br Results br Discussion Unraveling the molecular details of
2021-04-15
Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr
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Beside the previously reported Topo
2021-04-15
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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br Funding This work was supported by
2021-04-15
Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo
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Prostaglandin E receptor subtype EP is a
2021-04-15
Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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br Oxidoreductase like MEM for prodrug
2021-04-15
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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Plasminogen is composed of five
2021-04-15
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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KB SRC 4 australia In vitro studies in NSCLC cell lines
2021-04-15
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC KB SRC 4 australia with Growth inhibition (GI50) values ranging from 7 to 32
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Torin1 Interestingly our analyses of human PBMCs using a mon
2021-04-15
Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 Torin1 showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fraction of cel
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br Materials and methods br Results and discussion
2021-04-15
Materials and methods Results and discussion Conclusions Data about the ability of non-conventional ligands to operate class-A GPCRs have been accumulating. Specifically, increasing evidence indicates that oxysterols, oxidized derivatives of cholesterol, are involved in many activities that
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