The dopamine-somatostatin chimeric compound BIM-23A760 exerts antiproliferative and cytotoxic effects in human non-functioning pituitary tumors by activating ERK1/2 and p38 pathways

Erika Peverelli, Luca Olgiati, Marco Locatelli, Paolo Magni, Marco Faustini Fustini, Giorgio Frank, Giovanna Mantovani, Paolo Beck-Peccoz, Anna Spada, Andrea Lania

Research output: Contribution to journalArticlepeer-review

Abstract

The study investigated the effects of the dopamine-somatostatin chimeric compound BIM-23A760 on cell proliferation and apoptosis in cultured cells from human non-functioning pituitary tumors (NFPTs). Both BIM-23A760 and the dopaminergic agonist BIM-53097 induced a significant inhibition of cell proliferation associated with increased p27 expression, together with a significant increase in caspase-3 activity. Conversely, null or marginal effects were elicited by somatostatin analogs. Moreover, BIM-23A760 and BIM-53097 induced ERK1/2 and p38 phosphorylation and the blockade of these pathways prevented both the antiproliferative and the pro-apoptotic effects of these drugs. In conclusions the chimeric compound BIM-23A760 is able to exert cytostatic and cytotoxic effects in NFPTs, these phenomena being mainly mediated by DR2D and involving ERK1/2 and p38 pathways activation.

Original languageEnglish
Pages (from-to)170-176
Number of pages7
JournalCancer Letters
Volume288
Issue number2
DOIs
Publication statusPublished - Feb 28 2010

Keywords

  • Apoptosis
  • Cell proliferation
  • Chimera
  • Dopamine receptor
  • Pituitary adenoma
  • Somatostatin receptor

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

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