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 |
- 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
-
Targeting Translation for Treatment of Cancer - A Novel Role for IRES?
Current Cancer Drug Targets The mTOR/4E-BP1/eIF4E Signalling Pathway as a Source of Cancer Drug Targets
Current Medicinal Chemistry Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents
Current Topics in Medicinal Chemistry Natural Compounds as Anticancer Agents Targeting DNA Topoisomerases
Current Genomics Cellular FLICE-Like Inhibitory Protein (C-FLIP): A Novel Target for Cancer Therapy
Current Cancer Drug Targets Inflammaging of Female Reproductive System: A Molecular Landscape
Current Aging Science Biomarkers for Systemic Therapy in Ovarian Cancer
Current Cancer Drug Targets LncRNA HOTAIR as Prognostic Circulating Marker and Potential Therapeutic Target in Patients with Tumor Diseases
Current Drug Targets A Qualitative and Quantitative Study of the Innervation of the Human Non Pregnant Uterus
Current Protein & Peptide Science Understanding Tumor-Antigen Presentation in the New Era of Cancer Immunotherapy
Current Pharmaceutical Design MicroRNAs in Human Diseases
Recent Patents on DNA & Gene Sequences Rapid Non-genomic Vasodilator Actions of Oestrogens and Sex Steroids
Current Medicinal Chemistry HER2-Mediated Anticancer Drug Delivery: Strategies to Prepare Targeting Ligands Highly Specific for the Receptor
Current Medicinal Chemistry DLEU1: A Functional Long Noncoding RNA in Tumorigenesis
Current Pharmaceutical Design The Phosphoinositide 3-Kinase Pathway in Human Cancer: Genetic Alterations and Therapeutic Implications
Current Genomics The Pleiotropic Effects of PPARs on Vascular Cells and Angiogenesis: Implications for Tissue Engineering
Current Stem Cell Research & Therapy Induction of Tumour Cell Senescence: A New Strategy in Anticancer Treatment
Medicinal Chemistry Reviews - Online (Discontinued) In Silico Analysis and Molecular Docking Studies of Novel 6,7-dihydropyrano [2,3-d] pyrimidin-5-one Derivatives as Human Epidermal Growth Factor Receptor 2 (HER2) and Epidermal Growth Factor Receptor (EGFR) Inhibitors
Current Cancer Therapy Reviews Synthesis and Biological Evaluation of the Salicylamide and Salicylic Acid Derivatives as Anti-Estrogen Agents
Medicinal Chemistry A Unique Intracellular, Extracellular and Transmembrane Circulation of Potassium Ions in the Auditory Inner Ear as an Anticarcinogenic Principle? Part 1
Inflammation & Allergy - Drug Targets (Discontinued)