Crystal structure of the GpIbalpha-thrombin complex essential for platelet aggregation

Science. 2003 Jul 11;301(5630):222-6. doi: 10.1126/science.1083917.

Abstract

Direct interaction between platelet receptor glycoprotein Ibalpha (GpIbalpha) and thrombin is required for platelet aggregation and activation at sites of vascular injury. Abnormal GpIbalpha-thrombin binding is associated with many pathological conditions,including occlusive arterial thrombosis and bleeding disorders. The crystal structure of the GpIbalpha-thrombin complex at 2.6 angstrom resolution reveals simultaneous interactions of GpIbalpha with exosite I of one thrombin molecule,and with exosite II of a second thrombin molecule. In the crystal lattice,the periodic arrangement of GpIbalpha-thrombin complexes mirrors a scaffold that could serve as a driving force for tight platelet adhesion. The details of these interactions reconcile GpIbalpha-thrombin binding modes that are presently controversial,highlighting two distinct interfaces that are potential targets for development of novel antithrombotic drugs.

MeSH terms

  • Binding Sites
  • Blood Platelets / chemistry
  • Blood Platelets / physiology
  • Crystallization
  • Crystallography, X-Ray
  • Humans
  • Hydrogen Bonding
  • Hydrophobic and Hydrophilic Interactions
  • Models, Molecular
  • Platelet Adhesiveness
  • Platelet Aggregation*
  • Platelet Glycoprotein GPIb-IX Complex / chemistry*
  • Platelet Glycoprotein GPIb-IX Complex / metabolism*
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Thrombin / chemistry*
  • Thrombin / metabolism*

Substances

  • Platelet Glycoprotein GPIb-IX Complex
  • Thrombin

Associated data

  • PDB/1P8V