Structural insights into the regulation of PDK1 by phosphoinositides and inositol phosphates

EMBO J. 2004 Oct 13;23(20):3918-28. doi: 10.1038/sj.emboj.7600379. Epub 2004 Sep 30.

Abstract

3-phosphoinositide-dependent protein kinase-1 (PDK1) phosphorylates and activates many kinases belonging to the AGC subfamily. PDK1 possesses a C-terminal pleckstrin homology (PH) domain that interacts with PtdIns(3,4,5)P3/PtdIns(3,4)P2 and with lower affinity to PtdIns(4,5)P2. We describe the crystal structure of the PDK1 PH domain, in the absence and presence of PtdIns(3,4,5)P3 and Ins(1,3,4,5)P4. The structures reveal a 'budded' PH domain fold, possessing an N-terminal extension forming an integral part of the overall fold, and display an unusually spacious ligand-binding site. Mutagenesis and lipid-binding studies were used to define the contribution of residues involved in phosphoinositide binding. Using a novel quantitative binding assay, we found that Ins(1,3,4,5,6)P5 and InsP6, which are present at micromolar levels in the cytosol, interact with full-length PDK1 with nanomolar affinities. Utilising the isolated PDK1 PH domain, which has reduced affinity for Ins(1,3,4,5,6)P5/InsP6, we perform localisation studies that suggest that these inositol phosphates serve to anchor a portion of cellular PDK1 in the cytosol, where it could activate its substrates such as p70 S6-kinase and p90 ribosomal S6 kinase that do not interact with phosphoinositides.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Phosphoinositide-Dependent Protein Kinases
  • Amino Acid Sequence
  • Binding Sites
  • Binding, Competitive
  • Cell Line
  • Crystallography, X-Ray
  • Cytosol / chemistry
  • Cytosol / metabolism
  • Fluorescence Resonance Energy Transfer
  • Glutathione Transferase / metabolism
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Inositol Phosphates / metabolism*
  • Ligands
  • Lipid Metabolism
  • Models, Molecular
  • Mutagenesis, Site-Directed
  • Mutation
  • Phosphatidylinositols / metabolism*
  • Phosphorylation
  • Protein Serine-Threonine Kinases / chemistry*
  • Protein Serine-Threonine Kinases / genetics
  • Protein Serine-Threonine Kinases / metabolism*
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / metabolism
  • Spectrum Analysis, Raman
  • Water / chemistry

Substances

  • Inositol Phosphates
  • Ligands
  • Phosphatidylinositols
  • Recombinant Fusion Proteins
  • Water
  • Glutathione Transferase
  • 3-Phosphoinositide-Dependent Protein Kinases
  • PDPK1 protein, human
  • Protein Serine-Threonine Kinases