Abstract
The αvβ3 integrin is highly expressed in prostate cancer (PCa), in which it is a key player in tumour invasion, angiogenesis and metastasis formation. Therefore, αvβ3 integrin is considered a very promising target for molecular imaging of PCa. This study tested the potential of the novel αvβ3 integrin affine agent [68Ga]NOTA-RGD in comparison with the established [18F]fluoroethylcholine (FEC) and [18F]fluorodeoxyglucose (FDG) for assessing PCa using positron emission tomography (PET). [68Ga]NOTA-RGD showed a lower uptake in PC-3 and DU-145 cells compared with FEC and FDG. µPET imaging studies showed a good delineation of the PCa xenografts in mice. The means tumor-to-muscleand tumor-to-bone-ratio amounted 5.1 ± 1.4 and 5.2 ± 1.2 for [68Ga]NOTA-RGD compared with 2.6 ± 0.9 and 2.9 ± 1.6 for FDG, and 2.4 ± 0.7 and 0.8 ± 0.2 for FEC, respectively. The uptake of [68Ga]NOTA-RGD into tumor was fully inhibited by c(RGDfV), known to bind specifically to αvβ3 integrin, confirming the specificity of the tumor uptake in vivo. These results suggest that [68Ga]NOTA-RGD is a promising candidate for PET imaging of αvβ3 integrin expression in PCa and warrant further in vivo validations to ascertain its potential as an imaging agent for clinical use. The simple and fast preparation of [68Ga]NOTA-RGD may greatly facilitate its translation to a clinical setting.
Keywords: Angiogenesis, αvβ3 integrin, [68Ga]NOTA-RGD, PET imaging, prostate cancer.
Current Cancer Drug Targets
Title:PET Imaging with [68Ga]NOTA-RGD for Prostate Cancer: A Comparative Study with [18F]Fluorodeoxyglucose and [18F]Fluoroethylcholine
Volume: 14 Issue: 4
Author(s): Ina Israel, Dominik Richter, Jochen Stritzker, Michaela van Ooschot, Ulrike Donat, Andreas K. Buck and Samuel Samnick
Affiliation:
Keywords: Angiogenesis, αvβ3 integrin, [68Ga]NOTA-RGD, PET imaging, prostate cancer.
Abstract: The αvβ3 integrin is highly expressed in prostate cancer (PCa), in which it is a key player in tumour invasion, angiogenesis and metastasis formation. Therefore, αvβ3 integrin is considered a very promising target for molecular imaging of PCa. This study tested the potential of the novel αvβ3 integrin affine agent [68Ga]NOTA-RGD in comparison with the established [18F]fluoroethylcholine (FEC) and [18F]fluorodeoxyglucose (FDG) for assessing PCa using positron emission tomography (PET). [68Ga]NOTA-RGD showed a lower uptake in PC-3 and DU-145 cells compared with FEC and FDG. µPET imaging studies showed a good delineation of the PCa xenografts in mice. The means tumor-to-muscleand tumor-to-bone-ratio amounted 5.1 ± 1.4 and 5.2 ± 1.2 for [68Ga]NOTA-RGD compared with 2.6 ± 0.9 and 2.9 ± 1.6 for FDG, and 2.4 ± 0.7 and 0.8 ± 0.2 for FEC, respectively. The uptake of [68Ga]NOTA-RGD into tumor was fully inhibited by c(RGDfV), known to bind specifically to αvβ3 integrin, confirming the specificity of the tumor uptake in vivo. These results suggest that [68Ga]NOTA-RGD is a promising candidate for PET imaging of αvβ3 integrin expression in PCa and warrant further in vivo validations to ascertain its potential as an imaging agent for clinical use. The simple and fast preparation of [68Ga]NOTA-RGD may greatly facilitate its translation to a clinical setting.
Export Options
About this article
Cite this article as:
Israel Ina, Richter Dominik, Stritzker Jochen, Ooschot van Michaela, Donat Ulrike, Buck K. Andreas and Samnick Samuel, PET Imaging with [68Ga]NOTA-RGD for Prostate Cancer: A Comparative Study with [18F]Fluorodeoxyglucose and [18F]Fluoroethylcholine, Current Cancer Drug Targets 2014; 14 (4) . https://dx.doi.org/10.2174/1568009614666140403123452
DOI https://dx.doi.org/10.2174/1568009614666140403123452 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
-
Novel VEGF-independent Strategies Targeting Tumor Vasculature: Clinical Aspects
Current Pharmaceutical Design Treatment of Estrogen Receptor-Positive Breast Cancer
Current Medicinal Chemistry Delivery Systems for Birch-bark Triterpenoids and their Derivatives in Anticancer Research
Current Medicinal Chemistry Nutraceutical: A Drug, Dietary Supplement and Food Ingredient
Current Pharmacogenomics and Personalized Medicine CXCR4 and CXCL12 Expression in Rectal Tumors of Stage IV Patients Before and After Local Radiotherapy and Systemic Neoadjuvant Treatment
Current Pharmaceutical Design Tamoxifen and its New Derivatives in Cancer Research
Recent Patents on Anti-Cancer Drug Discovery Implications of Nanoscale Based Drug Delivery Systems in Delivery and Targeting Tubulin Binding Agent, Noscapine in Cancer Cells
Current Drug Metabolism Dual Acting Anti-Inflammatory Drugs
Current Topics in Medicinal Chemistry Immunomics in Skin Cancer - Improvement in Diagnosis, Prognosis and Therapy Monitoring
Current Proteomics A Novel Triazole Nucleoside Suppresses Prostate Cancer Cell Growth by Inhibiting Heat Shock Factor 1 and Androgen Receptor
Anti-Cancer Agents in Medicinal Chemistry Aurora-B Kinase Inhibitors for Cancer Chemotherapy
Mini-Reviews in Medicinal Chemistry Use of Corticosteroids in Critically Ill Septic Patients: A Review of Mechanisms of Adrenal Insufficiency in Sepsis and Treatment
Current Drug Targets Dichotomous Life of DNA Binding High Mobility Group Box1 Protein in Human Health and Disease
Current Protein & Peptide Science A 1536-Well Fluorescence Polarization Assay to Screen for Modulators of the MUSASHI Family of RNA-Binding Proteins
Combinatorial Chemistry & High Throughput Screening Perspectives of New Therapies for Endometriosis
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Integrative Exome Sequencing Analysis in Castration-Resistant Prostate Cancer in Chinese Population
Current Pharmaceutical Biotechnology The Role of Glioma Microenvironment in Immune Modulation: Potential Targets for Intervention
Letters in Drug Design & Discovery Oxytocin and Diabetes Mellitus: A Strong Biochemical Relation. Review
Current Diabetes Reviews Epothilones: From Discovery to Clinical Trials
Current Topics in Medicinal Chemistry Preface
Recent Patents on Anti-Cancer Drug Discovery