Search results for "somatostatin receptor"
showing 10 items of 20 documents
From Bench to Bedside—The Bad Berka Experience With First-in-Human Studies
2019
Precision oncology is being driven by rapid advances in novel diagnostics and therapeutic interventions, with treatments targeted to the needs of individual patients on the basis of genetic, biomarker, phenotypic, or psychosocial characteristics that distinguish a given patient from other patients with similar clinical presentations. Inherent in the theranostics paradigm is the assumption that diagnostic test results can precisely determine whether an individual is likely to benefit from a specific treatment. As part and integral in the current era of precision oncology, theranostics in the context of nuclear medicine aims to identify the appropriate molecular targets in neoplasms (diagnost…
Somatostatin and Somatostatin Receptors: From Signaling to Clinical Applications in Neuroendocrine Neoplasms
2021
Neuroendocrine neoplasms (NENs) are heterogeneous neoplasms which arise from neuroendocrine cells that are distributed widely throughout the body. Although heterogenous, many of them share their ability to overexpress somatostatin receptors (SSTR) on their cell surface. Due to this, SSTR and somatostatin have been a large subject of interest in the discovery of potential biomarkers and treatment options for the disease. The aim of this review is to describe the molecular characteristics of somatostatin and somatostatin receptors and its application in diagnosis and therapy on patients with NENs as well as the use in the near future of somatostatin antagonists.
closo-borane conjugated regulatory peptides retain high biological affinity: synthesis of closo-borane conjugated Tyr(3)-octreotate derivatives for B…
2008
Despite the improvements in cancer therapy during the past years, high-grade gliomas and many other types of cancer are still extremely resistant to current forms of therapy. Boron neutron capture therapy (BNCT) provides a promising way to destroy cancer cells without damaging healthy tissue. However, BNCT in practice is still limited due to the lack of boron-containing compounds that selectively deliver boron to cancer cells. Since many neuroendocrine tumors show an overexpression of the somatostatin receptor, it was our aim to synthesize compounds that contain a large number of boron atoms and still show high affinity toward this transmembrane receptor. The synthetic peptide Tyr (3)-octre…
Instant kit preparation of 68Ga-radiopharmaceuticals via the hybrid chelator DATA: clinical translation of [68Ga]Ga-DATA-TOC
2019
Purpose The widespread use of 68Ga for positron emission tomography (PET) relies on the development of radiopharmaceutical precursors that can be radiolabelled and dispensed in a simple, quick, and convenient manner. The DATA (6-amino-1,4-diazapine-triacetate) scaffold represents a novel hybrid chelator architecture possessing both cyclic and acyclic character that may allow for facile access to 68Ga-labelled tracers in the clinic. We report the first bifunctional DATA chelator conjugated to [Tyr3]octreotide (TOC), a somatostatin subtype 2 receptor (SST2)-targeting vector for imaging and functional characterisation of SSTR2 expressing tumours. Methods The radiopharmaceutical precursor, DATA…
New imaging procedures in thyroid-associated ophthalmopathy
1996
Lymphocytic and other mononuclear cell infiltrations of the retrobulbar space are observed in thyroid-associated ophthalmopathy (TAO). The identification of somatostatin receptors on lymphocytes has provided a rationale for receptor-imaging with the radiolabeled somatostatin analog Octreotide in TAO. Furthermore, previous investigations have shown that quantitative magnetic resonance imaging (MRI) allows non-invasive detection of acute inflammatory changes in extraocular muscles. Therefore, in patients with TAO and controls, scans of the orbits were obtained at 4h and 24h after i.v. injection of the radionuclide and orbital MRI was performed. Compared to controls, patients with TAO showed a…
In Vivo Molecular Imaging of Somatostatin Receptors in Pancreatic Islet Cells and Neuroendocrine Tumors by Miniaturized Confocal Laser-Scanning Fluor…
2010
The aim of the study was to evaluate real time in vivo molecular imaging of somatostatin receptors (sstrs) using a handheld miniaturized confocal laser scan microscope (CLM) in conjunction with fluorescein-labeled octreotate (OcF) in healthy mice and murine models of neuroendocrine tumors. For CLM a small rigid probe (diameter 7 mm) with an integrated single line laser (488 nm) was used (optical slice thickness 7 μm; lateral resolution 0.7 μm). OcF was synthesized via Fmoc solid-phase peptide synthesis and purified by HPLC showing high-affinity binding to the sstr2 (IC50 6.2 nmol). For in vitro evaluation, rat and human pancreatic cancer cells were used and characterized with respect to its…
Molecular imaging of gastroenteropancreatic neuroendocrine tumors.
2010
Somatostatin-receptor scintigraphy has become an obligatory molecular imaging method in the management of patients with neuroendocrine tumors when metastatic disease is suspected. Using positron emission tomography and new somatostatin analogues, sensitivity of somatostatin receptor imaging has further increased. With a combination of morphologic imaging methods, such as hybrid imaging by PET/CT, this method represents the method of choice in many centers and efforts are under way to translate somatostatin receptor imaging onto a cellular level by endoscopic confocal microscopy. Other clinically relevant functional pathways in neuroendocrine tumors that are accessible by PET imaging are glu…
Reporting, interpretation, and extrapolation issues (SPIN) in abstracts of orthodontic meta-analyses published from 2000 to 2020
2021
Summary Aim To assess the prevalence of and identify factors associated with SPIN in abstracts of orthodontic meta-analyses. Materials and methods Electronic search was performed within the contents of five orthodontic journals and the Cochrane Database of Systematic Reviews (CDSR) to identify meta-analyses of studies involving humans, from 1 January 2000 until 31 August 2020. Inclusion of SPIN in the abstract of meta-analyses, defined as misleading reporting, misleading interpretation, and inappropriate extrapolation of the findings, was documented. Extent of SPIN and associations with journal and year of publication, type of study, number of authors, continent of authorship, methodologist…
Control of Gastric Acid Secretion in Somatostatin Receptor 2 Deficient Mice: Shift from Endocrine/Paracrine to Neurocrine Pathways
2007
The gastrin-enterochromaffin-like (ECL) cell-parietal cell axis is known to play an important role in the regulation of gastric acid secretion. Somatostatin, acting on somatostatin receptor type 2 (SSTR2), interferes with this axis by suppressing the activity of the gastrin cells, ECL cells, and parietal cells. Surprisingly, however, freely fed SSTR2 knockout mice seem to display normal circulating gastrin concentration and unchanged acid output. In the present study, we compared the control of acid secretion in these mutant mice with that in wild-type mice. In SSTR2 knockout mice, the number of gastrin cells was unchanged; whereas the numbers of somatostatin cells were reduced in the antru…
111-Indium-DTPA-Octreotid-Szintigraphie bei kolorektalen Lebermetastasen
1997
The somatostatin analogue octreotide is effective in the treatment of neuroendocrine and other tumours. 111-In-labelled DTPA-octreotide scintigraphy is successful in localizing primary neuroendocrine tumours and metastases and other tumours containing somatostatin receptors. An antiproliferative effect of octreotide was also demonstrated for colorectal carcinoma. Since only about 40% of colorectal carcinomas express somatostatin receptors, we tried to establish whether 111-In-labelled DTPA-octreotide scintigraphy is able to reveal the receptor status of liver metastases in patients with colorectal liver metastases. This would be useful in selecting patients for adjuvant therapy studies with…