BACKGROUND There is a need for novel antitumor agents that demonstrate efficacy in currently refractory tumors without adding to the toxicity of therapy. The somatostatin analogs, which have demonstrated antineoplastic activities in experimental tumor models, and good tolerability and safety profiles are attractive candidates. MATERIALS AND METHODS Data from preclinical studies provide eviden...

Neuroendocrine tumours (NETs) may occur at many sites in the body although the majority occur within the gastroenteropancreatic axis. Non-gastroenteropancreatic NETs encompass phaeochromocytomas and paragangliomas, medullary thyroid carcinoma, anterior pituitary tumour, broncho-pulmonary NETs and parathyroid tumours. Like most endocrine tumours, NETs also express somatostatin (SST) receptors (s...

Hair cells and spiral ganglion neurons of the mammalian auditory system do not regenerate, and their loss leads to irreversible hearing loss. Aminoglycosides induce auditory hair cell death in vitro, and evidence suggests that phosphatidylinositol-3-kinase/Akt signaling opposes gentamicin toxicity via its downstream target, the protein kinase Akt. We previously demonstrated that somatostatin-a ...

Here, we show the modulation of somatostatin functions in the hippocampus by the orally active 'cognition enhancer' GABA(B) receptor antagonist, (3-aminopropyl)n-butylphosphinic acid (CGP-36742), both in vivo and in vitro. Using high-pressure liquid chromatography-coupled electrospray mass spectrometry, we measured a two-fold increase in the extracellular level of somatostatin to CGP-36742 appl...

Somatostatin receptors (SSTRs) are inhibitory G-protein coupled receptors that are ubiquitously expressed in normal and cancer cells. Somatostatins (SST) are the natural ligands for SSTRs and act as inhibitory regulators of hormone secretion and proliferation. Octreotide and RC-160 (vapreotide) are two well tolerated SSTR2/SSTR5 selective somatostatin analogues (SSA) that have been used in the ...

On their plasma membranes, cells express receptor proteins with high affinity for regulatory peptides, such as somatostatin. Changes in the density of these receptors during disease, for example, overexpression in many tumors, provide the basis for new imaging methods. The first peptide analogues successfully applied for visualization of receptor-positive tumors were radiolabeled somatostatin a...

Somatostatin is known to mediate its actions through five G-protein-coupled receptors (sst1-sst5). We have studied the expression of the sst1 receptor in the rat hypothalamus by using a subtype-specific antiserum. In Western blotting, the antiserum reacted specifically with a band with an apparent molecular weight of 80,000 in membranes prepared from hypothalamic tissue. The localization of the...