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A bioconjugate of Lys and Arg mimics biological activity of the Arg–Gly–Asp peptide sequence

Authors
Publisher
Elsevier Ltd
Volume
1
Issue
1
Identifiers
DOI: 10.1016/j.actbio.2004.09.005
Keywords
  • Cell Adhesion
  • Rgd Peptide Mimetic
  • Biomaterial Coatings
  • Integrin Antagonist
Disciplines
  • Biology
  • Medicine

Abstract

Abstract A peptidomimetic, 2-amino-6-[(2-amino-5{guanidino}pentanoyl) amino] hexanoic acid, was synthesized using Lys and Arg to produce a compound that mimics the biological activity of a cell adhesive Arg–Gly–Asp (RGD) peptide, GRGDSP. When immobilized on solid substrates, the peptidomimetic promoted cell adhesion similar to substrates with immobilized GRGDSP. Ligand competition studies demonstrated that cell interactions with the peptidomimetic were integrin-mediated. The peptidomimetic was very stable to proteolytic degradation in comparison to proteolytically unstable peptides. Both GRGDSP and peptidomimetic were stabilized when immobilized on solid substrates. This peptidomimetic has the broad therapeutic utility of the RGD peptides with higher stability and potentially enhanced therapeutic efficacy.

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