Articles with "rxr" as a keyword



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Epigallocatechin‐3‐gallate inhibited cancer stem cell–like properties by targeting hsa‐mir‐485‐5p/RXRα in lung cancer

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Published in 2018 at "Journal of Cellular Biochemistry"

DOI: 10.1002/jcb.27117

Abstract: Non–small‐cell lung cancer (NSCLC) appears to be a significant threat to public health worldwide. MicroRNAs have been identified as significant regulators for the development of NSCLC. Previous reports have suggested that hsa‐mir‐485‐5p is dysregulated in… read more here.

Keywords: cancer; hsa mir; mir 485; rxr ... See more keywords
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Ligand Design for Modulation of RXR Functions.

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Published in 2019 at "Methods in molecular biology"

DOI: 10.1007/978-1-4939-9585-1_4

Abstract: Retinoid X receptors (RXRs) are promiscuous partners of heterodimeric associations with other members of the Nuclear Receptor (NR) superfamily. RXR ligands ("rexinoids") either transcriptionally activate the "permissive" subclass of heterodimers or synergize with partner ligands… read more here.

Keywords: modulation rxr; ligand design; rxr functions; design modulation ... See more keywords
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The role of resveratrol, Sirtuin1 and RXRα as prognostic markers in ovarian cancer

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Published in 2021 at "Archives of Gynecology and Obstetrics"

DOI: 10.1007/s00404-021-06262-w

Abstract: Ovarian cancer is the most lethal gynecologic cancer. Resveratrol (RSV) is known to alter metabolism in cancer. It affects the nuclear retinoid-X-receptor (RXR), which implies a modulating effect of RXR to gynaecologic cancers. Furthermore, RSV… read more here.

Keywords: cancer; expression; sirt1; resveratrol ... See more keywords
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Bexarotene, a Selective RXRα Agonist, Reverses Hypotension Associated with Inflammation and Tissue Injury in a Rat Model of Septic Shock

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Published in 2017 at "Inflammation"

DOI: 10.1007/s10753-017-0691-5

Abstract: Abstract Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that can activate or inhibit the expression of many target genes by forming a heterodimer complex with the retinoid X receptor (RXR). The aim of this study… read more here.

Keywords: inflammation; expression; bexarotene selective; rat ... See more keywords
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Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists

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Published in 2017 at "Journal of Computer-Aided Molecular Design"

DOI: 10.1007/s10822-017-0025-6

Abstract: HX531, which contains a dibenzodiazepine skeleton, is one of the first retinoid X receptor (RXR) antagonists. Functioning via RXR-PPARγ heterodimer, this compound is receiving a lot of attention as a therapeutic drug candidate for diabetic… read more here.

Keywords: function fixed; docking mode; active conformation; retinoid receptor ... See more keywords
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Pharmacological Activation of RXR-α Promotes Hematoma Absorption via a PPAR-γ-dependent Pathway After Intracerebral Hemorrhage.

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Published in 2021 at "Neuroscience bulletin"

DOI: 10.1007/s12264-021-00735-3

Abstract: Endogenously eliminating the hematoma is a favorable strategy in addressing intracerebral hemorrhage (ICH). This study sought to determine the role of retinoid X receptor-α (RXR-α) in the context of hematoma absorption after ICH. Our results… read more here.

Keywords: hematoma absorption; pharmacological activation; intracerebral hemorrhage; activation rxr ... See more keywords
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DNA methylation at CpG island shore and RXRα regulate NR2F2 in heart tissues of tetralogy of Fallot patients.

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Published in 2020 at "Biochemical and biophysical research communications"

DOI: 10.1016/j.bbrc.2020.06.110

Abstract: The nuclear receptor subfamily 2 group F member 2 (NR2F2) gene encodes a ligand-inducible transcription factor involved in angiogenesis and heart development. This study aimed to elucidate the molecular mechanism of epigenetic regulation of NR2F2… read more here.

Keywords: island shore; methylation; cpg island; rxr ... See more keywords
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Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening.

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Published in 2019 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2019.01.007

Abstract: Retinoid X receptor alpha (RXRα), a central member of the nuclear receptor superfamily and a key regulator of many signal transduction pathways, has been an attractive drug target. We previously discovered that an N-terminally truncated… read more here.

Keywords: tetramer stabilizer; screening; atorvastatin; nuclear receptor ... See more keywords
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Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ.

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Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c01266

Abstract: The three retinoid X receptor subtypes (RXRα, RXRβ, RXRγ) exhibit critical regulatory roles in cell proliferation and differentiation, metabolism, and inflammation. Due to their importance in nuclear receptor signaling, RXRs are widely distributed and pan-RXR… read more here.

Keywords: rxr agonist; rxr rxr; new rxr; rxr ... See more keywords
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Evaluating Novel RXR Agonists That Induce ApoE and Tyrosine Hydroxylase in Cultured Human Glioblastoma Cells.

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Published in 2021 at "ACS chemical neuroscience"

DOI: 10.1021/acschemneuro.0c00707

Abstract: There is considerable interest in identifying effective and safe drugs for neurodegenerative disorders. Cell culture and animal model work have demonstrated that modulating gene expression through RXR-mediated pathways may mitigate or reverse cognitive decline. However,… read more here.

Keywords: apoe tyrosine; gene expression; gene; tyrosine hydroxylase ... See more keywords
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Creation of Fluorescent RXR Antagonists Based on CBTF-EE and Application to a Fluorescence Polarization Binding Assay.

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Published in 2021 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.1c00201

Abstract: Retinoid X receptor (RXR) ligands often bind in modes in which the carboxy group forms a hydrogen bond inside the ligand-binding pocket (LBP). However, our previously reported RXR antagonist, CBTF-EE (4a), binds with its carboxy… read more here.

Keywords: binding assay; fluorescence polarization; fluorescence; rxr antagonists ... See more keywords