Isoxazole Alters Metabolites and Gene Expression, Decreasing Proliferation and Promoting a Neuroendocrine Phenotype in β-Cells

  • ACS Chem Biol. 2016 Apr 15;11(4):1128-36. doi: 10.1021/acschembio.5b00993.
Michael A Kalwat ,  Zhimin Huang ,  Chonlarat Wichaidit ,  Kathleen McGlynn ,  Svetlana Earnest ,  Claudia Savoia  1 ,  Elhadji M Dioum  1 ,  Jay W Schneider ,  Michele R Hutchison ,  Melanie H Cobb
Affiliations
  • 1. Nestle Institute of Health Sciences , Lausanne, Switzerland.
Abstract

Novel strategies are needed to modulate β-cell differentiation and function as potential β-cell replacement or restorative therapies for diabetes. We previously demonstrated that small molecules based on the isoxazole scaffold drive neuroendocrine phenotypes. The nature of the effects of isoxazole compounds on β-cells was incompletely defined. We find that isoxazole induces genes that support neuroendocrine and β-cell phenotypes and suppresses genes important for proliferation. Isoxazole alters β-cell metabolites and protects glucose-responsive signaling pathways under lipotoxic conditions. Finally, we show that isoxazole improves glycemia in a mouse model of β-cell regeneration. Isoxazole is a prime candidate to alter cell fate in different contexts.