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Discovery of novel and selective GPR17 antagonists as pharmacological tools for developing new therapeutic strategies in diabetes and obesity.

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第一作者： Hu,Zhu

第一单位： Early Translational Branch, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, 20850, USA.

作者： Hu,Zhu ^[1] ; Jason M,Conley ^[2] ; Surendra,Karavadhi ^[1] ; Justin E,LaVigne ^[3] ; Val J,Watts ^[3] ; Hongmao,Sun ^[1] ; Min,Shen ^[1] ; Matthew D,Hall ^[1] ; Hongxia,Ren ^[4] ; Samarjit,Patnaik ^[5]

作者单位： Early Translational Branch, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, 20850, USA. ^[1] Herman B. Wells Center for Pediatric Research, Department of Pediatrics, USA. ^[2] Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN, 47907, USA. ^[3] Herman B. Wells Center for Pediatric Research, Department of Pediatrics, USA; Center for Diabetes and Metabolic Diseases, USA; Stark Neurosciences Research Institute, USA; Department of Anatomy, Cell Biology & Physiology, USA; Department of Biochemistry & Molecular Biology, USA; Department of Pharmacology & Toxicology, Indiana University School of Medicine, Indianapolis, IN, 46202, USA. Electronic address: renh@iu.edu. ^[4] Early Translational Branch, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, 20850, USA. Electronic address: samarjit.patnaik@nih.gov. ^[5]

关键词 Antagonist Calcium Cyclic AMP (cAMP)Diabetes G protein-coupled receptor (GPCR)Glucagon-like peptide 1 (GLP-1)High-throughput screening (HTS)MDL29,951 (MDL)Obesity Selectivity Signal transduction β-arrestin