57 articles for thisTarget
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Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.
Vanderbilt University
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists.
Shanghai Institute of Materia Medica
A novel series of indazole-/indole-based glucagon receptor antagonists.
Merck Research Laboratories
Recent progress in the development of small-molecule glucagon receptor antagonists.
Pfizer
Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.
Dainippon Sumitomo Pharma
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
Merck Research Laboratories
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Pfizer
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C.
Chinese Academy of Sciences
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes.
Merck Research Laboratories
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.
Bristol-Myers Squibb
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
Pfizer
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.
Merck Research Laboratories
Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.
Merck Research Laboratories
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Merck Research Laboratories
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Novel glucagon receptor antagonists with improved selectivity over the glucose-dependent insulinotropic polypeptide receptor.
Novo Nordisk
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Merck Research Laboratories
BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
Boehringer Ingelheim Pharma Gmbh And
New beta-alanine derivatives are orally available glucagon receptor antagonists.
Novo Nordisk
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.
Merck Research Laboratories
Design of novel Xenopus GLP-1-based dual glucagon-like peptide 1 (GLP-1)/glucagon receptor agonists.
Affiliated Tumor Hospital of Guangxi Medical University
Novel substituted naphthalen-1-yl-methanone derivatives as anti-hyperglycemic agents.
Central Drug Research Institute
Discovery of Insulin/GLP-1/Glucagon Triagonists for the Treatment of Diabetes and Obesity.
Merck
Fast small molecule similarity searching with multiple alignment profiles of molecules represented in one-dimension.
Pharmacopeia
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.
Merck Research Laboratories
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes.
Merck
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Merck Research Laboratories
Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists.
Indiana University
Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.
Novo Nordisk
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists.
Bayer Research Center
Optimization of the 4-aryl group of 4-aryl-pyridine glucagon antagonists: development of an efficient, alternative synthesis.
Bayer Research Center
Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.
Bayer Research Center
Automated Design of Macrocycles for Therapeutic Applications: From Small Molecules to Peptides and Proteins.
Schrodinger
Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural Optimization.
Indiana University
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.
Janssen Research & Development
Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.
Janssen Research & Development
Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.
Novo Nordisk
Design, synthesis, and effects of novel phenylpyrimidines as glucagon receptor antagonists.
Gachon University
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.
Chinese Academy of Sciences
Optimization of peptide-based polyagonists for treatment of diabetes and obesity.
Novo Nordisk Research Center Indianapolis
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.
China Pharmaceutical University
Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.
Sanofi-Aventis Deutschland
Design of Novel Exendin-Based Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists.
Sanofi-Aventis Deutschland
Origins of PDZ Binding Specificity. A Computational and Experimental Study Using NHERF1 and the Parathyroid Hormone Receptor.
The University of Queensland