Somatostatin receptors: from signaling to clinical practice.

Abstract

Somatostatin is a peptide with a potent and broad antisecretory action, which makes it an invaluable drug target for the pharmacological management of pituitary adenomas and neuroendocrine tumors. Somatostatin receptors (SSTR1, 2A and B, 3, 4 and 5) belong to the G protein coupled receptor family and have a wide expression pattern in both normal tissues and solid tumors. Investigating the function of each SSTR in several tumor types has provided a wealth of information about the common but also distinct signaling cascades that suppress tumor cell proliferation, survival and angiogenesis. This provided the rationale for developing multireceptor-targeted somatostatin analogs and combination therapies with signaling-targeted agents such as inhibitors of the mammalian (or mechanistic) target of rapamycin (mTOR). The ability of SSTR to internalize and the development of rabiolabeled somatostatin analogs have improved the diagnosis and treatment of neuroendocrine tumors.

• Authors: Marily Theodoropoulou, Günter K Stalla
• Journal: Frontiers in neuroendocrinology (Front Neuroendocrinol) Vol. 34 Issue 3 Pg. 228-52 (Aug 2013) ISSN: 1095-6808 [Electronic] United States
• PMID: 23872332 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
• Copyright: Copyright © 2013 Elsevier Inc. All rights reserved.

Chemical References

• PTR 3173
• Peptides, Cyclic
• Radiopharmaceuticals
• Receptors, Somatostatin
• SSTR2 protein, human
• somatostatin receptor type 1
• lanreotide
• Somatostatin
• pasireotide
• MTOR protein, human
• TOR Serine-Threonine Kinases
• TBR-760
• Octreotide
• Dopamine

Topics

• Animals
• Carcinoma, Neuroendocrine (diagnosis, drug therapy)
• Cell Proliferation (drug effects)
• Dopamine (analogs & derivatives, therapeutic use)
• Humans
• Octreotide (therapeutic use)
• Peptides, Cyclic (therapeutic use)
• Radiopharmaceuticals
• Receptors, Somatostatin (drug effects, physiology)
• Signal Transduction (drug effects)
• Somatostatin (adverse effects, analogs & derivatives, therapeutic use)
• TOR Serine-Threonine Kinases (antagonists & inhibitors)