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Radiopharmaceutical development of radiolabelled peptides

Receptor targeting with radiolabelled peptides has become very important in nuclear medicine and oncology in the past few years. The overexpression of many peptide receptors in numerous cancers, compared to their relatively low density in physiological organs, represents the molecular basis for in v... Full description

Journal Title: European journal of nuclear medicine and molecular imaging 2012, Vol.39 (Suppl 1), p.11-30
Main Author: Fani, Melpomeni
Other Authors: Maecke, Helmut R
Format: Electronic Article Electronic Article
Language: English
Subjects:
Publisher: Berlin/Heidelberg: Springer-Verlag
ID: ISSN: 1619-7070
Link: https://www.ncbi.nlm.nih.gov/pubmed/22388624
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recordid: cdi_proquest_journals_928004571
title: Radiopharmaceutical development of radiolabelled peptides
format: Article
creator:
  • Fani, Melpomeni
  • Maecke, Helmut R
subjects:
  • Bombesin
  • Cancer
  • Cardiology
  • Chemical properties
  • Cholecystokinin
  • Drug Design
  • Female
  • Gastrin
  • Gene expression
  • Humans
  • Imaging
  • Implants, Artificial
  • Isotope Labeling - methods
  • Isotopes
  • Male
  • Medicine
  • Medicine & Public Health
  • Neoplasms - diagnostic imaging
  • Neoplasms - radiotherapy
  • Neurons
  • Neuropeptides
  • Nuclear Medicine
  • Oncology
  • Orthopedics
  • Peptides
  • Peptides - chemistry
  • Peptides - isolation & purification
  • Peptides - therapeutic use
  • Pharmaceutical industry
  • Prosthesis
  • Radiology
  • Radionuclide Imaging
  • Radiopharmaceuticals - chemistry
  • Radiopharmaceuticals - isolation & purification
  • Radiopharmaceuticals - therapeutic use
  • Receptors, Peptide - metabolism
  • Review Article
ispartof: European journal of nuclear medicine and molecular imaging, 2012, Vol.39 (Suppl 1), p.11-30
description: Receptor targeting with radiolabelled peptides has become very important in nuclear medicine and oncology in the past few years. The overexpression of many peptide receptors in numerous cancers, compared to their relatively low density in physiological organs, represents the molecular basis for in vivo imaging and targeted radionuclide therapy with radiolabelled peptide-based probes. The prototypes are analogs of somatostatin which are routinely used in the clinic. More recent developments include somatostatin analogs with a broader receptor subtype profile or with antagonistic properties. Many other peptide families such as bombesin, cholecystokinin/gastrin, glucagon-like peptide-1 (GLP-1)/exendin, arginine-glycine-aspartic acid (RGD) etc. have been explored during the last few years and quite a number of potential radiolabelled probes have been derived from them. On the other hand, a variety of strategies and optimized protocols for efficient labelling of peptides with clinically relevant radionuclides such as 99m Tc, M 3+ radiometals ( 111 In, 86/90 Y, 177 Lu, 67/68 Ga), 64/67 Cu, 18 F or radioisotopes of iodine have been developed. The labelling approaches include direct labelling, the use of bifunctional chelators or prosthetic groups. The choice of the labelling approach is driven by the nature and the chemical properties of the radionuclide. Additionally, chemical strategies, including modification of the amino acid sequence and introduction of linkers/spacers with different characteristics, have been explored for the improvement of the overall performance of the radiopeptides, e.g. metabolic stability and pharmacokinetics. Herein, we discuss the development of peptides as radiopharmaceuticals starting from the choice of the labelling method and the conditions to the design and optimization of the peptide probe, as well as some recent developments, focusing on a selected list of peptide families, including somatostatin, bombesin, cholecystokinin/gastrin, GLP-1/exendin and RGD.
language: eng
source:
identifier: ISSN: 1619-7070
fulltext: no_fulltext
issn:
  • 1619-7070
  • 1619-7089
url: Link


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descriptionReceptor targeting with radiolabelled peptides has become very important in nuclear medicine and oncology in the past few years. The overexpression of many peptide receptors in numerous cancers, compared to their relatively low density in physiological organs, represents the molecular basis for in vivo imaging and targeted radionuclide therapy with radiolabelled peptide-based probes. The prototypes are analogs of somatostatin which are routinely used in the clinic. More recent developments include somatostatin analogs with a broader receptor subtype profile or with antagonistic properties. Many other peptide families such as bombesin, cholecystokinin/gastrin, glucagon-like peptide-1 (GLP-1)/exendin, arginine-glycine-aspartic acid (RGD) etc. have been explored during the last few years and quite a number of potential radiolabelled probes have been derived from them. On the other hand, a variety of strategies and optimized protocols for efficient labelling of peptides with clinically relevant radionuclides such as 99m Tc, M 3+ radiometals ( 111 In, 86/90 Y, 177 Lu, 67/68 Ga), 64/67 Cu, 18 F or radioisotopes of iodine have been developed. The labelling approaches include direct labelling, the use of bifunctional chelators or prosthetic groups. The choice of the labelling approach is driven by the nature and the chemical properties of the radionuclide. Additionally, chemical strategies, including modification of the amino acid sequence and introduction of linkers/spacers with different characteristics, have been explored for the improvement of the overall performance of the radiopeptides, e.g. metabolic stability and pharmacokinetics. Herein, we discuss the development of peptides as radiopharmaceuticals starting from the choice of the labelling method and the conditions to the design and optimization of the peptide probe, as well as some recent developments, focusing on a selected list of peptide families, including somatostatin, bombesin, cholecystokinin/gastrin, GLP-1/exendin and RGD.
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subjectBombesin ; Cancer ; Cardiology ; Chemical properties ; Cholecystokinin ; Drug Design ; Female ; Gastrin ; Gene expression ; Humans ; Imaging ; Implants, Artificial ; Isotope Labeling - methods ; Isotopes ; Male ; Medicine ; Medicine & Public Health ; Neoplasms - diagnostic imaging ; Neoplasms - radiotherapy ; Neurons ; Neuropeptides ; Nuclear Medicine ; Oncology ; Orthopedics ; Peptides ; Peptides - chemistry ; Peptides - isolation & purification ; Peptides - therapeutic use ; Pharmaceutical industry ; Prosthesis ; Radiology ; Radionuclide Imaging ; Radiopharmaceuticals - chemistry ; Radiopharmaceuticals - isolation & purification ; Radiopharmaceuticals - therapeutic use ; Receptors, Peptide - metabolism ; Review Article
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descriptionReceptor targeting with radiolabelled peptides has become very important in nuclear medicine and oncology in the past few years. The overexpression of many peptide receptors in numerous cancers, compared to their relatively low density in physiological organs, represents the molecular basis for in vivo imaging and targeted radionuclide therapy with radiolabelled peptide-based probes. The prototypes are analogs of somatostatin which are routinely used in the clinic. More recent developments include somatostatin analogs with a broader receptor subtype profile or with antagonistic properties. Many other peptide families such as bombesin, cholecystokinin/gastrin, glucagon-like peptide-1 (GLP-1)/exendin, arginine-glycine-aspartic acid (RGD) etc. have been explored during the last few years and quite a number of potential radiolabelled probes have been derived from them. On the other hand, a variety of strategies and optimized protocols for efficient labelling of peptides with clinically relevant radionuclides such as 99m Tc, M 3+ radiometals ( 111 In, 86/90 Y, 177 Lu, 67/68 Ga), 64/67 Cu, 18 F or radioisotopes of iodine have been developed. The labelling approaches include direct labelling, the use of bifunctional chelators or prosthetic groups. The choice of the labelling approach is driven by the nature and the chemical properties of the radionuclide. Additionally, chemical strategies, including modification of the amino acid sequence and introduction of linkers/spacers with different characteristics, have been explored for the improvement of the overall performance of the radiopeptides, e.g. metabolic stability and pharmacokinetics. Herein, we discuss the development of peptides as radiopharmaceuticals starting from the choice of the labelling method and the conditions to the design and optimization of the peptide probe, as well as some recent developments, focusing on a selected list of peptide families, including somatostatin, bombesin, cholecystokinin/gastrin, GLP-1/exendin and RGD.
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11Implants, Artificial
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20Neuropeptides
21Nuclear Medicine
22Oncology
23Orthopedics
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25Peptides - chemistry
26Peptides - isolation & purification
27Peptides - therapeutic use
28Pharmaceutical industry
29Prosthesis
30Radiology
31Radionuclide Imaging
32Radiopharmaceuticals - chemistry
33Radiopharmaceuticals - isolation & purification
34Radiopharmaceuticals - therapeutic use
35Receptors, Peptide - metabolism
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date2012-03-03
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issn1619-7070
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abstractReceptor targeting with radiolabelled peptides has become very important in nuclear medicine and oncology in the past few years. The overexpression of many peptide receptors in numerous cancers, compared to their relatively low density in physiological organs, represents the molecular basis for in vivo imaging and targeted radionuclide therapy with radiolabelled peptide-based probes. The prototypes are analogs of somatostatin which are routinely used in the clinic. More recent developments include somatostatin analogs with a broader receptor subtype profile or with antagonistic properties. Many other peptide families such as bombesin, cholecystokinin/gastrin, glucagon-like peptide-1 (GLP-1)/exendin, arginine-glycine-aspartic acid (RGD) etc. have been explored during the last few years and quite a number of potential radiolabelled probes have been derived from them. On the other hand, a variety of strategies and optimized protocols for efficient labelling of peptides with clinically relevant radionuclides such as 99m Tc, M 3+ radiometals ( 111 In, 86/90 Y, 177 Lu, 67/68 Ga), 64/67 Cu, 18 F or radioisotopes of iodine have been developed. The labelling approaches include direct labelling, the use of bifunctional chelators or prosthetic groups. The choice of the labelling approach is driven by the nature and the chemical properties of the radionuclide. Additionally, chemical strategies, including modification of the amino acid sequence and introduction of linkers/spacers with different characteristics, have been explored for the improvement of the overall performance of the radiopeptides, e.g. metabolic stability and pharmacokinetics. Herein, we discuss the development of peptides as radiopharmaceuticals starting from the choice of the labelling method and the conditions to the design and optimization of the peptide probe, as well as some recent developments, focusing on a selected list of peptide families, including somatostatin, bombesin, cholecystokinin/gastrin, GLP-1/exendin and RGD.
copBerlin/Heidelberg
pubSpringer-Verlag
pmid22388624
doi10.1007/s00259-011-2001-z