Identification of potent,nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration |
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| Authors: | 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 |
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| Institution: | Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States |
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| Abstract: | 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). |
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| Keywords: | Calcium sensing receptor Nutrient sensing GI-restricted |
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