ROR nuclear receptors: structures, related diseases and drug discovery

Reduction in lipophilicity improved the solubility, plasma–protein binding, and permeability of tertiary sulfonamide RORc inverse agonists

(2014) Benjamin P. Fauber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of tertiary sulfonamides as RORc inverse agonists

(2014) Benjamin P. Fauber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Therapeutic Potential of Nuclear Receptor Modulators for Treatment of Metabolic Disorders: PPARγ, RORs, and Rev-erbs

(2014) David P. Marciano et al.   Cell Metabolism

Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation

(2014) Yan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors

(2013) Yonghui Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc

(2013) Benjamin P. Fauber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

Computational methods for drug design and discovery: focus on China

(2013) Mingyue Zheng et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists

(2013) Ting Yang et al.   ACS Medicinal Chemistry Letters

Pharmacologic Repression of Retinoic Acid Receptor-Related Orphan Nuclear Receptor γ Is Therapeutic in the Collagen-Induced Arthritis Experimental Model

(2013) Mi Ra Chang et al.   Arthritis & Rheumatology

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

Computational drug discovery

(2012) Si-sheng Ou-Yang et al.   ACTA PHARMACOLOGICA SINICA

Revealing a natural marine product as a novel agonist for retinoic acid receptors with a unique binding mode and inhibitory effects on cancer cells

(2012) Shanshan Wang et al.   BIOCHEMICAL JOURNAL

Discovery of new non-steroidal FXR ligands via a virtual screening workflow based on Phase shape and induced fit docking

(2012) Jing Fu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small molecule amides as potent ROR-γ selective modulators

(2012) Pasha M. Khan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting Orphan Nuclear Receptors for Treatment of Metabolic Diseases and Autoimmunity

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

Discovery and structure–activity analysis of selective estrogen receptor modulators via similarity-based virtual screening

(2012) Jie Shen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

RORα, a Potential Tumor Suppressor and Therapeutic Target of Breast Cancer

(2012) Jun Du et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Discovery and Optimization of 1,3,4-Trisubstituted-pyrazolone Derivatives as Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonists

(2012) Huang Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regulation of p53 Stability and Apoptosis by a ROR Agonist

(2012) Yongjun Wang et al.   PLoS One

Action of RORs and their ligands in (patho)physiology

(2012) Laura A. Solt et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors

(2012) Jun R. Huh et al.   ACS Medicinal Chemistry Letters

Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor α/δ Agonist

(2011) Lihua Jin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Identification and Mechanism of 10-Carbon Fatty Acid as Modulating Ligand of Peroxisome Proliferator-activated Receptors

(2011) Raghu R. V. Malapaka 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

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

(2010) Yongjun Wang et al.   ACS Chemical Biology

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

(2010) Naresh Kumar et al.   ACS Chemical Biology

Development and Validation of a Cell-Based Assay for the Nuclear Receptor Retinoid-Related Orphan Receptor Gamma

(2010) Jennifer Wilkinson et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

The Orphan Nuclear Receptor TR4 Is a Vitamin A-activated Nuclear Receptor

(2010) X. Edward Zhou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Potent Ligands for Estrogen Receptor β by Structure-Based Virtual Screening

(2010) Jie Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2010) Lihua Jin et al.   MOLECULAR ENDOCRINOLOGY

IL-17 and Th17 Cells

(2009) Thomas Korn et al.   Annual Review of Immunology

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

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

(2008) Xuexian O. Yang et al.   IMMUNITY

Th17 cells in human disease

(2008) Laura A. Tesmer et al.   IMMUNOLOGICAL REVIEWS

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

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

Adopting New Orphans into the Family of Metabolic Regulators

(2008) Sarah Hummasti et al.   MOLECULAR ENDOCRINOLOGY

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

(2008) Thomas P. Burris   MOLECULAR ENDOCRINOLOGY

The differentiation of human TH-17 cells requires transforming growth factor-β and induction of the nuclear receptor RORγt

(2008) Nicolas Manel et al.   NATURE IMMUNOLOGY

Absence of the SRC-2 Coactivator Results in a Glycogenopathy Resembling Von Gierke's Disease

(2008) A. R. Chopra et al.   SCIENCE

Chromatin- and Transcription-Related Factors Repress Transcription from within Coding Regions throughout the Saccharomyces cerevisiae Genome

(2008) Vanessa Cheung et al.   PLOS BIOLOGY