Abstract
The failure of solid tumors to respond to chemotherapy is a complicated and clinically frustrating issue. The ability to predict which tumors will respond to treatment could reduce the human and monetary costs of cancer therapy by allowing pro-active selection of a chemotherapeutic to which the tumor does not express resistance. PET/CT imaging with a radiolabeled form of paclitaxel, F-18 fluoropaclitaxel (FPAC), may be able to predict the uptake of paclitaxel in solid tumors, and as a substrate of P-glycoprotein, it may also predict which tumors exhibit multidrug resistance (MDR), a phenotype in which tumors fail to respond to a wide variety of chemically unrelated chemotherapeutic agents. This article reviews the synthetic, preclinical and early human data obtained during the development phase of this promising new radiopharmaceutical.
Keywords: Drug development, Molecular Imaging, F-18 fluoropaclitaxel, Multidrug resistance, Paclitaxel, PET, Pgp, PET Imaging, 18F-Fluoropaclitaxel, P-glycoprotein, Tumor cells, chemotherapeutic agent, ABC (ATP Binding Cassette), Pgp expression, Cytochrome p450, Taxus brevifolia, Taxus baccata, Docetaxel, b-tubulin, Phenylisoserine moiety, [99mTc] sestamibi, [99mTc] tetrofosmin, tariquidar, XR9576, microPET, Pgp inhibitor, [18F]FPAC DMSO, Human breast tumor cell line, Standardized uptake value, MCF tumors, MIRDOSE, MDR modulator, Pgp modulation
Current Topics in Medicinal Chemistry
Title: PET Imaging of Multidrug Resistance in Tumors Using 18F-Fluoropaclitaxel
Volume: 10 Issue: 17
Author(s): Karen A. Kurdziel and Dale O. Kiesewetter
Affiliation:
Keywords: Drug development, Molecular Imaging, F-18 fluoropaclitaxel, Multidrug resistance, Paclitaxel, PET, Pgp, PET Imaging, 18F-Fluoropaclitaxel, P-glycoprotein, Tumor cells, chemotherapeutic agent, ABC (ATP Binding Cassette), Pgp expression, Cytochrome p450, Taxus brevifolia, Taxus baccata, Docetaxel, b-tubulin, Phenylisoserine moiety, [99mTc] sestamibi, [99mTc] tetrofosmin, tariquidar, XR9576, microPET, Pgp inhibitor, [18F]FPAC DMSO, Human breast tumor cell line, Standardized uptake value, MCF tumors, MIRDOSE, MDR modulator, Pgp modulation
Abstract: The failure of solid tumors to respond to chemotherapy is a complicated and clinically frustrating issue. The ability to predict which tumors will respond to treatment could reduce the human and monetary costs of cancer therapy by allowing pro-active selection of a chemotherapeutic to which the tumor does not express resistance. PET/CT imaging with a radiolabeled form of paclitaxel, F-18 fluoropaclitaxel (FPAC), may be able to predict the uptake of paclitaxel in solid tumors, and as a substrate of P-glycoprotein, it may also predict which tumors exhibit multidrug resistance (MDR), a phenotype in which tumors fail to respond to a wide variety of chemically unrelated chemotherapeutic agents. This article reviews the synthetic, preclinical and early human data obtained during the development phase of this promising new radiopharmaceutical.
Export Options
About this article
Cite this article as:
A. Kurdziel Karen and O. Kiesewetter Dale, PET Imaging of Multidrug Resistance in Tumors Using 18F-Fluoropaclitaxel, Current Topics in Medicinal Chemistry 2010; 10 (17) . https://dx.doi.org/10.2174/156802610792928077
DOI https://dx.doi.org/10.2174/156802610792928077 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Synthesis and Biological Activities of Naturally Functionalized Polyamines: An Overview
Current Medicinal Chemistry Mechanical Imaging - a Technology for 3-D Visualization and Characterization of Soft Tissue Abnormalities: A Review
Current Medical Imaging Effect of Non-Steroidal Anti-Inflammatory Drugs on Bone Turnover: An Evidence-Based Review
Reviews on Recent Clinical Trials Synthesis and Cytotoxic Activity of New β-Carboline Derivatives
Mini-Reviews in Medicinal Chemistry Partners in Crime: NGF and BDNF in Visceral Dysfunction
Current Neuropharmacology Network Pharmacology Strategies Toward Multi-Target Anticancer Therapies: From Computational Models to Experimental Design Principles
Current Pharmaceutical Design Treatment Strategies for Fatty Liver Diseases
Reviews on Recent Clinical Trials An Update on MDMX and Dual MDM2/X Inhibitors
Current Topics in Medicinal Chemistry Genetic Polymorphisms of Drug Metabolizing Enzymes and Transporters: The Long Way from Bench to Bedside
Current Topics in Medicinal Chemistry A Review of Aberrant DNA Methylation and Epigenetic Agents Targeting DNA Methyltransferases in Endometriosis
Current Drug Targets Drug Targeting Systems for Cancer Therapy: Nanotechnological Approach
Mini-Reviews in Medicinal Chemistry Trichothecin from Endophytic Fungus Trichothecium sp. and its Anticancer Effect on Murine Melanoma and Breast Cancer Cell Lines
Current Biochemical Engineering (Discontinued) Tetrazole Derivatives as Promising Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry miRNA 21: Diagnostic Prognostic and Therapeutic Marker for Oral Cancer
MicroRNA PP-1α and PP-1γ Display Antagonism and Differential Roles in Tumorigenicity of Lung Cancer Cells
Current Molecular Medicine Vitamin D, Sunlight and Cancer Connection
Anti-Cancer Agents in Medicinal Chemistry The Synergistic Effects of DNA-Targeted Chemotherapeutics and Histone Deacetylase Inhibitors As Therapeutic Strategies for Cancer Treatment
Current Medicinal Chemistry Receptor Tryosine Kinase Inhibitors as Potent Weapons in War Against Cancers
Current Pharmaceutical Design Pharmacophore, 3D-QSAR Models and Dynamic Simulation of 1,4-Benzothiazines for Colorectal Cancer Treatment
Combinatorial Chemistry & High Throughput Screening MicroRNA and Cancer: Tiny Molecules with Major Implications
Current Genomics