Tetrafibricin has a high selectivity for GPIIb/IIIa: comparison of the effects of tetrafibricin and RGDS on GPIIb/IIIa and the vitronectin receptor

Biochem Biophys Res Commun. 1994 Oct 14;204(1):325-32. doi: 10.1006/bbrc.1994.2463.

Abstract

The specificity of tetrafibricin was examined by comparing its activities on GPIIb/IIIa and on the vitronectin receptor (alpha v beta 3) with those of Arg-Gly-Asp-Ser (RGDS) on the same receptors. Tetrafibricin, which inhibited fibrinogen-GPIIb/IIIa binding 10 times more potently than RGDS, was three orders of magnitude less potent compared to RGDS on the inhibition of fibrinogen binding to alpha v beta 3. Furthermore, tetrafibricin potently inhibited platelet adhesion to both fibrinogen and von Willebrand factor. Whereas, there was no significant inhibition observed in the GPIIb/IIIa-independent cellular adhesions. These results suggest that tetrafibricin is highly selective for GPIIb/IIIa.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anti-Bacterial Agents / pharmacology*
  • Aorta
  • Blood Platelets / metabolism
  • Cattle
  • Cells, Cultured
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology*
  • Fibrinogen / metabolism
  • Glycoproteins / metabolism
  • Humans
  • Integrins / drug effects*
  • Integrins / isolation & purification
  • Integrins / metabolism
  • Kinetics
  • Macrolides*
  • Molecular Sequence Data
  • Oligopeptides / pharmacology*
  • Platelet Adhesiveness / drug effects
  • Platelet Adhesiveness / physiology
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Membrane Glycoproteins / drug effects*
  • Platelet Membrane Glycoproteins / isolation & purification
  • Platelet Membrane Glycoproteins / metabolism
  • Receptors, Cytoadhesin / drug effects*
  • Receptors, Cytoadhesin / isolation & purification
  • Receptors, Cytoadhesin / metabolism
  • Receptors, Vitronectin
  • Vitronectin
  • von Willebrand Factor / metabolism

Substances

  • Anti-Bacterial Agents
  • Glycoproteins
  • Integrins
  • Macrolides
  • Oligopeptides
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Receptors, Cytoadhesin
  • Receptors, Vitronectin
  • Vitronectin
  • von Willebrand Factor
  • tetrafibricin
  • Fibrinogen
  • arginyl-glycyl-aspartyl-serine