A target cell-specific activatable fluorescence probe for in vivo molecular imaging of cancer based on a self-quenched avidin-rhodamine conjugate

Cancer Res. 2007 Mar 15;67(6):2791-9. doi: 10.1158/0008-5472.CAN-06-3315.

Abstract

A target cell-specific activation strategy for improved molecular imaging of peritoneal implants has been proposed, in which fluorophores are activated only in living targeted cells. A current example of an activatable fluorophore is one that is normally self-quenched by attachment to a peptide backbone but which can be activated by specific proteases that degrade the peptide resulting in "dequenching." In this study, an alternate fluorescence activation strategy is proposed whereby self-quenching avidin-rhodamine X, which has affinity for lectin on cancer cells, is activated after endocytosis and degradation within the lysosome. Using this approach in a mouse model of peritoneal ovarian metastases, we document target-specific molecular imaging of submillimeter cancer nodules with minimal contamination by background signal. Cellular internalization of receptor-ligand pairs with subsequent activation of fluorescence via dequenching provides a generalizable and highly sensitive method of detecting cancer microfoci in vivo and has practical implications for assisting surgical and endoscopic procedures.

Publication types

  • Research Support, N.I.H., Intramural

MeSH terms

  • Animals
  • Avidin / chemistry
  • Avidin / pharmacokinetics*
  • Cell Line, Tumor
  • Detergents / chemistry
  • Female
  • Fluorescence
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacokinetics*
  • Humans
  • Image Processing, Computer-Assisted
  • Mice
  • Ovarian Neoplasms / metabolism*
  • Ovarian Neoplasms / pathology
  • Rhodamines / chemistry
  • Rhodamines / pharmacokinetics*
  • Spectrometry, Fluorescence

Substances

  • Detergents
  • Fluorescent Dyes
  • Rhodamines
  • Avidin