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The mechanisms by which coregulators control the
2019-10-21

The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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br Materials and methods br Results
2019-10-21

Materials and methods Results and discussion Conclusions In the present study, we have shown the important role of miR-204-5p in C2C12 myoblast differentiation. Overexpression of miR-204-5p inhibited myogenic differentiation and decreased the formation of slow-twitch myofibers, whereas miR-
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br Author Contributions br Acknowledgments This work was sup
2019-10-21

Author Contributions Acknowledgments This work was supported, in part, by a grant from the National Cancer Institute of the National Institutes of Health under Grant U01CA202241 and National Institutes of Health under Grant R01NS083856. Introduction The Eph (erythropoietin-producing human
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In addition to the ESIs identified that target both
2019-10-21

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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In this study we investigated whether the Ednra signaling is
2019-10-21

In this study, we investigated whether the Ednra signaling is involved in Hoxa9/Meis1-mediated leukemogenesis. We found an upregulation of Ednra in leukemic murine bone marrow (BM) PP242 sale overexpressing Hoxa9 and Meis1 compared to cells overexpressing Hoxa9 alone. We showed that overexpression
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During the past few years several studies have addressed
2019-10-21

During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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Some antioxidants including N acetylcysteine and SOD have
2019-10-21

Some antioxidants, including N-acetylcysteine and SOD, have been shown to decrease collagen deposition and protect the lungs in various animal models and even in clinical trials (Chan et al., 2013, Loomis-King et al., 2013, Rafii et al., 2013, Teixeira et al., 2008, Wang et al., 2013). Bleomycin-ind
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Mouse Cyp a is a homologous isoform of the
2019-10-21

Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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br Materials and methods br Results
2019-10-21

Materials and methods Results and discussion Summary Acknowledgments We thank Muhammad Anwar for animal rearing and surgery. We also thank Michael M. Myers for editing. Finally, we thank David Hirschberg for his technical advice. Funding for this project was provided by the Einhorn Famil
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br Materials and methods br Results br Discussion Macrophage
2019-10-21

Materials and methods Results Discussion Macrophages and dendritic cells respond to Toll-like receptor (TLR) ligands by upregulating CH25H expression [4], [5]. In the latter cell type TLR-dependent upregulation is mediated via a signalling pathway that involves NFκB and IFNβ secretion and c
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OHC is a potent regulator of
2019-10-21

25-OHC is a potent regulator of LXR-mediated pathways, that impact on Lithocholic Acid receptor lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OH
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Over the past decade targeting DNA repair proteins
2019-10-21

Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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Elevated production of cysLTs in asthma and rhinitis in gene
2019-10-19

Elevated production of cysLTs in 2-APB and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, therefore, that we
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Ki16198 and The X ray crystal structure of
2019-10-19

The X-ray crystal structure of palbociclib bound to CDK6 without a Ki16198 and (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V complex. I
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TMN 355 Prenylation may turn a flavonoid from
2019-10-19

Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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