Chemical screen identifies FDA-approved drugs and target pathways that induce precocious pancreatic endocrine differentiation

Proc Natl Acad Sci U S A. 2011 Nov 29;108(48):19264-9. doi: 10.1073/pnas.1113081108. Epub 2011 Nov 14.

Abstract

Pancreatic β-cells are an essential source of insulin and their destruction because of autoimmunity causes type I diabetes. We conducted a chemical screen to identify compounds that would induce the differentiation of insulin-producing β-cells in vivo. To do this screen, we brought together the use of transgenic zebrafish as a model of β-cell differentiation, a unique multiwell plate that allows easy visualization of lateral views of swimming larval fish and a library of clinical drugs. We identified six hits that can induce precocious differentiation of secondary islets in larval zebrafish. Three of these six hits were known drugs with a considerable background of published data on mechanism of action. Using pharmacological approaches, we have identified and characterized two unique pathways in β-cell differentiation in the zebrafish, including down-regulation of GTP production and retinoic acid biosynthesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetanilides / pharmacology
  • Animals
  • Animals, Genetically Modified
  • Caffeic Acids / pharmacology
  • Cell Differentiation / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation
  • DNA Primers / genetics
  • Dimethyl Sulfoxide
  • Dose-Response Relationship, Drug
  • Drug Discovery / methods*
  • Epirizole / pharmacology
  • Fluorescent Antibody Technique
  • Green Fluorescent Proteins
  • Guanosine Triphosphate / biosynthesis
  • HMGB1 Protein / metabolism
  • Insulin-Secreting Cells / cytology*
  • Insulin-Secreting Cells / drug effects*
  • Larva / drug effects
  • Microscopy, Confocal
  • Mycophenolic Acid / pharmacology
  • Pharmaceutical Preparations / metabolism*
  • Real-Time Polymerase Chain Reaction
  • Sulfanilic Acids / pharmacology
  • Tretinoin / metabolism
  • Zebrafish
  • p-Aminoazobenzene / analogs & derivatives
  • p-Aminoazobenzene / pharmacology

Substances

  • Acetanilides
  • Caffeic Acids
  • DNA Primers
  • HMGB1 Protein
  • N-(4-(3-(3,4-dihydroxyphenyl)acryloyl)phenyl)-2-(thiophen-2-yl)acetamide
  • Pharmaceutical Preparations
  • Sulfanilic Acids
  • Green Fluorescent Proteins
  • C.I. Solvent Yellow 56
  • Epirizole
  • Tretinoin
  • p-Aminoazobenzene
  • Guanosine Triphosphate
  • Mycophenolic Acid
  • Dimethyl Sulfoxide