Glycoprotein IIb peptide 656-667 mimics the fibrinogen gamma chain 402-411 binding site on platelet integrin GPIIb/IIIa

FEBS Lett. 1993 Nov 29;335(1):132-5. doi: 10.1016/0014-5793(93)80454-3.

Abstract

The human integrin glycoprotein IIb/IIIa complex plays a central role in haemostasis as an inducible receptor for fibrinogen and other adhesive proteins at the platelet plasma membrane. Current evidence indicates that the ligand-binding domain of GPIIb/IIIa is discontinuous and placed at the subunit interface. Here we show that a synthetic peptide containing the polypeptide stretch GPIIb 656-667, which is hidden within the resting platelet GPIIb/IIIa heterodimer but becomes exposed following platelet activation with thrombin, binds to soluble fibrinogen (n = 2.3 +/- 1.3; Kd = 2 +/- 0.8 x 10(-5) M). This interaction is Ca(2+)-independent and can be partially inhibited with synthetic fibrinogen gamma-chain peptide 400-411 but not with GRGDS. In addition, peptide GPIIb 656-667 inhibits in a dose-dependent manner the aggregation of activated platelets (IC50 = 170 microM). Altogether, our results indicate that the GPIIb 656-667 region may form part of the inducible fibrinogen binding site and may not overlap with the integrin RGD-recognition domain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Calcium / pharmacology
  • Fibrinogen / chemistry
  • Fibrinogen / metabolism*
  • Humans
  • Molecular Sequence Data
  • Oligopeptides
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism*
  • Platelet Activation
  • Platelet Aggregation / physiology
  • Platelet Membrane Glycoproteins / chemistry
  • Platelet Membrane Glycoproteins / metabolism*
  • Protein Conformation
  • Thrombin / pharmacology

Substances

  • Oligopeptides
  • Peptide Fragments
  • Platelet Membrane Glycoproteins
  • arginyl-glycyl-aspartic acid
  • Fibrinogen
  • Thrombin
  • Calcium