The somatostatin receptor subtype 5 in neuroendocrine tumours
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 sst5-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 sst5-receptor physiology, novel sst5-targeted treatment options predominantly directed towards pituitary adenomas, and gastroenteropancreatic neuroendocrine tumours. What the reader will gain: An understanding of the potential that novel sst5-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 sst5 in gastroenteropancreatic neuroendocrine tumours remains to be established. The sst5 subtype might function as sst2 modulator in terms of receptor internalization and desensitization, and seems less important compared with sst2-preferring SRIF analogues in the regulation of human insulin secretion by the pancreas. Finally, absence of sst5 in corticotroph adenomas could be related to tumour aggressiveness in Cushing's disease.
|Keywords||ACTH secreting adenoma, Acromegaly, Cushing disease, Cushing's, GEP tumours, Glucose, IC 50, L 779976, Pasireotide, acromegaly, adrenal tumor, angiopeptin, bim 23 a 760, bim 23206, bim 23244, bim 23268, binding affinity, clinical trial, desensitization, dextro phenylalanylphenylalanylphenylalanyl dextro tryptophyllysylthreonylphenylalanylthreoninamide, endocrine tumor, glucose, glucose blood level, human, human insulin, hyperglycemia, hypophysis adenoma, insulin, insulin blood level, insulin release, l 817818, messenger RNA, non functioning hypophysis adenoma, nonhuman, octreotide, pancreas, pasireotide, prolactinoma, protein expression, protein function, regulatory mechanism, review, somatostatin, somatostatin derivative, somatostatin receptor, somatostatin receptor 5, thyrotropin, treatment outcome, unclassified drug|
|Persistent URL||dx.doi.org/10.1517/13543781003604710, hdl.handle.net/1765/19479|
|Journal||Expert Opinion on Investigational Drugs: authoritative analysis of R&D trends|
van der Hoek, J, Lamberts, S.W.J, & Hofland, L.J. (2010). The somatostatin receptor subtype 5 in neuroendocrine tumours. Expert Opinion on Investigational Drugs: authoritative analysis of R&D trends, 19(3), 385–399. doi:10.1517/13543781003604710