139 articles for thisTarget
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Article Title
Organization
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.
Goethe-University Frankfurt
Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists.
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists.
Hiroshima International University
Novel FXR (farnesoid X receptor) modulators: Potential therapies for cholesterol gallstone disease.
Beckman Research Institute
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.
Phenex Pharmaceuticals
Novel approaches to map small molecule-target interactions.
Max Planck Institute of Molecular Physiology
The Halicylindramides, Farnesoid X Receptor Antagonizing Depsipeptides from a Petrosia sp. Marine Sponge Collected in Korea.
Daegu-Gyeongbuk Medical Innovation Foundation
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist.
Zydus Research Centre
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
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists.
East China University of Science and Technology
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Anthranilic acid derivatives as nuclear receptor modulators--development of novel PPAR selective and dual PPAR/FXR ligands.
Goethe-University Frankfurt
Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.
Goethe-University Frankfurt
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
Genentech
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
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.
Glaxosmithkline
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist.
Goethe-University Frankfurt
Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands.
University of Naples&Quot;Federico Ii&Quot
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor.
Beckman Research Institute
Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR).
Goethe-University Frankfurt
Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.
Istituto Italiano Di Tecnologia
Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists.
East China University of Science and Technology
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Genentech
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
City of Hope National Medical Center
Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: role of the chirality on the biological activity.
Universit£
Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands.
Istituto Italiano Di Tecnologia
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Pfizer
Discovery of new non-steroidal FXR ligands via a virtual screening workflow based on Phase shape and induced fit docking.
East China University of Science and Technology
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists.
Universit£
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity.
The University of Tokyo
Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus.
Seoul National University
Diversity-oriented synthesis: exploring the intersections between chemistry and biology.
Memorial Sloan-Kettering Cancer Center
Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.
Universite Louis Pasteur
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
Universita Di Perugia
Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation.
Graduate School of The Chinese Academy of Sciences
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
Centre National de la Recherche Scientifique/INSERM/ULP
Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.
Seoul National University
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.
Universit£
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands.
University of Tokyo
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
Universit£
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
The Scripps Research Institute
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.
Universit£
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
TBA
Identification of a chemical tool for the orphan nuclear receptor FXR.
Glaxo Wellcome Research & Development
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).
Universit£
Pharmacophore-based discovery of FXR-agonists. Part II: identification of bioactive triterpenes from Ganoderma lucidum.
University of Innsbruck
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
Glaxosmithkline
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
Vitae Pharmaceuticals
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3a,7a-dihydroxy-6a-ethyl-24-nor-5β-cholan-23-amine.
Universit£
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.
Glaxosmithkline
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.
F. Hoffmann-La Roche
Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia& diabetes.
F. Hoffmann-La Roche
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Vitae Pharmaceuticals
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates.
Wyeth Research
Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR).
Wyeth Research
FXR agonist activity of conformationally constrained analogs of GW 4064.
Glaxosmithkline
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.
Glaxosmithkline
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.
Seoul National University
Design, synthesis and biological evaluations of novel farnesoid X receptor (FXR) agonists.
Shandong University
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.
Southern Medical University Biomedical Research Center
Design, synthesis, and biological studies of dual URAT1 inhibitor and FXR agonist based on benzbromarone.
Guangdong Pharmaceutical University
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Biocon-Bristol Myers Squibb Research and Development Center
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators.
Universidade De SãO Paulo
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Second-Generation Dual FXR/sEH Modulators with Optimized Pharmacokinetics.
Goethe University Frankfurt
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Design, synthesis, and biological studies of novel 3-benzamidobenzoic acid derivatives as farnesoid X receptor partial agonist.
Guangdong Pharmaceutical University
Design and identification of a new farnesoid X receptor (FXR) partial agonist by computational structure-activity relationship analysis: Ligand-induced H8 helix fluctuation in the ligand-binding domain of FXR may lead to partial agonism.
Computer-Aided Molecular Modeling Research Center
Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator.
China Pharmaceutical University
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.
Hiroshima International University
Discovery of 3?,7?,11?-Trihydroxy-6?-ethyl-5?-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
Design and Structural Optimization of Dual FXR/PPAR? Activators.
Goethe University Frankfurt
Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists.
University of Naples "Federico Ii
Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.
University of Naples "Federico Ii
Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Goethe University Frankfurt
Highly potent non-steroidal FXR agonists protostane-type triterpenoids: Structure-activity relationship and mechanism.
Dalian Medical University
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 ROR? Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.
Universidad Nacional De Colombia
Andrographolide: A natural product template for the generation of structurally and biologically diverse diterpenes.
Institute of Higher Learning
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
Terns Pharmaceuticals
Identification of potent farnesoid X receptor (FXR) antagonist showing favorable PK profile and distribution toward target tissues: Comprehensive understanding of structure-activity relationship of FXR antagonists.
Hiroshima International University
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor ?/? Agonist for the Treatment of Primary Biliary Cirrhosis.
Wuxi Apptec (Shanghai) Co.
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
Eli Lilly
Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.
Ume£
Therapeutic Potential of FXR Agonists in the Treatment of Multiple Diseases.
Therachem Research Medilab
Structural optimization and in vitro profiling of N-phenylbenzamide-based farnesoid X receptor antagonists.
Goethe-University Frankfurt
Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5).
Ardelyx
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.
University of Perugia
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.
Wuxi Apptec (Shanghai)
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Genomics Institute of The Novartis Research Foundation
A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis.
Goethe-University Frankfurt
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.
Aventis Pharmaceuticals
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
Albany Medical College
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor.
Eli Lilly
Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
UniversitÄT WÜRzburg
Adenosine receptor agonists: synthesis and biological evaluation of the diastereoisomers of 2-(3-hydroxy-3-phenyl-1-propyn-1-yl)NECA.
UniversitÀ
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
Abbott Laboratories
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
National Institute of Mental Health
Targeting a prokaryotic protein in a eukaryotic pathogen: identification of lead compounds against cryptosporidiosis.
Brandeis University
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Absolute Science
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors.
University of Liverpool
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Universita Degli Studi Di Bari