Characterization of the cross-linking site of disintegrins albolabrin, bitistatin, echistatin, and eristostatin on isolated human platelet integrin GPIIb/IIIa

Biochem Biophys Res Commun. 1994 Jul 15;202(1):135-40. doi: 10.1006/bbrc.1994.1903.

Abstract

Disintegrins, a family of low molecular weight, RGD-containing peptides found in snake venoms prevent the binding of adhesive ligands to a number of integrin receptors. Albolabrin, bitistatin, echistatin, and eristostatin bind to the platelet fibrinogen receptor (GPIIb/IIIa) acting thus as potent inhibitors of platelet aggregation. Here, we have determined the cross-linking of these disintegrins on isolated GPIIb/IIIa. The cross-linking site of all of them was within GPIIIa 217-302, a domain that has been implicated in a number of receptor functions including heterodimer association, activation-dependent conformational changes, and fibrinogen binding.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Cross-Linking Reagents
  • Crotalid Venoms / metabolism
  • Humans
  • Intercellular Signaling Peptides and Proteins
  • Oligopeptides
  • Peptides / metabolism*
  • Peptides / pharmacology
  • Platelet Aggregation Inhibitors / metabolism
  • Platelet Membrane Glycoproteins / drug effects
  • Platelet Membrane Glycoproteins / metabolism*
  • Snake Venoms
  • Viper Venoms / metabolism*
  • Viper Venoms / pharmacology

Substances

  • Cross-Linking Reagents
  • Crotalid Venoms
  • Intercellular Signaling Peptides and Proteins
  • Oligopeptides
  • Peptides
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Snake Venoms
  • Viper Venoms
  • echistatin
  • bitistatin
  • albolabrin
  • eristostatin
  • arginyl-glycyl-aspartic acid