Selective inactivation of the Arg-Gly-Asp-Ser (RGDS) binding site in von Willebrand factor by site-directed mutagenesis

J Biol Chem. 1992 Feb 15;267(5):3409-15.

Abstract

In order to assess the requirement for the Arg-Gly-Asp-Ser (RGDS) consensus adhesion sequence in von Willebrand factor (vWF) for vWF binding to platelets and endothelial cells, point mutations were introduced into this sequence by site-directed mutagenesis. A glycine to alanine substitution yielded RADS-vWF, while an aspartate to glutamate substitution resulted in RGES-vWF. Recombinant RADS-vWF and RGES-vWF, purified from transformed Chinese hamster ovary cells, were compared with recombinant wild type vWF (WT-vWF) in functional assays with platelets and human umbilical vein endothelial cells (HU-VECs). High molecular weight RADS-vWF and RGES-vWF multimers inhibited binding of 125I-vWF to a mixture of insolubilized native type I and III collagen and competed effectively with 125I-vWF for binding to formalin-fixed platelets in the presence of ristocetin, indicating functional collagen and platelet glycoprotein Ib binding. However, RADS-vWF and RGES-vWF were unable to displace the binding of 125I-vWF to thrombin or ADP-activated platelets. The attachment of HUVECs to either RADS-vWF or RGES-vWF coated surfaces was reduced and spreading was almost completely inhibited, compared with WT-vWF. We conclude that point mutations of the RGDS sequence in vWF selectively impair binding to platelet glycoprotein IIb/IIIa and the HUVEC vitronectin receptor.

Publication types

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

MeSH terms

  • Animals
  • Base Sequence
  • Binding Sites
  • Blood Platelets / metabolism
  • Cell Adhesion
  • Cell Line
  • Cells, Cultured
  • Cloning, Molecular
  • Collagen / metabolism
  • Endothelium, Vascular / metabolism
  • Escherichia coli / genetics
  • Humans
  • Kinetics
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed*
  • Oligodeoxyribonucleotides
  • Oligopeptides*
  • Plasmids
  • Platelet Activation
  • Platelet Membrane Glycoproteins / metabolism
  • Ristocetin / pharmacology
  • Transfection
  • von Willebrand Factor / antagonists & inhibitors
  • von Willebrand Factor / genetics
  • von Willebrand Factor / metabolism*

Substances

  • Oligodeoxyribonucleotides
  • Oligopeptides
  • Platelet Membrane Glycoproteins
  • von Willebrand Factor
  • Ristocetin
  • Collagen
  • arginyl-glycyl-aspartyl-serine