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

doi:10.1016/j.canlet.2009.06.034

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 journal › Article › peer-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 language	English
Pages (from-to)	170-176
Number of pages	7
Journal	Cancer Letters
Volume	288
Issue number	2
DOIs	https://doi.org/10.1016/j.canlet.2009.06.034
Publication status	Published - 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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Peverelli, E., Olgiati, L., Locatelli, M., Magni, P., Fustini, M. F., Frank, G., Mantovani, G., Beck-Peccoz, P., Spada, A., & Lania, A. (2010). 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. Cancer Letters, 288(2), 170-176. https://doi.org/10.1016/j.canlet.2009.06.034

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

In: Cancer Letters, Vol. 288, No. 2, 28.02.2010, p. 170-176.

Research output: Contribution to journal › Article › peer-review

Peverelli, E, Olgiati, L, Locatelli, M, Magni, P, Fustini, MF, Frank, G, Mantovani, G, Beck-Peccoz, P, Spada, A & Lania, A 2010, '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', Cancer Letters, vol. 288, no. 2, pp. 170-176. https://doi.org/10.1016/j.canlet.2009.06.034

Peverelli, Erika ; Olgiati, Luca ; Locatelli, Marco ; Magni, Paolo ; Fustini, Marco Faustini ; Frank, Giorgio ; Mantovani, Giovanna ; Beck-Peccoz, Paolo ; Spada, Anna ; Lania, Andrea. / 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. In: Cancer Letters. 2010 ; Vol. 288, No. 2. pp. 170-176.

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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.",

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AU - Magni, Paolo

AU - Fustini, Marco Faustini

AU - Frank, Giorgio

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AU - Beck-Peccoz, Paolo

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AU - Lania, Andrea

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AB - 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.

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