CK2 phosphorylation of Pdx-1 regulates its transcription factor activity

Cell Mol Life Sci. 2010 Jul;67(14):2481-9. doi: 10.1007/s00018-010-0348-0. Epub 2010 Mar 26.

Abstract

The duodenal homeobox-1 protein Pdx-1 is one of the regulators for the transcription of the insulin gene. Pdx-1 is a phosphoprotein, and there is increasing evidence for the regulation of some of its functions by phosphorylation. Here, we asked whether protein kinase CK2 might phosphorylate Pdx-1 and how this phosphorylation could be implicated in the functional regulation of Pdx-1. We used fragments of Pdx-1 as well as phosphorylation mutants for experiments with protein kinase CK2. Transactivation was measured by reporter assays using the insulin promoter. Our data showed that Pdx-1 is phosphorylated by protein kinase CK2 at amino acids thr(231) and ser(232), and this phosphorylation was implicated in the regulation of the transcription factor activity of Pdx-1. Furthermore, inhibition of protein kinase CK2 by specific inhibitors led to an elevated release of insulin from pancreatic beta-cells. Thus, these findings identify CK2 as a novel mediator of the insulin metabolism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Casein Kinase II / antagonists & inhibitors
  • Casein Kinase II / genetics
  • Casein Kinase II / metabolism*
  • Cell Line
  • Cell Line, Tumor
  • Enzyme Inhibitors / pharmacology
  • Homeodomain Proteins / chemistry
  • Homeodomain Proteins / genetics
  • Homeodomain Proteins / metabolism*
  • Humans
  • Insulin / genetics
  • Insulin / metabolism*
  • Insulin-Secreting Cells / metabolism*
  • Mice
  • Molecular Sequence Data
  • Phosphorylation
  • Trans-Activators / chemistry
  • Trans-Activators / genetics
  • Trans-Activators / metabolism*
  • Transcription, Genetic
  • Transcriptional Activation*
  • Transfection

Substances

  • Enzyme Inhibitors
  • Homeodomain Proteins
  • Insulin
  • Trans-Activators
  • pancreatic and duodenal homeobox 1 protein
  • Casein Kinase II