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 | |
| Publication status | Published - Feb 28 2010 |
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Keywords
- Apoptosis
- Cell proliferation
- Chimera
- Dopamine receptor
- Pituitary adenoma
- Somatostatin receptor
ASJC Scopus subject areas
- Cancer Research
- Oncology
Cite this
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
}
TY - JOUR
T1 - 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
AU - Peverelli, Erika
AU - Olgiati, Luca
AU - Locatelli, Marco
AU - Magni, Paolo
AU - Fustini, Marco Faustini
AU - Frank, Giorgio
AU - Mantovani, Giovanna
AU - Beck-Peccoz, Paolo
AU - Spada, Anna
AU - Lania, Andrea
PY - 2010/2/28
Y1 - 2010/2/28
N2 - 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.
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.
KW - Apoptosis
KW - Cell proliferation
KW - Chimera
KW - Dopamine receptor
KW - Pituitary adenoma
KW - Somatostatin receptor
UR - http://www.scopus.com/inward/record.url?scp=74849085773&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=74849085773&partnerID=8YFLogxK
U2 - 10.1016/j.canlet.2009.06.034
DO - 10.1016/j.canlet.2009.06.034
M3 - Article
C2 - 19619936
AN - SCOPUS:74849085773
VL - 288
SP - 170
EP - 176
JO - Cancer Letters
JF - Cancer Letters
SN - 0304-3835
IS - 2
ER -