REV-ERB and ROR nuclear receptors as drug targets

Optimized Chemical Probes for REV-ERBα

(2013) Ryan P. Trump et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rev-Erbs repress macrophage gene expression by inhibiting enhancer-directed transcription

(2013) Michael T. Y. Lam et al.   NATURE

Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy

(2013) Estelle Woldt et al.   NATURE MEDICINE

Metabolism and the Circadian Clock Converge

(2013) Kristin Eckel-Mahan et al.   PHYSIOLOGICAL REVIEWS

Ursolic Acid Inhibits Adipogenesis in 3T3-L1 Adipocytes through LKB1/AMPK Pathway

(2013) Yonghan He et al.   PLoS One

Impact of insufficient sleep on total daily energy expenditure, food intake, and weight gain

(2013) R. R. Markwald et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

TH17 Cell Differentiation Is Regulated by the Circadian Clock

(2013) X. Yu et al.   SCIENCE

Increased Atherosclerotic Lesions in LDL Receptor Deficient Mice With Hematopoietic Nuclear Receptor Rev‐erbα Knock‐ Down

(2013) Hongling Ma et al.   Journal of the American Heart Association

Retinoic acid-related orphan receptors α and γ: key regulators of lipid/glucose metabolism, inflammation, and insulin sensitivity

(2013) Anton M. Jetten et al.   Frontiers in Endocrinology

Identification of a Selective RORγ Ligand That Suppresses TH17 Cells and Stimulates T Regulatory Cells

(2012) Laura A. Solt et al.   ACS Chemical Biology

Identification of SR2211: A Potent Synthetic RORγ-Selective Modulator

(2012) Naresh Kumar et al.   ACS Chemical Biology

Central and Peripheral Circadian Clocks in Mammals

(2012) Jennifer A. Mohawk et al.   Annual Review of Neuroscience

N-methylthioureas as new agonists of retinoic acid receptor-related orphan receptor

(2012) Yohan Park et al.   ARCHIVES OF PHARMACAL RESEARCH

Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists

(2012) Romain Noel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα

(2012) Youseung Shin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ursolic acid promotes the neuroprotection by activating Nrf2 pathway after cerebral ischemia in mice

(2012) Litao Li et al.   BRAIN RESEARCH

Targeting Orphan Nuclear Receptors for Treatment of Metabolic Diseases and Autoimmunity

(2012) Thomas P. Burris et al.   CHEMISTRY & BIOLOGY

The nuclear receptor REV-ERBα is required for the daily balance of carbohydrate and lipid metabolism

(2012) Julien Delezie et al.   FASEB JOURNAL

Role of Rev-erbα domains for transactivation of the connexin43 promoter with Sp1

(2012) Hiromitsu Negoro et al.   FEBS LETTERS

Shift Work and the Risk of Metabolic Syndrome: A Nested Case-Control Study

(2012) Ying Li et al.   INTERNATIONAL JOURNAL OF OCCUPATIONAL AND ENVIRONMENTAL HEALTH

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists

(2012) Laura A. Solt et al.   NATURE

Regulation of circadian behaviour and metabolism by REV-ERB-α and REV-ERB-β

(2012) Han Cho et al.   NATURE

Circadian topology of metabolism

(2012) Joseph Bass   NATURE

RORγ directly regulates the circadian expression of clock genes and downstream targets in vivo

(2012) Yukimasa Takeda et al.   NUCLEIC ACIDS RESEARCH

Regulation of p53 Stability and Apoptosis by a ROR Agonist

(2012) Yongjun Wang et al.   PLoS One

A Role for Rev-erbα Ligands in the Regulation of Adipogenesis

(2011) Douglas J. Kojetin et al.   CURRENT PHARMACEUTICAL DESIGN

Homozygous staggerer (sg/sg) mice display improved insulin sensitivity and enhanced glucose uptake in skeletal muscle

(2011) P. Lau et al.   DIABETOLOGIA

Adipogenesis and insulin sensitivity in obesity are regulated by retinoid-related orphan receptor gamma

(2011) Bettina Meissburger et al.   EMBO Molecular Medicine

The Clock GeneRev-erbα Regulates Pancreatic β-Cell Function: Modulation by Leptin and High-Fat Diet

(2011) Elaine Vieira et al.   ENDOCRINOLOGY

Digoxin — Time to take the gloves off?

(2011) Emma Eade et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Ursolic Acid Suppresses Interleukin-17 (IL-17) Production by Selectively Antagonizing the Function of RORγt Protein

(2011) Tao Xu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis of Digoxin That Antagonizes RORγt Receptor Activity and Suppresses Th17 Cell Differentiation and Interleukin (IL)-17 Production

(2011) Saori Fujita-Sato et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Digoxin and its derivatives suppress TH17 cell differentiation by antagonizing RORγt activity

(2011) Jun R. Huh et al.   NATURE

Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand

(2011) Laura A. Solt et al.   NATURE

Role of Sleep Timing in Caloric Intake and BMI

(2011) Kelly G. Baron et al.   Obesity

The nuclear receptor REV-ERB  mediates circadian regulation of innate immunity through selective regulation of inflammatory cytokines

(2011) J. E. Gibbs et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Circadian Rhythm Orchestrated by Histone Deacetylase 3 Controls Hepatic Lipid Metabolism

(2011) D. Feng et al.   SCIENCE

GSK4112, a Small Molecule Chemical Probe for the Cell Biology of the Nuclear Heme Receptor Rev-erbα

(2010) Daniel Grant et al.   ACS Chemical Biology

Identification of SR1078, a Synthetic Agonist for the Orphan Nuclear Receptors RORα and RORγ

(2010) Yongjun Wang et al.   ACS Chemical Biology

Identification of SR8278, a Synthetic Antagonist of the Nuclear Heme Receptor REV-ERB

(2010) Douglas Kojetin et al.   ACS Chemical Biology

Identification of SR3335 (ML-176): A Synthetic RORα Selective Inverse Agonist

(2010) Naresh Kumar et al.   ACS Chemical Biology

A second class of nuclear receptors for oxysterols: Regulation of RORα and RORγ activity by 24S-hydroxycholesterol (cerebrosterol)

(2010) Yongjun Wang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Regulation of Adipogenesis by Natural and Synthetic REV-ERB Ligands

(2010) Naresh Kumar et al.   ENDOCRINOLOGY

The mammalian clock component PERIOD2 coordinates circadian output by interaction with nuclear receptors

(2010) I. Schmutz et al.   GENES & DEVELOPMENT

Thiol-disulfide Redox Dependence of Heme Binding and Heme Ligand Switching in Nuclear Hormone Receptor Rev-erbβ

(2010) Nirupama Gupta et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Regulation of FGF21 Expression and Secretion by Retinoic Acid Receptor-related Orphan Receptor α

(2010) Yongjun Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Hydroxycholesterols as Natural Ligands of Orphan Nuclear Receptor RORγ

(2010) Lihua Jin et al.   MOLECULAR ENDOCRINOLOGY

Structure of Rev-erbα bound to N-CoR reveals a unique mechanism of nuclear receptor–co-repressor interaction

(2010) Caroline A Phelan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Circadian Integration of Metabolism and Energetics

(2010) J. Bass et al.   SCIENCE

Nuclear ReceptorsHomo sapiensRev-erbβ andDrosophila melanogasterE75 Are Thiolate-Ligated Heme Proteins Which Undergo Redox-Mediated Ligand Switching and Bind CO and NO

(2009) Katherine A. Marvin et al.   BIOCHEMISTRY

Negative feedback maintenance of heme homeostasis by its receptor, Rev-erb 

(2009) N. Wu et al.   GENES & DEVELOPMENT

Th17 cytokines and their emerging roles in inflammation and autoimmunity

(2009) Lynette A. Fouser et al.   IMMUNOLOGICAL REVIEWS

Rev-erb-α: an integrator of circadian rhythms and metabolism

(2009) Hélène Duez et al.   JOURNAL OF APPLIED PHYSIOLOGY

Modulation of Retinoic Acid Receptor-related Orphan Receptor α and γ Activity by 7-Oxygenated Sterol Ligands

(2009) Yongjun Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Liver X receptor agonist regulation of Th17 lymphocyte function in autoimmunity

(2009) Jihong Xu et al.   JOURNAL OF LEUKOCYTE BIOLOGY

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- /  Inverse Agonist

(2009) N. Kumar et al.   MOLECULAR PHARMACOLOGY

PGC-1α negatively regulates hepatic FGF21 expression by modulating the heme/Rev-Erbα axis

(2009) Jennifer L. Estall et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Adverse metabolic and cardiovascular consequences of circadian misalignment

(2009) F. A. J. L. Scheer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Structural Basis of Gas-Responsive Transcription by the Human Nuclear Hormone Receptor REV-ERBβ

(2009) Keith I Pardee et al.   PLOS BIOLOGY

Relationship between circadian oscillations of Rev-erbα expression and intracellular levels of its ligand, heme

(2008) Pamela M. Rogers et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The Meter of Metabolism

(2008) Carla B. Green et al.   CELL

T Helper 17 Lineage Differentiation Is Programmed by Orphan Nuclear Receptors RORα and RORγ

(2008) Xuexian O. Yang et al.   IMMUNITY

The Orphan Nuclear Receptor, RORα, Regulates Gene Expression That Controls Lipid Metabolism

(2008) Patrick Lau et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ligand modulation of REV-ERB  function resets the peripheral circadian clock in a phasic manner

(2008) Q. J. Meng et al.   JOURNAL OF CELL SCIENCE

Bifunctional Role of Rev-erb  in Adipocyte Differentiation

(2008) J. Wang et al.   MOLECULAR AND CELLULAR BIOLOGY

Nuclear Hormone Receptors for Heme: REV-ERBα and REV-ERBβ Are Ligand-Regulated Components of the Mammalian Clock

(2008) Thomas P. Burris   MOLECULAR ENDOCRINOLOGY