138 articles for thisTarget
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Virtual screening and experimental validation identify novel modulators of nuclear receptor RXRa from Drugbank database.
Xiamen University
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists.
Galderma R & D
Binding characterization, synthesis and biological evaluation of RXRa antagonists targeting the coactivator binding site.
Xiamen University
Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.
University of Gothenburg
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers.
University of Alabama At Birmingham
Positron emission tomography to elucidate pharmacokinetic differences of regioisomeric retinoid x receptor agonists.
Okayama University Graduate School of Medicine
Rexinoids isolated from Sophora tonkinensis with a gene expression profile distinct from the synthetic rexinoid bexarotene.
Aichi Gakuin University
Small molecule inhibitors targeting activator protein 1 (AP-1).
University of Texas Medical Branch
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity.
University of Alabama At Birmingham
Synthesis and SAR study of modulators inhibiting tRXRa-dependent AKT activation.
Xiamen University
Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency.
Okayama University Graduate School of Medicine
Design, synthesis, and biological evaluation of indenoisoquinoline rexinoids with chemopreventive potential.
Purdue University
Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.
Acadia Pharmaceuticals
Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventive agents.
The University of Illinois At Chicago
RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists.
TBA
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers.
TBA
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
Fluorescent retinoid X receptor ligands for fluorescence polarization assay.
Okayama University
Modification at the acidic domain of RXR agonists has little effect on permissive RXR-heterodimer activation.
Okayama University
Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor.
Aichi Gakuin University
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).
Arizona State University
Identification of a chromone-based retinoid containing a polyolefinic side chain via facile synthetic routes.
Temple University
Synthesis and structure-activity relationships of potent conformationally restricted retinoid X receptor ligands
TBA
Synthesis and biological activity of 1,2,3,4-tetrahydroquinoline and 3,4-(1H)-dihydroquinolin-2-one analogs of retinoic acid
TBA
Synthesis and receptor binding affinity of conformationally restricted retinoic acid analogues
TBA
Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere
TBA
Synthesis and pharmacological activity of conformationally restricted, acetylenic retinoid analogs
TBA
Differential RXR & RAR activity of stilbene retinoid analogs bearing thiazole and imidazole carboxylic acids
TBA
N-linked analogs of retinoid O-glucuronides: potential cancer chemopreventive/chemotherapeutic agents
TBA
Replacing alkyl sulfonamide with aromatic sulfonamide in sulfonamide-type RXR agonists favors switch towards antagonist activity.
Okayama University Graduate School of Medicine
Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
University of Lille
Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.
Tsukuba Research Institute
Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.
Tsukuba Research Institute
Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.
Johnson and Johnson Pharmaceutical Research and Development
RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.
Johnson and Johnson Pharmaceutical Research and Development
Ligand Screening System for the RXR? Heterodimer Using the Fluorescence RXR Agonist CU-6PMN.
University of Shizuoka
Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia.
Shaanxi University of Science & Technology
Targeting Nuclear Receptors in Neurodegeneration and Neuroinflammation.
Goethe University Frankfurt
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus,
Seoul National University
Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers.
TBA
Ligand recognition by RAR and RXR receptors: binding and selectivity.
Universidad De Santiago De Compostela
Synthesis and structure-activity relationships of a new series of retinoid-related biphenyl-4-ylacrylic acids endowed with antiproliferative and proapoptotic activity.
Università
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
University of Maryland
Increased Molecular Flexibility Widens the Gap between
Okayama University Graduate School of Medicine
Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.
Goethe-University Frankfurt
Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Ligand Pharmaceuticals
Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Ligand Pharmaceuticals
Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Ligand Pharmaceuticals
Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343.
Okayama University Graduate School of Medicine
Discovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.
Okayama University Graduate School of Medicine
Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Ligand Pharmaceuticals
Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.
Ligand Pharmaceuticals
Synthesis and biological activity of retinoic acid receptor-alpha specific amides.
Allergan
Creation of Fluorescent RXR Antagonists Based on CBTF-EE and Application to a Fluorescence Polarization Binding Assay.
Okayama University Graduate School of Medicine
Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.
Universidade De Vigo
An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide.
The Ohio State University
Discovery of 3?,7?,11?-Trihydroxy-6?-ethyl-5?-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?.
Goethe-University Frankfurt
Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes.
Allergan
An unhydrolyzable analogue of N-(4-hydroxyphenyl)retinamide. synthesis and preliminary biological studies.
The Ohio State University
Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor alpha antagonists.
Eisai
Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Allergan
3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity.
Okayama University Graduate School of Medicine
Design, synthesis and biological evaluation of tetrazole-containing RXR? ligands as anticancer agents.
Xiamen University
Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.
Eisai
Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.
Eisai
Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening.
Okayama University Graduate School of Medicine
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Goethe University Frankfurt
Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.
Eisai
Structure-activity relationship studies of novel heteroretinoids: induction of apoptosis in the HL-60 cell line by a novel isoxazole-containing heteroretinoid.
Università
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
Heteroarotinoids inhibit head and neck cancer cell lines in vitro and in vivo through both RAR and RXR retinoic acid receptors.
University of Oklahoma Health Sciences Center
Discovery and lead optimisation of a potent, selective and orally bioavailable RAR? agonist for the potential treatment of nerve injury.
King'S College
Synthesis, structure-activity relationships, and RARgamma-ligand interactions of nitrogen heteroarotinoids.
University of Oklahoma Health Sciences Center
A new class of potent RAR antagonists: dihydroanthracenyl, benzochromenyl and benzothiochromenyl retinoids.
Allergan
Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.
Allergan
Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.
Ligand Pharmaceuticals
Synthesis and characterization of heteroarotinoids demonstrate structure specificity relationships.
University of Oklahoma Health Sciences Center
Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype.
Goethe-University Frankfurt
Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.
University of Tokyo
Cytotoxic Components from Hypericum elodeoides Targeting RXR? and Inducing HeLa Cell Apoptosis through Caspase-8 Activation and PARP Cleavage.
Xiamen University
Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure-activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity.
University of Alabama At Birmingham
Synthesis and structure-activity relationships of retinoid X receptor selective diaryl sulfide analogs of retinoic acid.
Allergan
A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.
Goethe-University Frankfurt
Identification of the first retinoid X, receptor homodimer antagonist.
Ligand Pharmaceuticals
Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells.
Ligand Pharmaceuticals
Retinoic acid receptor beta,gamma-selective ligands: synthesis and biological activity of 6-substituted 2-naphthoic acid retinoids.
Pharmaceutical Research Institute
Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.
Ume£
Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Cird Galderma
Identification of a New RXR? Antagonist Targeting the Coregulator-Binding Site.
Xiamen University
Conformational effects on retinoid receptor selectivity. 1. Effect of 9-double bond geometry on retinoid X receptor activity.
Sri International
Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties.
Ligand Pharmaceuticals
Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids.
Ligand Pharmaceuticals
Discovery of a small molecular compound simultaneously targeting RXR and HADC: design, synthesis, molecular docking and bioassay.
Shenyang Pharmaceutical University
Conformational effects on retinoid receptor selectivity. 2. Effects of retinoid bridging group on retinoid X receptor activity and selectivity.
Sri International
Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells.
Ligand Pharmaceuticals
Synthesis and structure-activity relationships of stilbene retinoid analogs substituted with heteroaromatic carboxylic acids.
Allergan
Conformationally defined 6-s-trans-retinoic acid analogs. 2. Selective agonists for nuclear receptor binding and transcriptional activity.
University of Alabama At Birmingham
Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors.
Allergan
Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Acadia Pharmaceuticals
Identification of highly potent retinoic acid receptor alpha-selective antagonists.
Allergan
Probing biological activity through structural modelling of ligand-receptor interactions of 2,4-disubstituted thiazole retinoids.
Helwan University
Structure-based design of Trifarotene (CD5789), a potent and selective RAR? agonist for the treatment of acne.
Nestle Skin Health
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.
King'S College
Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics.
Swiss Federal Institute of Technology (Eth)
Indazole-based ligands for estrogen-related receptor ? as potential anti-diabetic agents.
Janssen Research and Development
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
