Advances in drug design with RXR modulators

Structural basis for a molecular allosteric control mechanism of cofactor binding to nuclear receptors

(2012) J. Osz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis for negative cooperativity within agonist-bound TR:RXR heterodimers

(2012) B.-D. K. Putcha et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

ApoE-Directed Therapeutics Rapidly Clear  -Amyloid and Reverse Deficits in AD Mouse Models

(2012) P. E. Cramer et al.   SCIENCE

RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists

(2012) Hiroki Kakuta et al.   ACS Medicinal Chemistry Letters

Intranasal Insulin Therapy for Alzheimer Disease and Amnestic Mild Cognitive Impairment

(2011) Suzanne Craft   ARCHIVES OF NEUROLOGY

Modulation of RXR function through ligand design

(2011) Efrén Pérez et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

The retinoid X receptors and their ligands

(2011) Marcia I. Dawson et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Replacement of the hydrophobic part of 9-cis-retinoic acid with cyclic terpenoid moiety results in RXR-selective agonistic activity

(2011) Takashi Okitsu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Diphenylamine-based retinoid antagonists: Regulation of RAR and RXR function depending on the N-substituent

(2011) Kiminori Ohta et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel Silicon-Containing Analogues of the Retinoid Agonist Bexarotene: Syntheses and Biological Effects on Human Pluripotent Stem Cells

(2011) Jennifer B. Bauer et al.   ChemMedChem

Structural Basis for Retinoic X Receptor Repression on the Tetramer

(2011) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure Basis of Bigelovin as a Selective RXR Agonist with a Distinct Binding Mode

(2011) Haitao Zhang et al.   JOURNAL OF MOLECULAR BIOLOGY

Common architecture of nuclear receptor heterodimers on DNA direct repeat elements with different spacings

(2011) Natacha Rochel et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB

(2011) Mariko Nakayama et al.   ACS Medicinal Chemistry Letters

The eccentric cleavage product of β-carotene, β-apo-13-carotenone, functions as an antagonist of RXRα

(2010) Abdulkerim Eroglu et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Modification at the acidic domain of RXR agonists has little effect on permissive RXR-heterodimer activation

(2010) Shuji Fujii et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

NSAID Sulindac and Its Analog Bind RXRα and Inhibit RXRα-Dependent AKT Signaling

(2010) Hu Zhou et al.   CANCER CELL

A Pilot, First-in-Human, Pharmacokinetic Study of 9cUAB30 in Healthy Volunteers

(2010) J. M. Kolesar et al.   Cancer Prevention Research

Retinoic acid receptor modulators: a perspective on recent advances and promises

(2010) Susana Álvarez et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Murine Oncogenicity and Pharmacokinetics Studies of 9-cis-UAB30, an RXR Agonist, for Breast Cancer Chemoprevention

(2010) Izet M. Kapetanovic et al.   INTERNATIONAL JOURNAL OF TOXICOLOGY

Danthron Functions as a Retinoic X Receptor Antagonist by Stabilizing Tetramers of the Receptor

(2010) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of a Naturally Occurring Rexinoid, Honokiol, That Activates the Retinoid X Receptor

(2010) Hitoshi Kotani et al.   JOURNAL OF NATURAL PRODUCTS

A unique secondary-structure switch controls constitutive gene repression by retinoic acid receptor

(2010) Albane le Maire et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The “Phantom Effect” of the Rexinoid LG100754: Structural and Functional Insights

(2010) Yoshiteru Sato et al.   PLoS One

Retinoid X receptors: common heterodimerization partners with distinct functions

(2010) Philippe Lefebvre et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers

(2010) Fuminori Ohsawa et al.   ACS Medicinal Chemistry Letters

Pyrazine Arotinoids with Inverse Agonist Activities on the Retinoid and Rexinoid Receptors

(2009) José García et al.   CHEMBIOCHEM

Silicon Analogues of the RXR-Selective Retinoid Agonist SR11237 (BMS649): Chemistry and Biology

(2009) W. Peter Lippert et al.   ChemMedChem

Derivation of a Retinoid X Receptor Scaffold from Peroxisome Proliferator-Activated Receptor γ Ligand 1-Di(1H-indol-3-yl)methyl-4-trifluoromethylbenzene

(2009) Marcia I. Dawson et al.   ChemMedChem

Activation of RXR–PPAR heterodimers by organotin environmental endocrine disruptors

(2009) Albane le Maire et al.   EMBO REPORTS

Highly twisted adamantyl arotinoids: Synthesis, antiproliferative effects and RXR transactivation profiles

(2009) Santiago Pérez-Rodríguez et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Modulating Retinoid X Receptor with a Series of (E)-3-[4-Hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic Acids and Their 4-Alkoxy Isomers†

(2009) Efrén Pérez Santín et al.   JOURNAL OF MEDICINAL CHEMISTRY

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)

(2009) Carl E. Wagner et al.   JOURNAL OF MEDICINAL CHEMISTRY

The effect of antagonists on the conformational exchange of the retinoid X receptor alpha ligand-binding domain

(2009) Jianyun Lu et al.   MAGNETIC RESONANCE IN CHEMISTRY

Activation of Retinoic Acid Receptors by Dihydroretinoids

(2009) A. R. Moise et al.   MOLECULAR PHARMACOLOGY

New retinoid chemotypes: 9-cis-Retinoic acid analogs with hydrophobic rings derived from terpenes as selective RAR agonists

(2008) Susana Álvarez et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Replacing alkyl sulfonamide with aromatic sulfonamide in sulfonamide-type RXR agonists favors switch towards antagonist activity

(2008) Ken-ichi Morishita et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The First Potent Subtype-Selective Retinoid X Receptor (RXR) Agonist Possessing a 3-Isopropoxy-4-isopropylphenylamino Moiety, NEt-3IP (RXRα/β-dual agonist)

(2008) Kayo Takamatsu et al.   ChemMedChem

A Phase I Study of Docetaxel and Bexarotene

(2008) Jonathan D. Wildi et al.   CHEMOTHERAPY

Phase III Trial Comparing Carboplatin, Paclitaxel, and Bexarotene With Carboplatin and Paclitaxel in Chemotherapy-Naïve Patients With Advanced or Metastatic Non–Small-Cell Lung Cancer: SPIRIT II

(2008) George R. Blumenschein et al.   JOURNAL OF CLINICAL ONCOLOGY

Randomized Phase III Trial Comparing Bexarotene (L1069-49)/Cisplatin/Vinorelbine With Cisplatin/Vinorelbine in Chemotherapy-Naïve Patients With Advanced or Metastatic Non–Small-Cell Lung Cancer: SPIRIT I

(2008) Rodryg Ramlau et al.   JOURNAL OF CLINICAL ONCOLOGY

Assessment of Scaffold Hopping Efficiency by Use of Molecular Interaction Fingerprints

(2008) Jennifer Venhorst et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the intact PPAR-γ–RXR-α nuclear receptor complex on DNA

(2008) Vikas Chandra et al.   NATURE

Reduction of Lipophilicity at the Lipophilic Domain of RXR Agonists Enables Production of Subtype Preference: RXRα-Preferential Agonist Possessing a Sulfonamide Moiety

(2007) Kayo Takamatsu et al.   ChemMedChem