Abstract
Progress in genomics and proteomics provides clinical oncology with new anti-cancer drugs, which target selectively aberrantly expressed membrane proteins and associated signalling pathways in malignant cells. Molecular targeting also enables specific delivery of cytotoxic substances to tumours sparing healthy tissues. Improved selectivity of the treatment reduces side effects and widens the therapeutic window. However, only a part of the patients might benefit from such treatment due to inter- and intrapatient heterogeneity of therapeutic target expression. This makes it necessary to identify patients, who may benefit from targeting therapy. Radiolabelled peptides can provide selective and sensitive detection of molecular therapeutic targets in both primary tumours and metastases in a single non-invasive procedure, making personalised treatment possible. The choice of detection method (single photon emission tomography or positron emission tomography), radionuclide for labelling and labelling chemistry can appreciably influence the imaging property of a tracer. The labelling method might affect the binding affinity, the cellular processing and retention of a radionuclide, the biodistribution of a targeting peptide, and excretion pathways of a non-bound tracer and radiocatabolites. This influences the sensitivity and specificity of the imaging. This influence is exemplified by three classes of tumour-targeting peptides: somatostatin analogues, bombesin analogues and Affibody molecules. The review suggests approaches for selection of an optimal labelling chemistry.
Keywords: Molecular imaging, cancer, peptides, radionuclide, radiolabelling, biodistribution, PET, SPECT
Current Medicinal Chemistry
Title: Influence of Labelling Methods on Biodistribution and Imaging Properties of Radiolabelled Peptides for Visualisation of Molecular Therapeutic Targets
Volume: 17 Issue: 24
Author(s): V. Tolmachev and A. Orlova
Affiliation:
Keywords: Molecular imaging, cancer, peptides, radionuclide, radiolabelling, biodistribution, PET, SPECT
Abstract: Progress in genomics and proteomics provides clinical oncology with new anti-cancer drugs, which target selectively aberrantly expressed membrane proteins and associated signalling pathways in malignant cells. Molecular targeting also enables specific delivery of cytotoxic substances to tumours sparing healthy tissues. Improved selectivity of the treatment reduces side effects and widens the therapeutic window. However, only a part of the patients might benefit from such treatment due to inter- and intrapatient heterogeneity of therapeutic target expression. This makes it necessary to identify patients, who may benefit from targeting therapy. Radiolabelled peptides can provide selective and sensitive detection of molecular therapeutic targets in both primary tumours and metastases in a single non-invasive procedure, making personalised treatment possible. The choice of detection method (single photon emission tomography or positron emission tomography), radionuclide for labelling and labelling chemistry can appreciably influence the imaging property of a tracer. The labelling method might affect the binding affinity, the cellular processing and retention of a radionuclide, the biodistribution of a targeting peptide, and excretion pathways of a non-bound tracer and radiocatabolites. This influences the sensitivity and specificity of the imaging. This influence is exemplified by three classes of tumour-targeting peptides: somatostatin analogues, bombesin analogues and Affibody molecules. The review suggests approaches for selection of an optimal labelling chemistry.
Export Options
About this article
Cite this article as:
Tolmachev V. and Orlova A., Influence of Labelling Methods on Biodistribution and Imaging Properties of Radiolabelled Peptides for Visualisation of Molecular Therapeutic Targets, Current Medicinal Chemistry 2010; 17 (24) . https://dx.doi.org/10.2174/092986710791859397
DOI https://dx.doi.org/10.2174/092986710791859397 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
- Announcements
Related Articles
-
Immunotoxins and Other Conjugates: Pre-clinical Studies
Mini-Reviews in Medicinal Chemistry Effect of Non-Ionizing Electromagnetic Fields of Anthropic Origin on Male Fertility
Current Chemical Biology Activities of Venom Proteins and Peptides with Possible Therapeutic Applications from Bees and WASPS
Protein & Peptide Letters The Difficulties in the Management of Breast Cancer and Pregnancy
Reviews on Recent Clinical Trials FAK and HAS Inhibition Synergistically Decrease Colon Cancer Cell Viability and Affect Expression of Critical Genes
Anti-Cancer Agents in Medicinal Chemistry Clinical Development of Inhibitors of the Insulin-like Growth Factor Receptor in Oncology
Current Drug Targets Regeneration of the Gastric Mucosa and its Glands from Stem Cells
Current Medicinal Chemistry Radiotherapy in Transitional Cell Carcinoma of Urinary Bladder Cancer –Where Does it Fit Into Treatment Protocol
Current Cancer Therapy Reviews A Comparative Study of Breast Cancer Screening by Age Across 10000 Tunisian Women
Reviews on Recent Clinical Trials Editorial (Thematic Issue: Special Issue on Herbal Medicines and Nano-Drug Delivery Systems)
Current Signal Transduction Therapy Nutlins and Ionizing Radiation in Cancer Therapy
Current Pharmaceutical Design Active Targeting Strategies for Anticancer Drug Nanocarriers
Current Drug Delivery Controlled Release of Growth Factors for Regenerative Medicine
Current Pharmaceutical Design Targeting the NFκB Signaling Pathways for Breast Cancer Prevention and Therapy
Current Medicinal Chemistry The Pattern of Non-AIDS-defining Cancers in the HIV Population: Epidemiology, Risk Factors and Prognosis. A Review
Current HIV Research Molecular Modelling of Berberine Derivatives as Inhibitors of Human Smoothened Receptor and Hedgehog Signalling Pathway Using a Newly Developed Algorithm on Anti-Cancer Drugs
Recent Patents on Anti-Cancer Drug Discovery Protein Kinase CK2 Inhibitors: Emerging Anticancer Therapeutic Agents?
Anti-Cancer Agents in Medicinal Chemistry Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents
Current Topics in Medicinal Chemistry Biosimilar Filgrastim in Autologous Peripheral Blood Hematopoietic Stem Cell Mobilization and Post-Transplant Hematologic Recovery
Current Medicinal Chemistry Optimal Sequencing of New Drugs in Metastatic Castration-Resistant Prostate Cancer: Dream or Reality?
Current Drug Targets