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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
The somatostatin receptor subtype 5 in neuroendocrine tumours
Joost van der Hoek1, Steven W J Lamberts, Leo J Hofland
1Department of Internal Medicine, Division of Endocrinology, Room Ee530b, Erasmus MC, Dr Molewaterplein 50, 3015 GE Rotterdam, The Netherlands. l.hofland@erasmusmc.nl
Importance Of The Field:
In recent years, scientific work has been intensified to unravel new (patho-) physiological insights, particularly regarding the functional role of somatostatin (SRIF) receptor subtype 5 (sst) and the development of novel sst(5)-targeted SRIF analogues, in order to broaden medical therapeutic opportunities in patients suffering from neuroendocrine diseases.
Areas Covered In This Review:
The scope of this review is primarily focused upon recent insights in sst(5)-receptor physiology, novel sst(5)-targeted treatment options predominantly directed towards pituitary adenomas, and gastroenteropancreatic neuroendocrine tumours.
What The Reader Will Gain:
An understanding of the potential that novel sst(5)-targeted SRIF analogues might have in the medical treatment of Cushing's disease and acromegaly, as demonstrated by translational research, based on pathophysiological data combined with results from clinical trials.
Take Home Message:
The role of targeting sst(5) in gastroenteropancreatic neuroendocrine tumours remains to be established. The sst(5) subtype might function as sst(2) modulator in terms of receptor internalization and desensitization, and seems less important compared with sst(2)-preferring SRIF analogues in the regulation of human insulin secretion by the pancreas. Finally, absence of sst(5) in corticotroph adenomas could be related to tumour aggressiveness in Cushing's disease.
Insights
Novel somatostatin (SRIF) analogues targeting the SRIF receptor subtype 5 (sst5) show potential for treating neuroendocrine diseases like Cushing's disease and acromegaly. Further research is needed to establish sst5's role in gastroenteropancreatic neuroendocrine tumors.
Area of Science:
- Endocrinology
- Oncology
- Pharmacology
Background:
- Intensified research into somatostatin (SRIF) receptor subtype 5 (sst5) physiology and targeted analogues.
- Focus on broadening therapeutic opportunities for neuroendocrine diseases.
Purpose of the Study:
- Review recent insights into sst5 receptor physiology.
- Explore novel sst5-targeted treatment options for pituitary adenomas and gastroenteropancreatic neuroendocrine tumors (GEP-NETs).
Main Methods:
- Literature review focusing on translational research and clinical trial data.
- Analysis of pathophysiological data related to sst5 receptor function.
Main Results:
- Translational research indicates potential of novel sst5-targeted SRIF analogues for Cushing's disease and acromegaly.
- The role of sst5 targeting in GEP-NETs requires further investigation.
Conclusions:
- Sst5 may modulate sst2 receptor activity and appears less critical than sst2 for pancreatic insulin secretion.
- Absence of sst5 in corticotroph adenomas may correlate with Cushing's disease aggressiveness.
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