Abstract
Frequent overexpression of the folate receptor (FR) on a variety of tumor types and on activated macrophages makes this re-ceptor an interesting target for both imaging and therapy of cancer and inflammation. The FR is a glycosylphophatidylinositol-anchored protein that binds the vitamin folic acid with high affinity and internalizes it via endocytosis. In normal tissues and organs, FR-expression is restricted to only a few sites where it is confined to the luminal surface of polarized epithelia and hence does not have access to intra-venously administered folic acid conjugates. Thus, using folic acid as a molecular “Trojan horse” to deliver attached probes to the dis-eased tissue has emerged as a powerful strategy. A variety of folic acid radioconjugates for potential application in nuclear medicine have been developed and (pre)clinically evaluated during the last two decades. Herein we report on folate receptor targeted tracer design and in vitro/in vivo investigations using folic acid -targeted radioconjugates suitable for SPECT and PET imaging as well as for potential therapeutic purposes.
Keywords: Folic acid, folate receptor, imaging, PET, SPECT, targeted radionuclide therapy, cancer, inflammation, macrophages, endocytosis
Current Pharmaceutical Design
Title: Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation
Volume: 18 Issue: 8
Author(s): Cristina Muller
Affiliation:
Keywords: Folic acid, folate receptor, imaging, PET, SPECT, targeted radionuclide therapy, cancer, inflammation, macrophages, endocytosis
Abstract: Frequent overexpression of the folate receptor (FR) on a variety of tumor types and on activated macrophages makes this re-ceptor an interesting target for both imaging and therapy of cancer and inflammation. The FR is a glycosylphophatidylinositol-anchored protein that binds the vitamin folic acid with high affinity and internalizes it via endocytosis. In normal tissues and organs, FR-expression is restricted to only a few sites where it is confined to the luminal surface of polarized epithelia and hence does not have access to intra-venously administered folic acid conjugates. Thus, using folic acid as a molecular “Trojan horse” to deliver attached probes to the dis-eased tissue has emerged as a powerful strategy. A variety of folic acid radioconjugates for potential application in nuclear medicine have been developed and (pre)clinically evaluated during the last two decades. Herein we report on folate receptor targeted tracer design and in vitro/in vivo investigations using folic acid -targeted radioconjugates suitable for SPECT and PET imaging as well as for potential therapeutic purposes.
Export Options
About this article
Cite this article as:
Muller Cristina, Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation, Current Pharmaceutical Design 2012; 18 (8) . https://dx.doi.org/10.2174/138161212799315777
DOI https://dx.doi.org/10.2174/138161212799315777 |
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
-
Natural Compounds as Anticancer Agents Targeting DNA Topoisomerases
Current Genomics The Targets of Curcumin
Current Drug Targets Glycosidated Phospholipids – a Promising Group of Anti-Tumour Lipids
Anti-Cancer Agents in Medicinal Chemistry Identification of Novel Sesamol Dimers with Unusual Methylenedioxy Ring-Opening Skeleton and Evaluation of Their Antioxidant and Cytotoxic Activities
Current Organic Synthesis UPA and PAI-1 Analysis from Fixed Tissues – New Perspectives for a Known Set of Predictive Markers
Current Medicinal Chemistry 10 Years of SELDI: What Have we Learnt?
Current Proteomics Exploring Mechanisms of MicroRNA Downregulation in Cancer
MicroRNA Assessing Drug Transport Across the Human Placental Barrier: From In Vivo and In Vitro Measurements to the Ex Vivo Perfusion Method and In silico Techniques
Current Pharmaceutical Biotechnology Central G-Protein Coupled Receptors (GPCR)s as Molecular Targets for the Treatment of Obesity: Assets, Liabilities and Development Status
Current Drug Targets - CNS & Neurological Disorders Is Metformin a Therapeutic Paradigm for Colorectal Cancer: Insight into the Molecular Pathway?
Current Drug Targets Pharmacologic Activation of p53 by Small-Molecule MDM2 Antagonists
Current Pharmaceutical Design Small Molecular Inhibitors of p-STAT3: Novel Agents for Treatment of Primary and Metastatic CNS Cancers
Recent Patents on CNS Drug Discovery (Discontinued) FOXO Transcription Factors and their Role in Disorders of the Female Reproductive Tract
Current Drug Targets Genetic Susceptibility to Endometrial Cancer
Current Women`s Health Reviews Molecular Targeting Agents in Renal Cell Carcinoma: Present Strategies and Future Perspectives
Current Pharmaceutical Design Induction of Tumour Cell Senescence: A New Strategy in Anticancer Treatment
Medicinal Chemistry Reviews - Online (Discontinued) The Synergistic Effect of Humanized Monoclonal Antibodies Targeting Insulin-Like Growth Factor 1 Receptor (IGF-1R) and Chemotherapy
Current Drug Targets The p53-Estrogen Receptor Loop in Cancer
Current Molecular Medicine Discovery of Selective Probes and Antagonists for G Protein-Coupled Receptors FPR/FPRL1 and GPR30
Current Topics in Medicinal Chemistry Lipids at the Cross-road of Autoimmunity in Multiple Sclerosis
Current Medicinal Chemistry