Expression of Somatostatin Receptors in Human Melanoma Cell Lines: Effect of Two Different Somatostatin Analogues, Octreotide and SOM230, on Cell Proliferation

Martínez-Alonso, Montserrat; Llecha, Nuria; Mayorga, ME; Sorolla, Anabel; Dolcet, Xavier; Sanmartín, Verónica; Abal, Leandro; Casanova, JM; Baradad, M.; Yeramian, Andrée; Egido, R.; Puig, Susana; Vilella, Ramón; Matías‐Guiu, Xavier; Marti, R.

doi:10.1177/147323000903700617

Cited by 19 publications

(12 citation statements)

References 27 publications

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“…This may reflect a comparatively low degree of tumour differentiation and is in keeping with the in-vitro study by Martinez-Alonso et al [1] who demonstrated a moderate antiproliferative effect of somatostatin analogues on melanoma cell lines at high concentrations only.…”

Section: Discussionsupporting

confidence: 68%

See 1 more Smart Citation

Comparison between F-18 fluorodeoxyglucose and Ga-68 DOTATOC in metastasized melanoma

Brogsitter

Zöphel

Wunderlich

et al. 2013

Nuclear Medicine Communications

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Section: Discussionsupporting

confidence: 68%

“…Melanoma cells are derived from the neural crest and therefore express SSTRs. Five subtypes of SSTR (SSTR1-SSTR5) have been described to date [1].…”

Section: Introductionmentioning

confidence: 99%

Comparison between F-18 fluorodeoxyglucose and Ga-68 DOTATOC in metastasized melanoma

Brogsitter

Zöphel

Wunderlich

et al. 2013

Nuclear Medicine Communications

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“…Indeed, it is very well known that this drug may have a capacity to control changes of some structural properties of the cells via secondary effects. In addition, the in vitro antiangiogenic effects of somatostatin and its analogues have been previously shown by studies on melanoma cells, which expressed one or more SSTR and were treated by using somatostatin or SSAs [20], [50].…”

Section: Discussionmentioning

confidence: 89%

The Somatostatin Analogue Octreotide Inhibits Growth of Small Intestine Neuroendocrine Tumour Cells

Martijn

Tao

et al. 2012

PLoS ONE

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Octreotide is a widely used synthetic somatostatin analogue that significantly improves the management of neuroendocrine tumours (NETs). Octreotide acts through somatostatin receptors (SSTRs). However, the molecular mechanisms leading to successful disease control or symptom management, especially when SSTRs levels are low, are largely unknown. We provide novel insights into how octreotide controls NET cells. CNDT2.5 cells were treated from 1 day up to 16 months with octreotide and then were profiled using Affymetrix microarray analysis. Quantitative real-time PCR and western blot analyses were used to validate microarray profiling in silico data. WST-1 cell proliferation assay was applied to evaluate cell growth of CNDT2.5 cells in the presence or absence of 1 µM octreotide at different time points. Moreover, laser capture microdissected tumour cells and paraffin embedded tissue slides from SI-NETs at different stages of disease were used to identify transcriptional and translational expression. Microarrays analyses did not reveal relevant changes in SSTR expression levels. Unexpectedly, six novel genes were found to be upregulated by octreotide: annexin A1 (ANXA1), rho GTPase-activating protein 18 (ARHGAP18), epithelial membrane protein 1 (EMP1), growth/differentiation factor 15 (GDF15), TGF-beta type II receptor (TGFBR2) and tumour necrosis factor (ligand) superfamily member 15 (TNFSF15). Furthermore, these novel genes were expressed in tumour tissues at transcript and protein levels. We suggest that octreotide may use a potential novel framework to exert its beneficial effect as a drug and to convey its action on neuroendocrine cells. Thus, six novel genes may regulate cell growth and differentiation in normal and tumour neuroendocrine cells and have a role in a novel octreotide mechanism system.

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“…Overall, the greater cellular uptake of the targeted micelles over the non-targeted ones indicated that the KE108-targeting ligand was effective at promoting SSTR-mediated endocytosis, while non-targeted micelles were taken up by the cells through non-specific endocytosis. Notably, besides NE cancers, these KE108-conjugated micelles can also be potentially effective drug delivery vehicles for several other types of cancers that overexpress SSTRs, including breast cancer [49] and melanoma [50]. …”

Section: Resultsmentioning

confidence: 99%

KE108-conjugated unimolecular micelles loaded with a novel HDAC inhibitor thailandepsin-A for targeted neuroendocrine cancer therapy

et al. 2016

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Neuroendocrine (NE) cancers can cause significant patient morbidity. Besides surgery, there are no curative treatments for NE cancers and their metastases, emphasizing the need for the development of other forms of therapy. In this study, multifunctional unimolecular micelles were developed for targeted NE cancer therapy. The unimolecular micelles were formed by multi-arm star amphiphilic block copolymer poly(amidoamine)–poly(valerolactone)–poly(ethylene glycol) conjugated with KE108 peptide and Cy5 dye (abbreviated as PAMAM–PVL–PEG–KE108/Cy5). The unimolecular micelles with a spherical core–shell structure exhibited a uniform size distribution and excellent stability. The hydrophobic drug thailandepsin-A (TDP-A), a recently discovered HDAC inhibitor, was physically encapsulated into the hydrophobic core of the micelles. KE108 peptide, a somatostatin analog possessing high affinity for all five subtypes of somatostatin receptors (SSTR 1–5), commonly overexpressed in NE cancer cells, was used for the first time as an NE cancer targeting ligand. KE108 exhibited superior targeting abilities compared to other common somatostatin analogs, such as octreotide, in NE cancer cell lines. The in vitro assays demonstrated that the TDP-A-loaded, KE108-targeted micelles exhibited the best capabilities in suppressing NE cancer cell growth. Moreover, the in vivo near-infrared fluorescence imaging on NE-tumor-bearing nude mice showed that KE108-conjugated micelles exhibited the greatest tumor accumulation due to their passive targeting and active targeting capabilities. Finally, TDP-A-loaded and KE108-conjugated micelles possessed the best anticancer efficacy without detectable systemic toxicity. Thus, these novel TDP-A-loaded and KE108-conjugated unimolecular micelles offer a promising approach for targeted NE cancer therapy.

show abstract

Expression of Somatostatin Receptors in Human Melanoma Cell Lines: Effect of Two Different Somatostatin Analogues, Octreotide and SOM230, on Cell Proliferation

Cited by 19 publications

References 27 publications

Comparison between F-18 fluorodeoxyglucose and Ga-68 DOTATOC in metastasized melanoma

Comparison between F-18 fluorodeoxyglucose and Ga-68 DOTATOC in metastasized melanoma

The Somatostatin Analogue Octreotide Inhibits Growth of Small Intestine Neuroendocrine Tumour Cells

KE108-conjugated unimolecular micelles loaded with a novel HDAC inhibitor thailandepsin-A for targeted neuroendocrine cancer therapy

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