Synthesis and sst2 binding profiles of new (Tyr3)octreotate analogs

Christos Petrou, Vassiliki Magafa, Anastasia Nikolopoulou, George Pairas, Berthold Nock, Theodosia Maina, Paul Cordopatis

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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 languageEnglish
Pages (from-to)725-730
Number of pages6
JournalJournal of Peptide Science
Volume14
Issue number6
DOIs
Publication statusPublished - Jun 2008

Keywords

  • [Tyra]octreotate
  • AR4-2J cells
  • Binding affinity
  • Somatostatin analogs
  • sst

Cite this

Petrou, C., Magafa, V., Nikolopoulou, A., Pairas, G., Nock, B., Maina, T., & Cordopatis, P. (2008). Synthesis and sst2 binding profiles of new (Tyr3)octreotate analogs. Journal of Peptide Science, 14(6), 725-730. https://doi.org/10.1002/psc.989