Modulation of alpha-thrombin function by distinct interactions with platelet glycoprotein Ibalpha

Science. 2003 Jul 11;301(5630):218-21. doi: 10.1126/science.1084183.

Abstract

Thrombin bound to platelets contributes to stop bleeding and, in pathological conditions, may cause vascular thrombosis. We have determined the structure of platelet glycoprotein Ibalpha (GpIbalpha) bound to thrombin at 2.3 angstrom resolution and defined two sites in GpIbalpha that bind to exosite II and exosite I of two distinct alpha-thrombin molecules, respectively. GpIbalpha occupancy may be sequential, as the site binding to alpha-thrombin exosite I appears to be cryptic in the unoccupied receptor but exposed when a first thrombin molecule is bound through exosite II. These interactions may modulate alpha-thrombin function by mediating GpIbalpha clustering and cleavage of protease-activated receptors, which promote platelet activation, while limiting fibrinogen clotting through blockade of exosite I.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Binding Sites
  • Blood Coagulation
  • Blood Platelets / chemistry
  • Blood Platelets / metabolism
  • Crystallization
  • Crystallography, X-Ray
  • Fibrinogen / metabolism
  • Humans
  • Hydrogen Bonding
  • Ligands
  • Models, Molecular
  • Mutation
  • Platelet Aggregation
  • Platelet Glycoprotein GPIb-IX Complex / chemistry*
  • Platelet Glycoprotein GPIb-IX Complex / genetics
  • Platelet Glycoprotein GPIb-IX Complex / metabolism*
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Thrombin / chemistry*
  • Thrombin / metabolism*

Substances

  • Ligands
  • Platelet Glycoprotein GPIb-IX Complex
  • Recombinant Proteins
  • Fibrinogen
  • Thrombin

Associated data

  • PDB/100K
  • PDB/1P9A
  • PDB/1PPB