Fluorescein-labeled stable neurotensin derivatives.
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.
Maes
Veronique
V
Organic Chemistry Department, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.
Hultsch
Christina
C
Kohl
Suzann
S
Bergmann
Ralf
R
Hanke
Thomas
T
Tourwé
Dirk
D