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Updated: Jul 7, 2026

A Practical Guide for the Production and PET/CT Imaging of 68Ga-DOTATATE for Neuroendocrine Tumors in Daily Clinical Practice
Published on: April 17, 2019
Somatostatin, cortistatin and their receptors in tumours
1Department of Clinical & Biological Sciences, University of Turin at San Luigi Hospital, Orbassano, University of Turin, Torino, Italy.
Abstract:
Somatostatin (SS) and its synthetic analogs have a role in the treatment of neuroendocrine tumours both in terms of symptoms control and antiproliferative activities. These effects are mediated by five SS receptors, widely expressed in both human neuroendocrine and non-neuroendocrine tumours, which were demonstrated to be diagnostically and therapeutically valuable targets. Cortistatin (CST), a brain cortex peptide, partially homologous to SS and having similar functions is also expressed in peripheral tissues and tumours. CST binds all SS receptors, and, differently from SS, also the ghrelin receptor GHSR1a and the CST specific receptor MrgX2. The expression profile of CST is mostly restricted to neuroendocrine tumours (gastrointestinal, pancreas, lung, parathyroid, thyroid, adrenal). In these tumours, CST probably acts via the SS or ghrelin receptor, the MrgX2 receptor being absent. Thus, in comparison to SS analogs, CST synthetic analogs may represent additional diagnostic/therapeutic tools in those tumours expressing the receptors for SS, for ghrelin or for both peptides.
Insights
Somatostatin and Cortistatin analogs offer new diagnostic and therapeutic options for neuroendocrine tumors. Cortistatin shows promise by targeting somatostatin, ghrelin, and its own specific receptors, expanding treatment potential.
Area of Science:
- Endocrinology
- Oncology
- Molecular Biology
Background:
- Somatostatin (SS) and analogs are used for neuroendocrine tumor (NET) symptom control and antiproliferative effects.
- SS receptors are key targets in NET diagnosis and therapy.
- Cortistatin (CST), a peptide homologous to SS, is also found in tumors.
Purpose of the Study:
- To explore the potential of Cortistatin (CST) and its analogs as diagnostic and therapeutic tools for neuroendocrine tumors.
- To compare the receptor binding profiles of SS and CST.
Main Methods:
- Analysis of receptor expression profiles in neuroendocrine tumors.
- Review of known binding affinities of SS and CST to various receptors.
Main Results:
- CST binds to all SS receptors, the ghrelin receptor (GHSR1a), and its specific receptor MrgX2.
- CST expression is primarily observed in neuroendocrine tumors.
- In NETs, CST likely acts via SS or GHSR1a receptors, as MrgX2 is typically absent.
Conclusions:
- CST synthetic analogs may offer additional diagnostic and therapeutic avenues for NETs.
- The distinct receptor binding profile of CST, compared to SS, provides new therapeutic strategies.
- Targeting SS, ghrelin, or both receptors with CST analogs shows potential for personalized NET treatment.
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