Synthesis and sst2 binding profiles of new [Tyr3]octreotate analogs

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 p...

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Bibliographic Details
Published in:Journal of peptide science 2008-06, Vol.14 (6), p.725-730
Main Authors: Petrou, Christos, Magafa, Vassiliki, Nikolopoulou, Anastasia, Pairas, George, Nock, Berthold, Maina, Theodosia, Cordopatis, Paul
Format: Article
Language:English
Subjects:
[Tyr3]octreotate
AR4-2J cells
binding affinity
somatostatin analogs
sst2
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Summary: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. Copyright © 2008 European Peptide Society and John Wiley & Sons, Ltd.
ISSN:1075-2617
1099-1387
DOI:10.1002/psc.989