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Open AccessJournal ArticleDOI

Radiolabeled peptides: valuable tools for the detection and treatment of cancer.

Melpomeni Fani, +2 more
- 01 Jan 2012 - 
- Vol. 2, Iss: 5, pp 481-501
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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.

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Citations
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Fluorine-18 radiochemistry, labeling strategies and synthetic routes.

TL;DR: The current radiosynthesis routes and strategies for 18F labeling of small molecules and biomolecules are described and the need for simple and efficient 18F-labeling procedures is described.
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The ubiquitous DOTA and its derivatives: the impact of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid on biomedical imaging

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References
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Journal ArticleDOI

Treatment With the Radiolabeled Somatostatin Analog [177Lu-DOTA0,Tyr3]Octreotate: Toxicity, Efficacy, and Survival

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.
Journal ArticleDOI

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.

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.
Journal ArticleDOI

Radiolabeled Somatostatin Analog [177Lu-DOTA0,Tyr3]Octreotate in Patients With Endocrine Gastroenteropancreatic Tumors

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.
Journal ArticleDOI

Localisation of endocrine-related tumours with radioiodinated analogue of somatostatin

TL;DR: Radioiodinated tyr-3-octreotide can label somatostatin receptors in endocrine-related tumours in vivo and can therefore be used for tumour localisation.
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