Abstract
During the past decade, radiolabeled receptor-binding peptides have emerged as an important class of radiopharmaceuticals for tumor diagnosis and therapy. The specific receptor binding property of the ligand can be exploited by labeling the ligand with a radionuclide and using the radiolabeled ligand as a vehicle to guide the radioactivity to the tissues expressing a particular receptor. The concept of using radiolabeled receptor binding peptides to target receptor-expressing tissues in vivo has stimulated a large body of research in nuclear medicine. Receptor binding peptides labeled with gamma emitters (123I, 111In, 99mTc) can visualize receptor-expressing tissues, a technique referred to as peptide-receptor radionuclide imaging (PRRI). In addition, labeled with beta emitters (131I, 90Y, 188Re, 177Lu) these peptides have the potential to irradiate receptor-expressing tissues, an approach referred to as peptide-receptor radionuclide therapy (PRRT). The first and most succesful imaging agent to date is the somatostatin analog octreotide. It is used for somatostatin receptor scintigraphy and PRRT of neuroendocrine tumors. Other peptides such as Minigastrin, GLP-1, CCK, bombesin, substance P, neurotensin, and RGD peptides are currently under development or undergoing clinical trials. In this review, an overview of the criteria of peptide ligand development, the selection of radioisotopes, labeling methods, and chemical aspects of radiopeptide synthesis is given. In addition, the current state of clinical use of radiopeptides for diagnosis and therapy of tumors is discussed.
Keywords: Peptides, chelators, radionuclides, radiolabeling, tumor targeting, imaging, radionuclide therapy
Anti-Cancer Agents in Medicinal Chemistry
Title: Development and Application of Peptide-Based Radiopharmaceuticals
Volume: 7 Issue: 5
Author(s): Ingrid Dijkgraaf, Otto C. Boerman, Wim J.G. Oyen, Frans H.M. Corstens and Martin Gotthardt
Affiliation:
Keywords: Peptides, chelators, radionuclides, radiolabeling, tumor targeting, imaging, radionuclide therapy
Abstract: During the past decade, radiolabeled receptor-binding peptides have emerged as an important class of radiopharmaceuticals for tumor diagnosis and therapy. The specific receptor binding property of the ligand can be exploited by labeling the ligand with a radionuclide and using the radiolabeled ligand as a vehicle to guide the radioactivity to the tissues expressing a particular receptor. The concept of using radiolabeled receptor binding peptides to target receptor-expressing tissues in vivo has stimulated a large body of research in nuclear medicine. Receptor binding peptides labeled with gamma emitters (123I, 111In, 99mTc) can visualize receptor-expressing tissues, a technique referred to as peptide-receptor radionuclide imaging (PRRI). In addition, labeled with beta emitters (131I, 90Y, 188Re, 177Lu) these peptides have the potential to irradiate receptor-expressing tissues, an approach referred to as peptide-receptor radionuclide therapy (PRRT). The first and most succesful imaging agent to date is the somatostatin analog octreotide. It is used for somatostatin receptor scintigraphy and PRRT of neuroendocrine tumors. Other peptides such as Minigastrin, GLP-1, CCK, bombesin, substance P, neurotensin, and RGD peptides are currently under development or undergoing clinical trials. In this review, an overview of the criteria of peptide ligand development, the selection of radioisotopes, labeling methods, and chemical aspects of radiopeptide synthesis is given. In addition, the current state of clinical use of radiopeptides for diagnosis and therapy of tumors is discussed.
Export Options
About this article
Cite this article as:
Dijkgraaf Ingrid, Boerman C. Otto, Oyen J.G. Wim, Corstens H.M. Frans and Gotthardt Martin, Development and Application of Peptide-Based Radiopharmaceuticals, Anti-Cancer Agents in Medicinal Chemistry 2007; 7 (5) . https://dx.doi.org/10.2174/187152007781668733
DOI https://dx.doi.org/10.2174/187152007781668733 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Emergency Services: A Birds Eye Perspective on the Many Different Functions of Stress Proteins
Current Protein & Peptide Science Applied Computational Techniques on Schizophrenia Using Genetic Mutations
Current Topics in Medicinal Chemistry Platelet Biomarkers in Tumor Growth
Current Proteomics Recombinant Human Insulin-Like Growth Factor-1: A New Cardiovascular Disease Treatment Option?
Cardiovascular & Hematological Agents in Medicinal Chemistry Chemoinformatics in Multi-target Drug Discovery for Anti-cancer Therapy: In Silico Design of Potent and Versatile Anti-brain Tumor Agents
Anti-Cancer Agents in Medicinal Chemistry Molecular Genetics and Biomarkers of Polyglutamine Diseases
Current Molecular Medicine Rate Limiting Steps of AAV Transduction and Implications for Human Gene Therapy
Current Gene Therapy Biologically Active Selenophenes and Benzo[b]selenophenes
Current Organic Synthesis Chemical Composition and Biological Activity of Essential Oils of Cumin and Coriander Fruits from Egypt
The Natural Products Journal Polymeric Nano-Encapsulation of Curcumin Enhances its Anti-Cancer Activity in Breast (MDA-MB231) and Lung (A549) Cancer Cells Through Reduction in Expression of HIF-1α and Nuclear p65 (Rel A)
Current Drug Delivery Meet Our Editorial Board Member
Current Cancer Therapy Reviews Meet the Editorial Board
Anti-Cancer Agents in Medicinal Chemistry Vitamin D and Acute Respiratory Tract Infection
Current Respiratory Medicine Reviews Trichinella spiralis and Tumors: Cause, Coincidence or Treatment?
Anti-Cancer Agents in Medicinal Chemistry The Potential of Natural Products as Effective Treatments for Allergic Inflammation: Implications for Allergic Rhinitis
Current Topics in Medicinal Chemistry Angiogenesis Inhibitors: Implications for Combination with Conventional Therapies
Current Pharmaceutical Design Book Review
Current Cancer Drug Targets The DREAM of Pain Relief
Current Rheumatology Reviews AGE-RAGE System and Carcinogenesis
Current Pharmaceutical Design Canonical and Non-Canonical Barriers Facing AntimiR Cancer Therapeutics
Current Medicinal Chemistry