1. Academic Validation
  2. Isoxazole Alters Metabolites and Gene Expression, Decreasing Proliferation and Promoting a Neuroendocrine Phenotype in β-Cells

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

Affiliation

  • 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.

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