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Affinity profiles for human somatostatin receptor subtypes SST1–SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use
In vivo somatostatin receptor scintigraphy using Octreoscan is a valuable method for the visualisation of human endocrine tumours and their metastases and small structural modifications, chelator substitution or metal replacement were shown to considerably affect the binding affinity. Expand
Peptide receptors as molecular targets for cancer diagnosis and therapy.
- J. Reubi
- Endocrine reviews
- 1 August 2003
The paradigmatic peptide somatostatin and its receptors are extensively reviewed in the light of in vivo targeting of neuroendocrine tumors and the role of the more recently described targeting peptides vasoactive intestinal peptides, gastrin-releasing peptide, and cholecystokinin/gastrin is discussed. Expand
Somatostatin receptor scintigraphy with [111In-DTPA-d-Phe1]- and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients
- E. Krenning, D. Kwekkeboom, +12 authors S. Lamberts
- European Journal of Nuclear Medicine
- 1 August 1993
The successful application of radiolabelled octreotide in scintigraphy indicates the possible usefulness of other radiolABelled peptides, either native peptides or derivatives of these, in, for example, nuclear oncology. Expand
The VPAC2 Receptor Is Essential for Circadian Function in the Mouse Suprachiasmatic Nuclei
Mice carrying a null mutation of the VPAC(2) receptor for VIP and PACAP (Vipr2(-/-)) are incapable of sustaining normal circadian rhythms of rest/activity behavior and the role of intercellular neuropeptidergic signaling in maintenance of circadian function within the SCN is highlighted. Expand
Somatostatin receptor sst1–sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands
It is concluded that sst2, with high affinity for current radiopharmaceuticals such as Octreoscan, is predominantly expressed in a majority of tumours, and suggests the existence of an as yet unknown subtype in selected tumours. Expand
Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting
This review summarises the investigations of the concomitant expression of 13 different peptide receptors, in more than 100 neuroendocrine tumours of the human intestine, pancreas and lung, using in vitro receptor autoradiography with subtype-selective ligands and reveals a characteristic receptor pattern in several tumour types. Expand
Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation.
A massive GRP receptor overexpression in prostate tissues that are neoplastically transformed or, like prostatic intraepithelial neoplasias, are in the process of malignant transformation is demonstrated. Expand
Guidelines for the Diagnosis and Treatment of Neuroendocrine Gastrointestinal Tumours
Guidelines for the diagnosis and treatment of neuroendocrine gastrointestinal tumours. A consensus statement on behalf of the European Neuroendocrine Tumour Society (ENETS).
Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals?
- P. Antunes, M. Ginj, +4 authors H. Maecke
- Chemistry, Medicine
- European Journal of Nuclear Medicine and…
- 16 January 2007
This study demonstrates that 67/68Ga-DOTA-octapeptides show distinctly better preclinical, pharmacological performances than the 111In-labelled peptides, especially on sst2-expressing cells and the corresponding animal models, and may be excellent candidates for further development for clinical studies. Expand