Selection of peptides binding to the alpha 5 beta 1 integrin from phage display library

J Biol Chem. 1993 Sep 25;268(27):20205-10.

Abstract

The alpha 5 beta 1 integrin binds fibronectin through the integrin recognition sequence Arg-Gly-Asp (RGD). We have used a 6-amino acid peptide library expressed on filamentous phage to identify peptide ligands for alpha 5 beta 1. We found that this integrin selectively binds RGD-containing peptides from the library. Of the 32 different sequences obtained, 28 had the RGD motif, 3 contained sequences related to RGD, and only 1 had a clearly different sequence. One of the RGD-containing phage encoded a potentially cyclic insert CRGDCL. The cyclic peptide GAC*RGDC*LGA (where * denotes cysteines forming a disulfide bond) was 10-fold more efficient than any of the linear RGD-containing hexapeptides in inhibiting the binding of RGD-expressing phage to alpha 5 beta 1 or the attachment of alpha 5 beta 1-expressing cells to fibronectin. This peptide also inhibited cell attachment mediated by the alpha v beta 1, alpha v beta 3, and alpha v beta 5 integrins with about 10-fold higher efficiency than linear GRGDSP. One peptide containing an RGD-related sequence, NGRAHA, was also found to inhibit phage attachment and cell adhesion, especially adhesion mediated by the alpha v beta 5 integrin. These results indicate that novel and high affinity ligands for integrins can be isolated from a random peptide library.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Bacteriophages
  • Base Sequence
  • Binding, Competitive
  • CHO Cells
  • Cricetinae
  • Databases, Factual
  • Fibronectins / metabolism
  • Gene Library
  • Integrins / metabolism*
  • Kinetics
  • Molecular Sequence Data
  • Oligodeoxyribonucleotides
  • Oligopeptides / metabolism*
  • Polymerase Chain Reaction
  • Receptors, Fibronectin
  • Transfection

Substances

  • Fibronectins
  • Integrins
  • Oligodeoxyribonucleotides
  • Oligopeptides
  • Receptors, Fibronectin
  • arginyl-glycyl-aspartic acid