Abstract
One of the main objectives of our current work is the development of new somatostatin analogs that would retain the general characteristics of [Tyr3]octreotate (Tate) while showing potential for clinical application. In this respect, study of their interaction with the sst2 is crucial in providing preliminary structure-activity relationships data. In the present work we report on the synthesis and the preliminary biological evaluation of a total of 15 new structurally modified [Tyr3]octreotate analogs. The binding affinities were determined during competition binding assays in sst2-positive rat acinar pancreatic AR4-2J cell membranes using [125I-Tyr3]octreotide as the radioligand.
Original language | English |
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Pages (from-to) | 725-730 |
Number of pages | 6 |
Journal | Journal of Peptide Science |
Volume | 14 |
Issue number | 6 |
DOIs | |
Publication status | Published - Jun 2008 |
Keywords
- [Tyra]octreotate
- AR4-2J cells
- Binding affinity
- Somatostatin analogs
- sst