Abstract
Prostate cancer is one of the most common causes of cancer in men. Evaluating the different stages of prostate cancer with conventional imaging techniques still proves difficult. Nuclear imaging might provide a technique that is able to evaluate prostate cancer, but clinical application has been limited due to lack of accuracy of current radiopharmaceuticals. The development of radiopharmaceuticals that can be targeted to specific antigens, overexpressed in prostate cancer, but sparse in normal tissue, is crucial. Peptides are of particular interest because of their favourable characteristics, leading to increased attention for nuclear imaging of the gastrin-releasing-peptide-receptor (GRPR) with radiolabelled bombesin-like peptides. Several derivatives of bombesin and its truncated form have been prepared for imaging with single photon emission computed tomography (SPECT) or positron emission tomography (PET), thereby delivering potent candidates for further clinical evaluation. This article provides an overview of the development and preclinical evaluation of radiolabelled bombesin analogues for in vivo targeting of GRPR in prostate cancer. The effect of the radionuclide, chelator, spacer and unnatural amino acids on affinity, metabolic stability and image quality are discussed, as well as agonistic or antagonistic properties. Potent candidates are proposed based on these selection criteria: (I) high affinity for GRPR, with rapid and specific tumour uptake (II) high hydrophilicity resulting in the preferred renal-urinary mode of excretion and low hepatobiliary excretion, (III) high stability, but relatively rapid clearance from blood. Also, a summary is made of clinical studies that report on the detection of prostate cancer with GRPR targeted radiopharmaceuticals.
Keywords: Bombesin, GRPR, nuclear imaging, prostate cancer, PET, SPECT
Current Pharmaceutical Design
Title: Nuclear Imaging of Prostate Cancer with Gastrin-Releasing-Peptide- Receptor Targeted Radiopharmaceuticals
Volume: 14 Issue: 28
Author(s): H. J.K. Ananias, I. J. de Jong, R. A. Dierckx, C. van de Wiele, W. Helfrich and P. H. Elsinga
Affiliation:
Keywords: Bombesin, GRPR, nuclear imaging, prostate cancer, PET, SPECT
Abstract: Prostate cancer is one of the most common causes of cancer in men. Evaluating the different stages of prostate cancer with conventional imaging techniques still proves difficult. Nuclear imaging might provide a technique that is able to evaluate prostate cancer, but clinical application has been limited due to lack of accuracy of current radiopharmaceuticals. The development of radiopharmaceuticals that can be targeted to specific antigens, overexpressed in prostate cancer, but sparse in normal tissue, is crucial. Peptides are of particular interest because of their favourable characteristics, leading to increased attention for nuclear imaging of the gastrin-releasing-peptide-receptor (GRPR) with radiolabelled bombesin-like peptides. Several derivatives of bombesin and its truncated form have been prepared for imaging with single photon emission computed tomography (SPECT) or positron emission tomography (PET), thereby delivering potent candidates for further clinical evaluation. This article provides an overview of the development and preclinical evaluation of radiolabelled bombesin analogues for in vivo targeting of GRPR in prostate cancer. The effect of the radionuclide, chelator, spacer and unnatural amino acids on affinity, metabolic stability and image quality are discussed, as well as agonistic or antagonistic properties. Potent candidates are proposed based on these selection criteria: (I) high affinity for GRPR, with rapid and specific tumour uptake (II) high hydrophilicity resulting in the preferred renal-urinary mode of excretion and low hepatobiliary excretion, (III) high stability, but relatively rapid clearance from blood. Also, a summary is made of clinical studies that report on the detection of prostate cancer with GRPR targeted radiopharmaceuticals.
Export Options
About this article
Cite this article as:
Ananias J.K. H., de Jong J. I., Dierckx A. R., de Wiele van C., Helfrich W. and Elsinga H. P., Nuclear Imaging of Prostate Cancer with Gastrin-Releasing-Peptide- Receptor Targeted Radiopharmaceuticals, Current Pharmaceutical Design 2008; 14 (28) . https://dx.doi.org/10.2174/138161208786404335
DOI https://dx.doi.org/10.2174/138161208786404335 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Isoprenylation of Intracellular Proteins as a New Target for the Therapy of Human Neoplasms: Preclinical and Clinical Implications
Current Drug Targets Pharmacology of TRP Channels in the Vasculature
Current Vascular Pharmacology Chemokines as Pharmacological Targets
Mini-Reviews in Medicinal Chemistry bHLH Transcription Factors Inhibitors for Cancer Therapy: General Features for In Silico Drug Design
Current Medicinal Chemistry Is there a Potential Immune Dysfunction with Anabolic Androgenic Steroid Use?: A Review
Mini-Reviews in Medicinal Chemistry Dual Carbonic Anhydrase - Cyclooxygenase-2 Inhibitors
Current Topics in Medicinal Chemistry A Review on the Monoacylglycerol Lipase: At the Interface Between Fat and Endocannabinoid Signalling
Current Medicinal Chemistry Recent Developments in Receptor-Selective Retinoids
Current Pharmaceutical Design Gut Permeability and Microbiota in Parkinson’s Disease: Role of Depression, Tryptophan Catabolites, Oxidative and Nitrosative Stress and Melatonergic Pathways
Current Pharmaceutical Design Characterization of Stem-Like Cells Directly Isolated from Freshly Resected Laryngeal Squamous Cell Carcinoma Specimens
Current Stem Cell Research & Therapy Hitting the Golden TORget: Curcumin’s Effects on mTOR Signaling
Anti-Cancer Agents in Medicinal Chemistry IGF-1 Gene Therapy as a Potentially Useful Therapy for Spontaneous Prolactinomas in Senile Rats
Current Gene Therapy Streamlined In Vivo Selection and Screening of Human Prostate Carcinoma Avid Phage Particles for Development of Peptide Based In Vivo Tumor Imaging Agents
Combinatorial Chemistry & High Throughput Screening The Use of Nimesulide and Its Analogues in Cancer Chemoprevention
Anti-Cancer Agents in Medicinal Chemistry Membrane Transporters as Determinants of the Pharmacology of Platinum Anticancer Drugs
Current Cancer Drug Targets Safety and Side Effects of Cannabidiol, a Cannabis sativa Constituent
Current Drug Safety Recent Updates on the Therapeutic Potential of HER2 Tyrosine Kinase Inhibitors for the Treatment of Breast Cancer
Current Cancer Drug Targets Cancer Kinases and its Novel Inhibitors: Past, Present and Future Challenges
Current Drug Targets Hepatocyte Growth Factor is a Potential Lymphangiogenic Factor; Clinical Implications
Current Signal Transduction Therapy New Therapeutic Strategies for Castration-Resistant Prostate Cancer
Recent Patents on Anti-Cancer Drug Discovery