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Functionalized cyclic RGD peptidomimetics: conjugable ligands for αvβ3 receptor imaging

Bioconjug Chem. 2009 Aug 19;20(8):1611-7. doi: 10.1021/bc900155j. Epub 2009 Jul 22.

Abstract

The α(v)β(3) integrin is an adhesion molecule involved in physiological and pathological angiogenesis as well as in tumor invasion and metastasis, and therefore, there is a strong interest in developing novel agents interacting with this molecule. We report the synthesis and characterization of fluorescent α(v)β(3) integrin probes and their use to visualize integrin α(v)β(3) expression on human normal and cancer cells. The fluorescent probes we describe here may be of use for noninvasive imaging of α(V)β(3) integrin expression also in vivo.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cells, Cultured
  • Endothelial Cells / metabolism
  • Fluorescent Dyes / analysis
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • Humans
  • Integrin alphaVbeta3 / analysis*
  • Integrin alphaVbeta3 / metabolism
  • Ligands
  • Molecular Imaging / methods*
  • Molecular Structure
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / metabolism
  • Peptidomimetics / chemical synthesis
  • Peptidomimetics / chemistry*
  • Stereoisomerism

Substances

  • Fluorescent Dyes
  • Integrin alphaVbeta3
  • Ligands
  • Peptides, Cyclic
  • Peptidomimetics
  • cyclic arginine-glycine-aspartic acid peptide