Nkx6.1 regulates islet β-cell proliferation via Nr4a1 and Nr4a3 nuclear receptors

Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5242-7. doi: 10.1073/pnas.1320953111. Epub 2014 Mar 24.

Abstract

Loss of functional β-cell mass is a hallmark of type 1 and type 2 diabetes, and methods for restoring these cells are needed. We have previously reported that overexpression of the homeodomain transcription factor NK6 homeobox 1 (Nkx6.1) in rat pancreatic islets induces β-cell proliferation and enhances glucose-stimulated insulin secretion, but the pathway by which Nkx6.1 activates β-cell expansion has not been defined. Here, we demonstrate that Nkx6.1 induces expression of the nuclear receptor subfamily 4, group A, members 1 and 3 (Nr4a1 and Nr4a3) orphan nuclear receptors, and that these factors are both necessary and sufficient for Nkx6.1-mediated β-cell proliferation. Consistent with this finding, global knockout of Nr4a1 results in a decrease in β-cell area in neonatal and young mice. Overexpression of Nkx6.1 and the Nr4a receptors results in increased expression of key cell cycle inducers E2F transcription factor 1 and cyclin E1. Furthermore, Nkx6.1 and Nr4a receptors induce components of the anaphase-promoting complex, including ubiquitin-conjugating enzyme E2C, resulting in degradation of the cell cycle inhibitor p21. These studies identify a unique bipartite pathway for activation of β-cell proliferation, suggesting several unique targets for expansion of functional β-cell mass.

Publication types

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

MeSH terms

  • Animals
  • Animals, Newborn
  • Cell Proliferation*
  • Chromatin Immunoprecipitation
  • DNA-Binding Proteins / physiology*
  • Homeodomain Proteins / genetics
  • Homeodomain Proteins / physiology*
  • Islets of Langerhans / cytology*
  • Male
  • Mice, Knockout
  • Nerve Tissue Proteins / physiology*
  • Nuclear Receptor Subfamily 4, Group A, Member 1 / physiology*
  • Oligonucleotide Array Sequence Analysis
  • RNA, Messenger / genetics
  • Rats
  • Rats, Wistar
  • Ubiquitin-Conjugating Enzymes / metabolism
  • Up-Regulation

Substances

  • DNA-Binding Proteins
  • Homeodomain Proteins
  • Nerve Tissue Proteins
  • Nkx6-1 protein, rat
  • Nr4a1 protein, rat
  • Nr4a3 protein, rat
  • Nuclear Receptor Subfamily 4, Group A, Member 1
  • RNA, Messenger
  • Ubiquitin-Conjugating Enzymes

Associated data

  • GEO/GSE55079