Illuminating somatostatin analog action at neuroendocrine tumor receptors

Reubi, Jean-Claude; Schonbrunn, Agnes (2013). Illuminating somatostatin analog action at neuroendocrine tumor receptors. Trends in Pharmacological Sciences, 34(12), pp. 676-688. Elsevier 10.1016/j.tips.2013.10.001

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Somatostatin analogs for the diagnosis and therapy of neuroendocrine tumors (NETs) have been used in clinical applications for more than two decades. Five somatostatin receptor subtypes have been identified and molecular mechanisms of somatostatin receptor signaling and regulation have been elucidated. These advances increased understanding of the biological role of each somatostatin receptor subtype, their distribution in NETs, as well as agonist-specific regulation of receptor signaling, internalization, and phosphorylation, particularly for the sst2 receptor subtype, which is the primary target of current somatostatin analog therapy for NETs. Various hypotheses exist to explain differences in patient responsiveness to somatostatin analog inhibition of tumor secretion and growth as well as differences in the development of tumor resistance to therapy. In addition, we now have a better understanding of the action of both first generation (octreotide, lanreotide, Octreoscan) and second generation (pasireotide) FDA-approved somatostatin analogs, including the biased agonistic character of some agonists. The increased understanding of somatostatin receptor pharmacology provides new opportunities to design more sophisticated assays to aid the future development of somatostatin analogs with increased efficacy.

Item Type:

Journal Article (Review Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Reubi-Kattenbusch, Jean-Claude

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

1873-3735

Publisher:

Elsevier

Language:

English

Submitter:

Andrea Arnold

Date Deposited:

02 Apr 2014 15:41

Last Modified:

10 Oct 2019 15:07

Publisher DOI:

10.1016/j.tips.2013.10.001

PubMed ID:

24183675

Uncontrolled Keywords:

sst receptors, octreotide, lanreotide, pasireotide

URI:

https://boris.unibe.ch/id/eprint/46328

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