A specifically radiolabeled somatostatin analog with strong antitumor activity induces apoptosis and accumulates in the cytosol and the nucleus of HT29 human colon carcinoma cells

Zsolt Szegedi, József Takács, Béla Szende, Zsolt Vadász, Anikó Horváth, Éva Gulyás, Géza Tóth, István Peták, József Bocsi, György Kéri

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

The new heptapeptide somatostatin analog TT-232 decreases proliferation of HT-29 human colon carcinoma cells in vitro by reducing mitotic and increasing apoptotic activity. We have synthesized and characterized a specifically tritium labeled 3H-Tyr3-TT-232 (30 Ci/mmol) to investigate the effect and the fate of this antitumor peptide on human colon tumor cells. 3H-labeled TT-232 could be detected on the cell surface, on cytoplasmic membranes and also in the nucleus of HT-29 cells, 1-6 h after the administration of 0.5 and 50 μg/mL [ 3H]TT-232. Binding and internalization of TT-232 to human colon tumor cells at a relatively high dose provide further evidence for the existence of low-affinity somatostatin receptors in such cells, which might mediate the apoptosis-inducing effect. Our data suggest the possible use of TT-232 in the treatment of human colon tumors.

Original languageEnglish
Pages (from-to)25-34
Number of pages10
JournalEndocrine
Volume10
Issue number1
DOIs
Publication statusPublished - May 10 1999

Keywords

  • Antitumor activity
  • Apoptosis
  • Colon tumor
  • Internalization
  • Somatostatin analog

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology

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