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Steven M. Sparks Paul K. Spearing Caroline J. Diaz David J. Cowan Channa Jayawickreme Grace Chen Thomas J. Rimele Claudia Generaux Lindsey T. Harston Shane G. Roller 《Bioorganic & medicinal chemistry letters》2017,27(20):4673-4677
Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in mineral and amino acid nutrient sensing and thus is an attractive target for modulation in the intestine. Herein we describe the optimization of gastrointestinally restricted calcium-sensing receptor agonists starting from a 3-aminopyrrolidine-containing template leading to the identification of GI-restricted agonist 19 (GSK3004774). 相似文献
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