Ligand and cation binding are dual functions of a discrete segment of the integrin beta 3 subunit: cation displacement is involved in ligand binding

Cell. 1994 Nov 18;79(4):659-67. doi: 10.1016/0092-8674(94)90551-7.

Abstract

The alpha IIb beta 3 integrin binds Arg-Gly-Asp-containing (RGD-containing) ligands in a cation-dependent interaction. A fourteen amino acid sequence, beta 3 (118-131), and an antibody to it, inhibited ligand binding functions of alpha IIb beta 3, and a 1:1 stoichiometric beta 3 (118-131)-RGD complex was detected by mass spectroscopy. Cation binding to beta 3 (118-131) was demonstrated by terbium luminescence and mass spectroscopy. Notably, ligand displaced cation from the beta 3(118-131) peptide and also from purified alpha IIb beta 3. Thus, beta 3 (118-131), a highly conserved region in integrin beta subunits, binds both ligand and cation. Formation of a ternary complex between cation, ligand, and receptor, with subsequent displacement of cation from beta 3 (118-131) and a second site within the receptor, may be central to the mechanism of ligand recognition by integrins.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / pharmacology
  • Binding Sites
  • Blood Platelets / drug effects
  • Blood Platelets / physiology
  • Cations
  • Humans
  • Hybridomas
  • Integrin beta3
  • Integrins / chemistry
  • Integrins / metabolism*
  • Kinetics
  • Ligands
  • Mass Spectrometry
  • Mice
  • Mice, Inbred BALB C / immunology
  • Molecular Sequence Data
  • Oligopeptides / metabolism
  • Peptide Fragments / chemical synthesis
  • Peptide Fragments / pharmacology
  • Plasmacytoma
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Glycoprotein GPIIb-IIIa Complex

Substances

  • Antibodies, Monoclonal
  • Cations
  • Integrin beta3
  • Integrins
  • Ligands
  • Oligopeptides
  • Peptide Fragments
  • Platelet Aggregation Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • arginyl-glycyl-aspartic acid