2. Academic Validation
  3. Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration

Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration

  • Bioorg Med Chem Lett. 2017 Oct 15;27(20):4673-4677. doi: 10.1016/j.bmcl.2017.09.008.
Steven M Sparks 1,  Paul K Spearing 2,  Caroline J Diaz 2,  David J Cowan 2,  Channa Jayawickreme 2,  Grace Chen 2,  Thomas J Rimele 2,  Claudia Generaux 2,  Lindsey T Harston 2,  Shane G Roller 2
Affiliations

Affiliations

  • 1 Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States. Electronic address: ssparks@viamet.com.
  • 2 Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
PMID: 28916340 DOI: 10.1016/j.bmcl.2017.09.008
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).

Keywords

Calcium sensing receptor; GI-restricted; Nutrient sensing.

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