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Statin Use at the Time of Initiation of Androgen Deprivation Therapy and Time to Progression in Patients With Hormone-Sensitive Prostate Cancer
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July 2015 |
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Pharmacologic Repression of Retinoic Acid Receptor-Related Orphan Nuclear Receptor γ Is Therapeutic in the Collagen-Induced Arthritis Experimental Model: Pharmacologic Repression of RORγ as Therapy for CIA
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February 2014 |
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Orphan nuclear receptor RORγ confers doxorubicin resistance in prostate cancer
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July 2020 |
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Structural States of RORγt: X-ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds
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June 2017 |
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NSDHL promotes triple-negative breast cancer metastasis through the TGFβ signaling pathway and cholesterol biosynthesis
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April 2021 |
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Migration of MDA-MB-231 breast cancer cells depends on the availability of exogenous lipids and cholesterol esterification
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July 2011 |
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Steroid Hormones, Steroid Receptors, and Breast Cancer Stem Cells
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June 2015 |
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The cholesterol metabolite 27-hydroxycholesterol regulates p53 activity and increases cell proliferation via MDM2 in breast cancer cells
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September 2015 |
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Sterol-regulatory element-binding protein (SREBP)-2 contributes to polygenic hypercholesterolaemia
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September 2002 |
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Sequence dependence of protein isoprenylation
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August 1991 |
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X-Ray Structure of the hRORα LBD at 1.63 Å
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December 2002 |
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Targeting castration-resistant prostate cancer with a novel RORγ antagonist elaiophylin
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December 2020 |
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SUMOylation of RORα potentiates transcriptional activation function
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January 2009 |
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Protein kinase A activates and phosphorylates RORα4 in vitro and takes part in RORα activation by CaMK-IV
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May 2011 |
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The tumor-suppressor cholesterol metabolite, dendrogenin A, is a new class of LXR modulator activating lethal autophagy in cancers
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July 2018 |
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Intracrine mechanism of estrogen synthesis in breast cancer
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December 2003 |
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Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
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January 2018 |
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Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc
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December 2013 |
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Identification of tertiary sulfonamides as RORc inverse agonists
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May 2014 |
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Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
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January 2018 |
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Steroid Hormone Receptors in Prostate Cancer: A Hard Habit to Break?
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December 2009 |
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The Orphan Nuclear Receptor RORγt Directs the Differentiation Program of Proinflammatory IL-17+ T Helper Cells
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September 2006 |
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A Validated Regulatory Network for Th17 Cell Specification
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October 2012 |
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Nuclear Receptors, RXR, and the Big Bang
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March 2014 |
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A Multiscale Map of the Stem Cell State in Pancreatic Adenocarcinoma
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April 2019 |
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Anticancer Activity of the Cholesterol Exporter ABCA1 Gene
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September 2012 |
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27-Hydroxycholesterol Promotes Cell-Autonomous, ER-Positive Breast Cancer Growth
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November 2013 |
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Sirtuin-1 Activation Controls Tumor Growth by Impeding Th17 Differentiation via STAT3 Deacetylation
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April 2017 |
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Increased Cholesterol Biosynthesis Is a Key Characteristic of Breast Cancer Stem Cells Influencing Patient Outcome
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June 2019 |
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Genome-wide Localization of SREBP-2 in Hepatic Chromatin Predicts a Role in Autophagy
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April 2011 |
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Cholesteryl Ester Accumulation Induced by PTEN Loss and PI3K/AKT Activation Underlies Human Prostate Cancer Aggressiveness
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March 2014 |
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Identification of Natural RORγ Ligands that Regulate the Development of Lymphoid Cells
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February 2015 |
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Post-translational regulation of RORγt—A therapeutic target for the modulation of interleukin-17-mediated responses in autoimmune diseases
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August 2016 |
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Subgroups of Castration-resistant Prostate Cancer Bone Metastases Defined Through an Inverse Relationship Between Androgen Receptor Activity and Immune Response
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May 2017 |
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T0901317 is a potent PXR ligand: Implications for the biology ascribed to LXR
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March 2007 |
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Molecular Antagonism and Plasticity of Regulatory and Inflammatory T Cell Programs
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July 2008 |
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Interleukin-1 and IL-23 Induce Innate IL-17 Production from γδ T Cells, Amplifying Th17 Responses and Autoimmunity
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August 2009 |
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Small-Molecule RORγt Antagonists Inhibit T Helper 17 Cell Transcriptional Network by Divergent Mechanisms
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April 2014 |
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Plasma oxysterol levels in luminal subtype breast cancer patients are associated with clinical data
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March 2020 |
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Differential and day-time dependent expression of nuclear receptors RORα, RORβ, RORγ and RXRα in the rodent pancreas and islet
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January 2013 |
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Oxysterols and nuclear receptors
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March 2019 |
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Expanding the View of IKK: New Substrates and New Biology
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March 2021 |
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SREBPs in Lipid Metabolism, Insulin Signaling, and Beyond
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May 2018 |
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The ROS-mediated activation of STAT-3/VEGF signaling is involved in the 27-hydroxycholesterol-induced angiogenesis in human breast cancer cells
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December 2016 |
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T0901317 is a dual LXR/FXR agonist
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September 2004 |
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Discovery of 1-{4-[3-Fluoro-4-((3 S ,6 R )-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist
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June 2015 |
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Discovery of [ cis -3-({(5 R )-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H -inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H )-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
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March 2018 |
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Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer
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April 2019 |
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Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists
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December 2019 |
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Orthosteric and Allosteric Dual Targeting of the Nuclear Receptor RORγt with a Bitopic Ligand
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February 2021 |
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Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist
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March 2020 |
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Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors
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June 2015 |
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Discovery of N -(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases
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January 2020 |
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Identification of SR2211: A Potent Synthetic RORγ-Selective Modulator
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February 2012 |
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Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists
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December 2013 |
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Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action
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December 2014 |
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The p21 ras C-terminus is required for transformation and membrane association
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August 1984 |
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Complex structure of the fission yeast SREBP-SCAP binding domains reveals an oligomeric organization
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November 2016 |
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A transcription factor response element for gene expression during circadian night
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August 2002 |
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Reciprocal developmental pathways for the generation of pathogenic effector TH17 and regulatory T cells
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April 2006 |
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TGF-β-induced Foxp3 inhibits TH17 cell differentiation by antagonizing RORγt function
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March 2008 |
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The aryl hydrocarbon receptor links TH17-cell-mediated autoimmunity to environmental toxins
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March 2008 |
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Digoxin and its derivatives suppress TH17 cell differentiation by antagonizing RORγt activity
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March 2011 |
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Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand
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April 2011 |
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Oxysterols direct B-cell migration through EBI2
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July 2011 |
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Deubiquitinase DUBA is a post-translational brake on interleukin-17 production in T cells
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December 2014 |
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Sterol metabolism controls TH17 differentiation by generating endogenous RORγ agonists
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January 2015 |
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Identification of an allosteric binding site for RORγt inhibition
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December 2015 |
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Interactions among the transcription factors Runx1, RORγt and Foxp3 regulate the differentiation of interleukin 17–producing T cells
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October 2008 |
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Runx3 specifies lineage commitment of innate lymphoid cells
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September 2015 |
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Itch inhibits IL-17-mediated colon inflammation and tumorigenesis by ROR-γt ubiquitination
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June 2016 |
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A two-amino-acid substitution in the transcription factor RORγt disrupts its function in TH17 differentiation but not in thymocyte development
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August 2017 |
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ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer
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March 2016 |
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27-Hydroxycholesterol is an endogenous SERM that inhibits the cardiovascular effects of estrogen
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September 2007 |
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The interplay between cell signalling and the mevalonate pathway in cancer
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August 2016 |
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RHO–GTPases and cancer
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February 2002 |
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Principles for modulation of the nuclear receptor superfamily
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November 2004 |
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REV-ERB and ROR nuclear receptors as drug targets
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February 2014 |
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Nuclear receptor transrepression pathways that regulate inflammation in macrophages and T cells
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May 2010 |
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Controlling nuclear receptors: the circular logic of cofactor cycles
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July 2005 |
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Androgen synthesis in prostate cancer: do all roads lead to Rome?
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November 2016 |
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Liver X Receptor activation downregulates AKT survival signaling in lipid rafts and induces apoptosis of prostate cancer cells
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March 2010 |
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SREBP maintains lipid biosynthesis and viability of cancer cells under lipid- and oxygen-deprived conditions and defines a gene signature associated with poor survival in glioblastoma multiforme
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January 2015 |
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Abrogating cholesterol esterification suppresses growth and metastasis of pancreatic cancer
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May 2016 |
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A reciprocal feedback between the PDZ binding kinase and androgen receptor drives prostate cancer
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September 2018 |
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The cholesterol metabolite 27 hydroxycholesterol facilitates breast cancer metastasis through its actions on immune cells
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October 2017 |
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RORγ is a targetable master regulator of cholesterol biosynthesis in a cancer subtype
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October 2019 |
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RAS-targeted therapies: is the undruggable drugged?
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June 2020 |
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Liver X receptors in lipid signalling and membrane homeostasis
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June 2018 |
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Mechanisms and regulation of cholesterol homeostasis
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December 2019 |
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Bile acid metabolites control TH17 and Treg cell differentiation
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November 2019 |
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Microbial bile acid metabolites modulate gut RORγ+ regulatory T cell homeostasis
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December 2019 |
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Cholesterol metabolism in cancer: mechanisms and therapeutic opportunities
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February 2020 |
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The cholesterol biosynthesis enzyme oxidosqualene cyclase is a new target to impair tumour angiogenesis and metastasis dissemination
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March 2015 |
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Natural products as modulators of retinoic acid receptor-related orphan receptors (RORs)
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January 2021 |
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Expression of the Lipid Transporters ABCA3 and ABCA1 is Diminished in Human Breast Cancer Tissue
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November 2009 |
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Sterol-regulated transport of SREBPs from endoplasmic reticulum to Golgi: Oxysterols block transport by binding to Insig
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April 2007 |
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Aryl hydrocarbon receptor regulates Stat1 activation and participates in the development of Th17 cells
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July 2008 |
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Oxysterols are agonist ligands of ROR t and drive Th17 cell differentiation
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August 2014 |
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Identification of a tumor-promoter cholesterol metabolite in human breast cancers acting through the glucocorticoid receptor
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October 2017 |
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Cooperativity between the orthosteric and allosteric ligand binding sites of RORγt
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February 2021 |
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Protein Prenyltransferases
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March 1996 |
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Ursolic Acid Suppresses Interleukin-17 (IL-17) Production by Selectively Antagonizing the Function of RORγt Protein
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July 2011 |
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Modulation of Retinoic Acid Receptor-related Orphan Receptor α and γ Activity by 7-Oxygenated Sterol Ligands
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February 2010 |
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The E3 Deubiquitinase USP17 Is a Positive Regulator of Retinoic Acid-related Orphan Nuclear Receptor γt (RORγt) in Th17 Cells
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September 2014 |
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Structural studies unravel the active conformation of apo RORγt nuclear receptor and a common inverse agonism of two diverse classes of RORγt inhibitors
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May 2017 |
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Retinoic acid receptor-related orphan receptor gamma-t (RORγt) inhibitors in clinical development for the treatment of autoimmune diseases: a patent review (2016-present)
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August 2019 |
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A master regulator of cholesterol biosynthesis constitutes a therapeutic liability of triple negative breast cancer
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January 2020 |
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SIRT1 deacetylates RORγt and enhances Th17 cell generation
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April 2015 |
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Cholesterol uptake and regulation in high-grade and lethal prostate cancers
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June 2017 |
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RORγ directly regulates the circadian expression of clock genes and downstream targets in vivo
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June 2012 |
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Retinoid acid-related orphan receptor γ, RORγ, participates in diurnal transcriptional regulation of lipid metabolic genes
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August 2014 |
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Inhibition of interleukin-17, interleukin-23 and the TH17 cell pathway in the treatment of psoriatic arthritis and psoriasis
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January 2015 |
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The hepatic circadian clock fine-tunes the lipogenic response to feeding through RORα/γ
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June 2017 |
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Role of LXRs in control of lipogenesis
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November 2000 |
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A phase I randomized controlled trial to evaluate safety and clinical effect of topically applied GSK2981278 ointment in a psoriasis plaque test
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March 2018 |
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The role of transforming growth factor β in T helper 17 differentiation
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May 2018 |
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Cholesterol esters as growth regulators of lymphocytic leukaemia cells: Cholesterol esters and lymphocytic leukaemias
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June 2011 |
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Retinoic Acid-Related Orphan Receptors (RORs): Regulatory Functions in Immunity, Development, Circadian Rhythm, and Metabolism
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January 2015 |
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The Benzenesulfoamide T0901317 [ N -(2,2,2-Trifluoroethyl)- N -[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-α/γ Inverse Agonist
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November 2009 |
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Increasing Human Th17 Differentiation through Activation of Orphan Nuclear Receptor Retinoid Acid-Related Orphan Receptor γ (RORγ) by a Class of Aryl Amide Compounds
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June 2012 |
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Nuclear Receptors and Their Selective Pharmacologic Modulators
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February 2013 |
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GLK-IKKβ signaling induces dimerization and translocation of the AhR-RORγt complex in IL-17A induction and autoimmune disease
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September 2018 |
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Vitamin D Receptor As an Intestinal Bile Acid Sensor
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May 2002 |
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Lineage Relationship Analysis of RORγt + Innate Lymphoid Cells
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27-Hydroxycholesterol Links Hypercholesterolemia and Breast Cancer Pathophysiology
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Regulation of Absorption and ABC1-Mediated Efflux of Cholesterol by RXR Heterodimers
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Retrospective on Cholesterol Homeostasis: The Central Role of Scap
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(Inverse) Agonists of Retinoic Acid–Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease
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January 2020 |
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Cholesterol Sensing, Trafficking, and Esterification
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Cholesterol Sensitivity of Endogenous and Myristoylated Akt
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Dysregulation of Cholesterol Homeostasis in Human Prostate Cancer through Loss of ABCA1
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Cholesterol Metabolism and Prostate Cancer Lethality
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June 2016 |
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CYP27A1 Loss Dysregulates Cholesterol Homeostasis in Prostate Cancer
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January 2017 |
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The Effects of Cholesterol-Derived Oncometabolites on Nuclear Receptor Function in Cancer
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August 2018 |
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Inhibition of SOAT1 Suppresses Glioblastoma Growth via Blocking SREBP-1-Mediated Lipogenesis
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June 2016 |
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Therapeutic Targeting of MDR1 Expression by RORγ Antagonists Resensitizes Cross-Resistant CRPC to Taxane via Coordinated Induction of Cell Death Programs
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November 2019 |
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Cholesterol Esterification Inhibition Suppresses Prostate Cancer Metastasis by Impairing the Wnt/β-catenin Pathway
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Targeting C4-Demethylating Genes in the Cholesterol Pathway Sensitizes Cancer Cells to EGF Receptor Inhibitors via Increased EGF Receptor Degradation
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Studies on the Cholesterol-Free Mouse: Strong Activation of LXR-Regulated Hepatic Genes When Replacing Cholesterol With Desmosterol
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The LDL Receptor
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Cholesterol targeting alters lipid raft composition and cell survival in prostate cancer cells and xenografts
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Cholesterol and the risk of grade-specific prostate cancer incidence: evidence from two large prospective cohort studies with up to 37 years' follow up
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Frequent down-regulation of ABC transporter genes in prostate cancer
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Liver ChIP-seq analysis in FGF19-treated mice reveals SHP as a global transcriptional partner of SREBP-2
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11β-Hydroxysteroid dehydrogenases control access of 7β,27-dihydroxycholesterol to retinoid-related orphan receptor γ
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Lipid rafts as signaling hubs in cancer cell survival/death and invasion: implications in tumor progression and therapy
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May 2020 |
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Use of Statins and the Risk of Death in Patients With Prostate Cancer
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The Oxysterol, 27-Hydroxycholesterol, Links Cholesterol Metabolism to Bone Homeostasis Through Its Actions on the Estrogen and Liver X Receptors
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Retinoic Acid-Related Orphan Receptor γ (RORγ): A Novel Participant in the Diurnal Regulation of Hepatic Gluconeogenesis and Insulin Sensitivity
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Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin
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February 2016 |
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Innate lymphoid cells are pivotal actors in allergic, inflammatory and autoimmune diseases
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May 2015 |
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Retinoid-Related Orphan Receptors (RORs): Critical Roles in Development, Immunity, Circadian Rhythm, and Cellular Metabolism
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Retinoid-related orphan receptor regulates several genes that control metabolism in skeletal muscle cells: links to modulation of reactive oxygen species production
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The tumor suppressor TERE1 (UBIAD1) prenyltransferase regulates the elevated cholesterol phenotype in castration resistant prostate cancer by controlling a program of ligand dependent SXR target genes
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Elevated Levels of Cholesterol-Rich Lipid Rafts in Cancer Cells Are Correlated with Apoptosis Sensitivity Induced by Cholesterol-Depleting Agents
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Retinoic acid-related orphan receptors α and γ: key regulators of lipid/glucose metabolism, inflammation, and insulin sensitivity
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Targeting SREBP-2-Regulated Mevalonate Metabolism for Cancer Therapy
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August 2020 |
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The Mevalonate Pathway, a Metabolic Target in Cancer Therapy
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February 2021 |
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Digoxin, an Overlooked Agonist of RORγ/RORγT
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January 2019 |
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The Role of Gamma Delta T Cells in Autoimmune Rheumatic Diseases
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ABCG1 as a potential oncogene in lung cancer
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Role of liver X receptors in cholesterol efflux and inflammatory signaling (Review)
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Cutting Edge: Ubiquitin-Specific Protease 4 Promotes Th17 Cell Function under Inflammation by Deubiquitinating and Stabilizing RORγt
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Ubiquitination of RORγt at Lysine 446 Limits Th17 Differentiation by Controlling Coactivator Recruitment
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Regulation of Th17 Differentiation by IKKα-Dependent and -Independent Phosphorylation of RORγt
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June 2017 |
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The REV-ERBs and RORs: molecular links between circadian rhythms and lipid homeostasis
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April 2011 |