Ternary complex of human RORγ ligand-binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment

Re-emergence of an orphan therapeutic target for the treatment of resistant prostate cancer – a thorough conformational and binding analysis for ROR-γ protein

(2017) Umar Ndagi et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer

(2016) Junjian Wang et al.   NATURE MEDICINE

Structural determinant for inducing RORgamma specific inverse agonism triggered by a synthetic benzoxazinone ligand

(2016) Douglas J. Marcotte et al.   BMC STRUCTURAL BIOLOGY

Discovery of 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide analogs as new RORC modulators

(2015) Ingo Muegge et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel pyrazole-containing benzamides as potent RORγ inverse agonists

(2015) Tao Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of biaryl carboxylamides as potent RORγ inverse agonists

(2015) Jianhua Chao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of Natural RORγ Ligands that Regulate the Development of Lymphoid Cells

(2015) Fabio R. Santori et al.   Cell Metabolism

Benzoxazepines Achieve Potent Suppression of IL-17 Release in Human T-Helper 17 (TH17) Cells through an Induced-Fit Binding Mode to the Nuclear Receptor RORγ

(2015) Roine I. Olsson et al.   ChemMedChem

Comparison of ixekizumab with etanercept or placebo in moderate-to-severe psoriasis (UNCOVER-2 and UNCOVER-3): results from two phase 3 randomised trials

(2015) Christopher E M Griffiths et al.   LANCET

Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors

(2015) Yonghui Wang et al.   ACS Medicinal Chemistry Letters

SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor

(2015) Kazuyuki Hirata et al.   ACS Medicinal Chemistry Letters

Identification of an allosteric binding site for RORγt inhibition

(2015) Marcel Scheepstra et al.   Nature Communications

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

Secukinumab in Plaque Psoriasis — Results of Two Phase 3 Trials

(2014) Richard G. Langley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action

(2014) Olivier René et al.   ACS Medicinal Chemistry Letters

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

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

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

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

(2011) Jun R. Huh et al.   NATURE

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

(2010) Lihua Jin et al.   MOLECULAR ENDOCRINOLOGY

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

Localized thermodynamic coupling between hydrogen bonding and microenvironment polarity substantially stabilizes proteins

(2009) Jianmin Gao et al.   NATURE STRUCTURAL & MOLECULAR 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