Crystal structure of the CDK4/6 inhibitory protein p18INK4c provides insights into ankyrin-like repeat structure/function and tumor-derived p16INK4 mutations

Nat Struct Biol. 1998 Jan;5(1):74-81. doi: 10.1038/nsb0198-74.

Abstract

p18INK4c is a member of a family of INK4 proteins that function to arrest the G1 to S cell cycle transition by inhibiting the activity of the cyclin-dependent kinases 4 and 6. The X-ray crystal structure of the human p18INK4c protein to a resolution of 1.95 A reveals an elongated molecule comprised of five contiguous 32- or 33-residue ankyrin-like repeat units. Each ankyrin-like repeat contains a beta-strand helix-turn-helix extended strand beta-strand motif that associates with neighboring motifs through beta-sheet, and helical bundle interactions. Conserved ankyrin-like repeat residues function to facilitate the ankyrin repeat fold and the tertiary interactions between neighboring repeat units. A large percentage of residues that are conserved among INK4 proteins and that map to positions of tumor-derived p16INK4 mutations play important roles in protein stability. A subset of these residues suggest an INK4 binding surface for the cyclin-dependent kinases 4 and 6. This surface is centered around a region that shows structural features uncharacteristic of ankyrin-like repeat units.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Ankyrin Repeat*
  • Carrier Proteins / ultrastructure*
  • Cell Cycle Proteins*
  • Consensus Sequence
  • Crystallography, X-Ray
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinase Inhibitor p18
  • Cyclin-Dependent Kinases*
  • Enzyme Inhibitors / chemistry*
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Neoplasms / genetics
  • Point Mutation
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Recombinant Proteins
  • Sequence Alignment
  • Sequence Homology, Amino Acid
  • Structure-Activity Relationship
  • Tumor Suppressor Proteins*

Substances

  • CDKN2C protein, human
  • Carrier Proteins
  • Cell Cycle Proteins
  • Cyclin-Dependent Kinase Inhibitor p18
  • Enzyme Inhibitors
  • Recombinant Proteins
  • Tumor Suppressor Proteins
  • Protein Serine-Threonine Kinases
  • CDK6 protein, human
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinases

Associated data

  • PDB/1IHB