Radiolabeled peptides: valuable tools for the detection and treatment of cancer.
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TLDR
Recent developments in the field of small peptides, and their applications in the diagnosis and treatment of cancer are presented.Abstract:
Human cancer cells overexpress many peptide receptors as molecular targets. Radiolabeled peptides that bind with high affinity and specificity to the receptors on tumor cells hold great potential for both diagnostic imaging and targeted radionuclide therapy. The advantage of solid-phase peptide synthesis, the availability of different chelating agents and prosthetic groups and bioconjugation techniques permit the facile preparation of a wide variety of peptide-based targeting molecules with diverse biological and tumor targeting properties. Some of these peptides, including somatostatin, bombesin, vasoactive intestinal peptide, gastrin, neurotensin, exendin and RGD are currently under investigation. It is anticipated that in the near future many of these peptides may find applications in nuclear oncology. This article presents recent developments in the field of small peptides, and their applications in the diagnosis and treatment of cancer.read more
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References
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Treatment With the Radiolabeled Somatostatin Analog [177Lu-DOTA0,Tyr3]Octreotate: Toxicity, Efficacy, and Survival
Dik J. Kwekkeboom,Wouter W. de Herder,Boen L. Kam,Casper H.J. van Eijck,Martijn van Essen,P. P. M. Kooij,Richard A Feelders,Maarten O. van Aken,Eric P. Krenning +8 more
TL;DR: Treatment with peptide receptor radionuclide therapy with the radiolabeled somatostatin analog [(177)Lu-DOTA(0),Tyr(3)]octreotate has few adverse effects and compares favorably to the limited number of alternative treatment modalities.
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Peptide receptors as molecular targets for cancer diagnosis and therapy.
TL;DR: 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.
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Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use.
Jean Claude Reubi,Jean-Claude Schär,Beatrice Waser,Sandra Wenger,A. Heppeler,Jörg S. Schmitt,Helmut R. Mäcke +6 more
TL;DR: 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.
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Radiolabeled Somatostatin Analog [177Lu-DOTA0,Tyr3]Octreotate in Patients With Endocrine Gastroenteropancreatic Tumors
Dik J. Kwekkeboom,Jaap J.M. Teunissen,Willem H. Bakker,P. P. M. Kooij,Wouter W. de Herder,Richard A Feelders,Casper H.J. van Eijck,Jan-Paul Esser,Boen L. Kam,Eric P. Krenning +9 more
TL;DR: Treatment with 177Lu-octreotate results in tumor remission in a high percentage of patients with GEP tumors, and results are better in patients with a limited tumor load.
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Localisation of endocrine-related tumours with radioiodinated analogue of somatostatin
Eric P. Krenning,Wouter A.P. Breeman,P. P. M. Kooij,Johan S. Laméris,Willem H. Bakker,Jan W. Koper,L. Ausema,Jean Claude Reubi,S. W. J. Lamberts +8 more
TL;DR: Radioiodinated tyr-3-octreotide can label somatostatin receptors in endocrine-related tumours in vivo and can therefore be used for tumour localisation.