106 articles for thisTarget
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Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
Vitae Pharmaceuticals
Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency andß-selectivity of liver X receptor agonist.
Kowa
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.
Vitae Pharmaceuticals
Identification and in Vivo Evaluation of Liver X Receptorß-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Wuxi Apptec
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
The University of Tokyo
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
The University of Tokyo
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.
Daiichi Sankyo Rd Novare
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptorß-selective agonists.
Kowa
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
Genentech
Design and discovery of 2-oxochromene derivatives as liver X receptorß-selective agonists.
Kowa
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Genentech
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).
Genentech
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRß.
Bristol-Myers Squibb
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
The University of Tokyo
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Genentech
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
Korea University
Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages.
Korea University
Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.
New York University School of Medicine
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Glaxosmithkline
Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.
Korea University
Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.
The University of Tokyo
Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.
Johnson & Johnson Pharmaceutical Research and Development
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
Wyeth Pharmaceuticals
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Merck Research Laboratories
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.
Wyeth Pharmaceuticals
Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.
Wyeth Pharmaceuticals
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
Wyeth Pharmaceuticals
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
Wyeth Pharmaceuticals
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
Wyeth Pharmaceuticals
The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.
Glaxosmithkline
Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.
The University of Tokyo
Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.
Wyeth Research
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
Astrazeneca R&D SöDertäLje
Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
Glaxosmithkline
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
Merck Research Laboratories
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
Merck Research Laboratories
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
Merck Research Laboratories
Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.
Wyeth Pharmaceuticals
Discovery of Anti-Hypercholesterolemia Agents Targeting LXRα from Marine Microorganism-Derived Natural Products.
Guangxi University of Chinese Medicine
Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors.
University of Tokyo
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Guangdong Pharmaceutical University
Discovery of Spiro[pyrrolidine-3,3'-oxindole] LXRβ Agonists for the Treatment of Osteoporosis.
Sun Yat-Sen University
Emerging targets and potential therapeutic agents in non-alcoholic fatty liver disease treatment.
Sichuan University
Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist.
Guangzhou Medical University
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
F. Hoffmann-La Roche
Design, synthesis and structure-activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists.
Tokyo Medical and Dental University
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis.
Merck Research Laboratories
LXR-Mediated Regulation of Marine-Derived Piericidins Aggravates High-Cholesterol Diet-Induced Cholesterol Metabolism Disorder in Mice.
Southern Medical University
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Bristol Myers Squibb
Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
Sun Yat-Sen University
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.
Bristol Myers Squibb
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Bristol Myers Squibb
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357.
Boehringer Ingelheim Pharmaceuticals
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Bristol Myers Squibb
Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus
Chinese Academy of Sciences
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Goethe University Frankfurt
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
Chinese Academy of Sciences
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.
Bristol-Myers Squibb
Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold.
Benha University
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
Bristol-Myers Squibb
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003.
Shionogi
Recent Advances in the Medicinal Chemistry of Liver X Receptors.
Saint Louis University School of Medicine
Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
The University of Tokyo
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.
The University of Tokyo
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
Janssen Research and Development
DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
Goethe-University Frankfurt
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
University of Perugia
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Heterocyclic-imidazole compounds, pharmaceutical compositions thereof, preparation method therefor and use thereof
Shanghai Huilun Life Science & Technology
Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones
Janssen Ireland
Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
Merck Sharp & Dohme
Multimodal Recognition of Diverse Peptides by the C-Terminal SH2 Domain of Phospholipase C-¿1 Protein.
University of Colorado Boulder
Indoline scaffold SHP-2 inhibitors and cancer treatment method
University of South Florida
Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Merck Research Laboratories
The identification of a novel natural activator of p300 histone acetyltranferase provides new insights into the modulation mechanism of this enzyme.
Universitá
Molecular docking and ligand specificity in fragment-based inhibitor discovery.
University of California San Francisco
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.
Emory University
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives.
Sapienza University of Rome
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
National Institutes of Health
Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.
Probiodrug