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Epigenetic regulation of somatostatin and somatostatin receptors in neuroendocrine tumors and other types of cancer.
Open accessAbstract
Both somatostatin (SST) and somatostatin receptors (SSTRs) are proteins with important functions in both physiological tissue and in tumors, particularly in neuroendocrine tumors (NETs). NETs are frequently characterized by high SSTRs expression levels. SST analogues (SSAs) that bind and activate SSTR have anti-proliferative and anti-secretory activity, thereby reducing both the growth as well as the hormonal symptoms of NETs. Moreover, the high expression levels of SSTR type-2 (SSTR2) in NETs is a powerful target for therapy with radiolabeled SSAs. Due to the important role of both SST and SSTRs, it is of great importance to elucidate the mechanisms involved in regulating their expression in NETs, as well as in other types of tumors. The field of epigenetics recently gained interest in NET research, highlighting the importance of this process in regulating the expression of gene and protein expression. In this review we will discuss the role of the epigenetic machinery in controlling the expression of both SSTRs and the neuropeptide SST. Particular attention will be given to the epigenetic regulation of these proteins in NETs, whereas the involvement of the epigenetic machinery in other types of cancer will be discussed as well. In addition, we will discuss the possibility to target enzymes involved in the epigenetic machinery to modify the expression of the SST-system, thereby possibly improving therapeutic options.
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Most PRRTs using radiolabeled SSAs and antagonists have until now depended substantially on the most prominently expressed SSTR2.
“Most PRRTs using radiolabeled SSAs and antagonists has until now depended substantially on the most prominently expressed SSTR2 (142).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [142]
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Metadata
- Authors
- Klomp, M. J., Dalm, S. U., de Jong, M., Feelders, R. A., Hofland, J., & Hofland, L. J.
- Affiliations
- Erasmus MC (NL)
- Corresponding author
- Hofland, J.
- Hofland, L.J.
- Venue
- Reviews in Endocrine and Metabolic Disorders
- Published
- 2020-10-21
- Volume
- 22
- Issue
- 3
- Pages
- 495-510
- ISSN
- 1389-9155 (ISSN-L)
- 1573-2606
- PMC
- PMC8346415
- OpenAlex
- W3094440986
- Cited by
- 69
- References
- 114
- Citations by year
- 2026: 7 · 2025: 13 · 2024: 13 · 2023: 14 · 2022: 15 · 2021: 6 · 2020: 1
- FWCI
- 1.32
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Locations
- Reviews in Endocrine and Metabolic Disorders (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion, other-oa)
- Funders
- Mrace Grant 2017
- Topics
- Health Sciences › Medicine › Oncology › Neuroendocrine Tumor Research Advances
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
- Keywords
- somatostatin, somatostatin receptors, somatostatin receptor 2, neuroendocrine tumors, epigenetic regulation, gene expression regulation, somatostatin analogues, radiolabeled somatostatin analogues, cancer
- MeSH terms
- Humans, Somatostatin, Receptors, Somatostatin, Neuroendocrine Tumors, Epigenesis, Genetic
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