scholarly journals Dopamine receptor type 2 ( DRD2 ) and somatostatin receptor type 2 ( SSTR2 ) agonists are effective in inhibiting proliferation of progenitor/stem‐like cells isolated from nonfunctioning pituitary tumors

2017 ◽  
Vol 140 (8) ◽  
pp. 1870-1880 ◽  
Author(s):  
E. Peverelli ◽  
E Giardino ◽  
D. Treppiedi ◽  
M. Meregalli ◽  
M. Belicchi ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Somatostatin Receptor ◽  
Pituitary Tumors ◽  
Receptor Type

scholarly journals Human non-functioning pituitary tumors invasiveness: inhibitory effects of dopamine receptor type 2 (DRD2) agonist and cofilin involvement

2016 ◽  
Author(s):  
Erika Peverelli ◽  
Elena Giardino ◽  
Donatella Treppiedi ◽  
Marco Locatelli ◽  
Valentina Vaira ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Pituitary Tumors ◽  
Receptor Type ◽  
Inhibitory Effects

β-arrestin 2 is required for dopamine receptor type 2 inhibitory effects on AKT phosphorylation and cell proliferation in pituitary tumors

2020 ◽  
Author(s):  
Federica Mangili ◽  
Elena Giardino ◽  
Donatella Treppiedi ◽  
Anna Maria Barbieri ◽  
Rosa Catalano ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Dopamine Receptor ◽  
Pituitary Tumors ◽  
Receptor Type ◽  
Inhibitory Effects ◽  
Akt Phosphorylation

scholarly journals SAT-312 Beta-Arrestin 2 Is Required for Dopamine Receptor Type 2 Inhibitory Effects on Akt Phosphorylation and Cell Proliferation in Pituitary Tumors

2020 ◽  
Vol 4 (Supplement_1) ◽  
Author(s):  
Federica Mangili ◽  
Elena Giardino ◽  
Donatella Treppiedi ◽  
Anna Maria Barbieri ◽  
Rosa Catalano ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Dopamine Receptor ◽  
Pituitary Tumors ◽  
Receptor Type ◽  
Inhibitory Effects ◽  
Akt Phosphorylation ◽  
First Choice ◽  
Antimitotic Effect

Abstract Dopamine receptor type 2 (DRD2) agonists are the first-choice treatment for PRL-secreting pituitary tumors but are poorly effective in non-functioning pituitary neuroendocrine tumors (NF-PitNETs). DRD2 reduces AKT phosphorylation in lactotrophs, but no data are available in NF-PitNETs. DRD2 effects on AKT are mediated by a β-arrestin 2-dependent mechanism in mouse striatum. The aim of this study was to investigate DRD2 effects on AKT phosphorylation and cell proliferation in human primary cultured NF-PitNET cells and in rat tumoral lactotroph cells MMQ, and to test β-arrestin 2 involvement. We found that DRD2 agonist BIM53097 induced a reduction of p- AKT /total-AKT ratio in MMQ (-32.8±17.6%, p<0.001 vs basal) and in a subset (n=15/41,36.6%) of NF-PitNETs (subgroup 1). In the remaining NF-PitNETs (subgroup 2), BIM53097 induced an increase of p- AKT. The ability of BIM53097 to reduce p-AKT correlated to its antimitotic effect, since the majority of subgroup 1 NF-PitNETs was responsive to BIM53097 and nearly all subgroup 2 NF-PitNETs were resistant. β-arrestin2 was expressed in MMQ and in 80% of subgroup 1 NF-PitNETs, whereas it was undetectable in 77% of subgroup 2 NF-PitNETs. In MMQ, β-arrestin 2 silencing prevented DRD2 inhibitory effects on p-AKT and cell proliferation. Accordingly, β-arrestin 2 transfection in subgroup 2 NF-PitNETs conferred to BIM53097 the ability to inhibit both p-AKT and cell growth. In conclusion, we demonstrated that β-arrestin 2 is required for DRD2 inhibitory effects on AKT phosphorylation and cell proliferation in MMQ and NF-PitNETs, paving the way for a potential role of β-arrestin 2 as a biomarker predicting NF-PitNETs responsiveness to treatment with dopamine agonists.

scholarly journals Octreotide promotes apoptosis in human somatotroph tumor cells by activating somatostatin receptor type 2

2006 ◽  
Vol 13 (3) ◽  
pp. 955-962 ◽  
Author(s):  
E Ferrante ◽  
C Pellegrini ◽  
S Bondioni ◽  
E Peverelli ◽  
M Locatelli ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Cultured Cells ◽  
Somatostatin Receptor ◽  
Hormone Secretion ◽  
Somatostatin Analogs ◽  
Receptor Type ◽  
Apoptotic Activity ◽  
Long Acting ◽  
Induced Apoptosis

Somatostatin analogs currently used in the treatment of acromegaly and other neuroendocrine tumors inhibit hormone secretion and cell proliferation by binding to somatostatin receptor type (SST) 2 and 5. The antiproliferative pathways coupled to these receptors have been only partially characterized. The aim of this study was to evaluate the effect of octreotide and super selective SST2 (BIM23120) and SST5 (BIM23206) analogs on apoptotic activity and apoptotic gene expression in human somatotroph tumor cells. Eight somatotroph tumors expressing similar levels of SST2 and SST5 evaluated by real-time PCR and western blot analyses were included in the study. In cultured cells obtained from these tumors, octreotide induced a dose-dependent increase of caspase-3 activity (160 ± 20% vs basal at 10 nM) and cleaved cytokeratin 18 levels (172 ± 25% vs basal) at concentrations higher than 0.1 nM. This effect was due to SST2 activation since BIM23120 elicited comparable responses, while BIM23206 was ineffective. BIM23120-stimulated apoptosis was dependent on phosphatases, since it was abrogated by the inhibitor orthovanadate, and independent from the induction of apoptosis-related genes, such as p53, p63, p73, Bcl-2, Bax, BID, BIK, TNFSF8, and FADD. In somatotroph tumors, both BIM23120 and BIM2306 caused growth arrest as indicated by the increase in p27 and decrease in cyclin D1 expression. In conclusion, the present study showed that octreotide-induced apoptosis in human somatotroph tumor cells by activating SST2. This effect, together with the cytostatic action exerted by both SST2 and SST5 analogs, might account for the tumor shrinkage observed in acromegalic patients treated with long-acting somatostatin analogs.

scholarly journals N-glycosylation of somatostatin receptor type 2 protects rats from acute pancreatitis

2021 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Ming Huang ◽  
Min-Min Chen ◽  
Dong Han ◽  
Wei Chen ◽  
Feng Xu
Keyword(s):  
Acute Pancreatitis ◽  
Somatostatin Receptor ◽  
Receptor Type

Somatostatin receptor type 2 mediated suppression of Helicobacter pylori proliferation in vitro

1998 ◽  
Vol 114 ◽  
pp. A1193
Author(s):  
K. Yamashita ◽  
H. Kaneko ◽  
T. Konagaya ◽  
S. Yamamoto ◽  
K. Kusugami ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Somatostatin Receptor ◽  
Receptor Type ◽  
Proliferation In Vitro

scholarly journals 177Lu-DOTA-EB-TATE, A Radiolabeled Analog of Somatostatin Receptor Type 2, for the Imaging and Treatment of Thyroid Cancer

2020 ◽  
pp. clincanres.3453.2020
Author(s):  
Shilpa Thakur ◽  
Brianna Daley ◽  
Corina Millo ◽  
Craig Cochran ◽  
Orit Jacobson ◽  
...  
Keyword(s):  
Thyroid Cancer ◽  
Somatostatin Receptor ◽  
Receptor Type
Sign in / Sign up

Export Citation Format

Share Document