56 articles for thisTarget
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Article Title
Organization
Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists.
Janssen Research and Development
Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.
Janssen Research and Development
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist.
Zydus Research Centre
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.
Chung-Ang University
Modification on ursodeoxycholic acid (UDCA) scaffold. discovery of bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1).
University of Naples&Quot;Federico Ii&Quot
Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes.
Chinese Academy of Sciences
Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists.
The Beckman Research Institute
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
4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.
Istituto Italiano Di Tecnologia
Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.
Genomics Institute of The Novartis Research Foundation
Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
Chinese Academy of Sciences
Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists.
F. Hoffmann-La Roche
Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries.
Pfizer
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Pfizer
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.
Glaxosmithkline
Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists.
Chinese Academy of Sciences
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
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
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3a,7a-dihydroxy-6a-ethyl-24-nor-5β-cholan-23-amine.
University of Perugia
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
Kalypsys
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
Design and exploration of gut-restricted bifunctional molecule with TGR5 agonistic and DPP4 inhibitory effects for treating ulcerative colitis.
Shanghai Institute of Materia Medica
Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives.
Tes Pharma
Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.
University of Perugia
Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases.
Eli Lilly
Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor.
University of Health Sciences and Pharmacy
Discovery of novel ketoxime ether derivatives with potent FXR agonistic activity, oral effectiveness and high liver/blood ratio.
Nanchang 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
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.
University of Naples "Federico Ii
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5
Chinese Academy of Sciences
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Chinese Academy of Sciences
Structural modifications that increase gut restriction of bile acid derivatives.
University of Minnesota
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.
Henan University
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis.
University of Naples "Federico Ii
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
7-Methylation of Chenodeoxycholic Acid Derivatives Yields a Substantial Increase in TGR5 Receptor Potency.
University of Minnesota
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.
Heinrich Heine University
Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5).
Ardelyx
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.
Wuxi Apptec (Shanghai)
Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes.
Cadila Healthcare
Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance.
Universities of Lille
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
Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
Lycera