Fluorescein-labeled stable neurotensin derivatives

J Pept Sci. 2006 Aug;12(8):505-8. doi: 10.1002/psc.757.

Abstract

Neurotensin(8-13) analogs containing a glycine or 5-aminovaleroyl spacer were labeled with fluorescein through formation of an N-terminal thiourea function. The receptor binding was measured in HT-29 cell cultures and showed a substantial decrease in affinity, especially for the metabolically stabilized [MeArg(9), Tle(11)] analog. Using fluorescence microscopy, the internalization of the fluorescent neurotensin analogs into HT-29 cells was observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Fluorescein-5-isothiocyanate / chemistry
  • Fluorescent Dyes / chemistry*
  • HT29 Cells
  • Humans
  • Microscopy, Fluorescence / methods
  • Molecular Structure
  • Neurotensin / analogs & derivatives*
  • Neurotensin / chemistry
  • Neurotensin / metabolism
  • Protein Binding
  • Protein Transport
  • Receptors, Neurotensin / metabolism

Substances

  • Fluorescent Dyes
  • Receptors, Neurotensin
  • Neurotensin
  • Fluorescein-5-isothiocyanate