An AlphaScreen Assay for the Discovery of Synthetic Chemical Inhibitors of Glucagon Production

Matthew R. Evans, Shuguang Wei, Bruce A Posner, Roger H Unger, Michael G Roth

Research output: Contribution to journalArticle

5 Scopus citations


Glucose homeostasis is primarily controlled by two opposing hormones, insulin and glucagon, and diabetes results when insulin fails to inhibit glucagon action. Recent efforts to control glucagon in diabetes have focused on antagonizing the glucagon receptor, which is effective in lowering blood glucose levels but leads to hyperglucogonemia in rodents. An alternative strategy would be to control glucagon production with small molecules. In pursuit of this goal, we developed a homogeneous AlphaScreen assay for measuring glucagon in cell culture media and used this in a high-throughput screen to discover synthetic compounds that inhibited glucagon secretion from an alpha cell-like cell line. Some of these compounds inhibited transcription of the glucagon gene.

Original languageEnglish (US)
Pages (from-to)325-332
Number of pages8
JournalJournal of Biomolecular Screening
Issue number4
StatePublished - Apr 1 2016



  • AlphaScreen
  • competition assay
  • diabetes
  • glucagon

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biotechnology
  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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