Effects of ATP on ligand recognition of platelet fibrinogen receptor on GPIIb-IIIa

Am J Physiol. 1994 Sep;267(3 Pt 2):H1098-106. doi: 10.1152/ajpheart.1994.267.3.H1098.

Abstract

The recent discovery of 8-azido-ATP binding sites on the platelet fibrinogen receptor glycoprotein complex GPIIb-IIIa suggests that extracellular ATP may directly modulate function of GPIIb-IIIa. In this study we investigated the effect of ATP on ligand binding to GPIIb-IIIa. Fibrinogen-mediated aggregation of washed platelets was inhibited by ATP and 8-azido-ATP in a dose-dependent manner, independent of the agonist (thrombin, collagen, epinephrine, phorbol 12-myristate 13-acetate) used to induce platelet activation. In addition, 8-azido-ATP and ATP inhibited binding of 125I-labeled fibrinogen to thrombin- and phorbol ester-activated platelets. Interaction of nonstimulated platelets with solid-phase fibrinogen was also reduced by 8-azido-ATP and ATP. Moreover, fibrinogen mimetic peptide-induced conformational change of GPIIb-IIIa on resting platelets was reduced in the presence of both nucleotides. Finally, photoincorporation of 8-azido-[gamma-32P]ATP into GPIIb-IIIa was suppressed by GRGDSP but not by the biologically inactive GRGESP peptide. Thus interaction of ATP with 8-azido-ATP binding sites present on GPIIb-IIIa modulate receptor function, which may play a role in regulation of in vivo platelet aggregation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / analogs & derivatives
  • Adenosine Triphosphate / metabolism
  • Adenosine Triphosphate / pharmacology*
  • Affinity Labels
  • Amino Acid Sequence
  • Azides / metabolism
  • Azides / pharmacology
  • Blood Platelets / metabolism*
  • Cell Adhesion / drug effects
  • Crotalid Venoms / metabolism
  • Fibrinogen / metabolism
  • Fibrinogen / physiology
  • Humans
  • Ligands
  • Light
  • Molecular Conformation
  • Molecular Sequence Data
  • Nucleotides / pharmacology
  • Oligopeptides / pharmacology
  • Peptides / pharmacology
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Membrane Glycoproteins / metabolism*

Substances

  • Affinity Labels
  • Azides
  • Crotalid Venoms
  • Ligands
  • Nucleotides
  • Oligopeptides
  • Peptides
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • 8-azidoadenosine 5'-triphosphate
  • Adenosine Triphosphate
  • Fibrinogen
  • glycyl-arginyl-glycyl-aspartyl-seryl-proline
  • Agkistrodon platelet aggregation inhibitor