Abstract
The current way to increase efficacy of cancer therapy is the use of molecular recognition of aberrantly expressed gene products for selective treatment. However, only a fraction of the patients have tumors with a particular molecular target. Radionuclide imaging of molecular targets might help to stratify patient for cancer treatment. Affibody molecules are scaffold proteins, which can be selected for high affinity recognition of proteinaceous molecular targets. The capacity to re-fold under physiological conditions allows labeling of Affibody molecules in a broad range of pH and temperatures with preserved binding properties. Peptide synthesis or introduction of a unique cysteine enables sitespecific labeling of Affibody molecules, resulting in uniform conjugates with well-defined pharmacological characteristics. The small size (7 kDa) of Affibody molecules provides rapid extravasation, rapid tumor penetration, and rapid clearance of unbound tracer from healthy organs and tissues. In combination with sub-nanomolar affinity, this results in high contrast in vivo imaging a few hours after injection. Excellent targeting has been demonstrated in pre-clinical studies with HER2-targeting Affibody molecules labeled with 99mTc and 111In for single photon computed tomography (SPECT), and 18F, 64Cu, 124I and 68Ga for positron emission tomography (PET). Pilot clinical data confirm the high potential of Affibody molecules.
Keywords: Affibody molecules, EGFR, HER2, molecular imaging, radionuclide, scaffold proteins, targeting
Current Pharmaceutical Biotechnology
Title: Radionuclide Molecular Imaging Using Affibody Molecules
Volume: 11 Issue: 6
Author(s): Sara Ahlgren and Vladimir Tolmachev
Affiliation:
Keywords: Affibody molecules, EGFR, HER2, molecular imaging, radionuclide, scaffold proteins, targeting
Abstract: The current way to increase efficacy of cancer therapy is the use of molecular recognition of aberrantly expressed gene products for selective treatment. However, only a fraction of the patients have tumors with a particular molecular target. Radionuclide imaging of molecular targets might help to stratify patient for cancer treatment. Affibody molecules are scaffold proteins, which can be selected for high affinity recognition of proteinaceous molecular targets. The capacity to re-fold under physiological conditions allows labeling of Affibody molecules in a broad range of pH and temperatures with preserved binding properties. Peptide synthesis or introduction of a unique cysteine enables sitespecific labeling of Affibody molecules, resulting in uniform conjugates with well-defined pharmacological characteristics. The small size (7 kDa) of Affibody molecules provides rapid extravasation, rapid tumor penetration, and rapid clearance of unbound tracer from healthy organs and tissues. In combination with sub-nanomolar affinity, this results in high contrast in vivo imaging a few hours after injection. Excellent targeting has been demonstrated in pre-clinical studies with HER2-targeting Affibody molecules labeled with 99mTc and 111In for single photon computed tomography (SPECT), and 18F, 64Cu, 124I and 68Ga for positron emission tomography (PET). Pilot clinical data confirm the high potential of Affibody molecules.
Export Options
About this article
Cite this article as:
Ahlgren Sara and Tolmachev Vladimir, Radionuclide Molecular Imaging Using Affibody Molecules, Current Pharmaceutical Biotechnology 2010; 11 (6) . https://dx.doi.org/10.2174/138920110792246609
DOI https://dx.doi.org/10.2174/138920110792246609 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
Call for Papers in Thematic Issues
Artificial Intelligence in Bioinformatics
Bioinformatics is an interdisciplinary field that analyzes and explores biological data. This field combines biology and information system. Artificial Intelligence (AI) has attracted great attention as it tries to replicate human intelligence. It has become common technology for analyzing and solving complex data and problems and encompasses sub-fields of machine ...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
-
Chitosan and Its Use in Design of Insulin Delivery System
Recent Patents on Drug Delivery & Formulation Stem Cells Derived from Human Exfoliated Deciduous Teeth (SHED) in Neuronal Disorders: A Review
Current Stem Cell Research & Therapy Biomarkers, Critical Disease Pathways, Drug Targets, and Alternative Medicine in Male Breast Cancer
Current Drug Targets Role of Adiponectin in the Metabolic Syndrome: Current Perspectives on its Modulation as a Treatment Strategy
Current Pharmaceutical Design Mycotoxins Levels in Human Milk: A Menace to Infants and Children Health
Current Nutrition & Food Science Hydroxytyrosol and Oleuropein Inhibit Migration and Invasion of MDA-MB-231 Triple-Negative Breast Cancer Cell via Induction of Autophagy
Anti-Cancer Agents in Medicinal Chemistry Recent Advances in Thymidine Kinase 2 (TK2) Inhibitors and New Perspectives for Potential Applications
Current Pharmaceutical Design Subject Index to Volume 3
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Aurora Kinase Inhibitors in Head and Neck Cancer
Current Topics in Medicinal Chemistry Genetic Polymorphisms of ATP-Binding Cassette Transporters ABCB1 and ABCC2 and their Impact on Drug Disposition
Current Drug Targets The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases – Part I
Current Medicinal Chemistry Natural Products Targeting Cancer Stem Cells: A Revisit
Current Medicinal Chemistry Expression Level and Hormonal Regulation of ABC Transporters in Breast Cancer
Current Cancer Therapy Reviews Parp Inhibitors for the Treatment of Ovarian Cancer
Current Cancer Drug Targets The Role of Phospholipase D Enzyme(s) in Modulating Cell Signaling: Implications for Cancer Drug Development
Current Bioactive Compounds miRNA-497 Enhances the Sensitivity of Colorectal Cancer Cells to Neoadjuvant Chemotherapeutic Drug
Current Protein & Peptide Science Reversal of Cardiac Iron Loading and Dysfunction in Thalassemic Mice by Curcuminoids
Medicinal Chemistry The Yin and Yang of microRNA Assay Methods
MicroRNA Hydrogen Sulfide and its Modulation in Arterial Hypertension and Atherosclerosis
Cardiovascular & Hematological Agents in Medicinal Chemistry Nanoparticle Drug Delivery Systems: Recent Patents and Applications in Nanomedicine
Recent Patents on Nanomedicine