Abstract
Multidrug resistance (MDR) mediated by overexpression of MDR1 (ABCB1) P-glycoprotein (Pgp) is one of the best characterized transporter-mediated barriers to successful chemotherapy in cancer patients and is also a rapidly emerging target in the progression of neurodegenerative disorders, such as Alzheimers and Parkinsons diseases. Therefore, molecular imaging probes capable of imaging noninvasively Pgp and closely related transporter activities in tissues as well as tumors would be expected to contribute to personalized medicine. Interrogation of Pgp-mediated transport activity in vivo via noninvasive SPECT imaging could be beneficial for stratification of patient populations likely to benefit from a given therapeutic treatment, assist in the management of chemotherapy and aid the study of neurodegenerative diseases.
Keywords: Multidrug resistance, ABC transporters, P-glycoprotein, SPECT, PET, metal complexes, radiopharmaceuticals, technetium-99m, blood-brain barrier, cancer, gene therapy, ATP-binding cassette (ABC), Transmembrane domains, Nucleotide-binding domains (NBDs), 99mTc-Sestamibi, Pgp expression, Verapamil, Cyclosporin, Pgp inhibitors, Quinidine, Q-complexes, 99mTc-Furifosmin, PSC 833, LY335979, Pgp activity, Pgp substrate, Schiff-base Ga(III) complexes, Multiple myeloma (MM), valspodar, Tariquidar, Parkinsonian syndrome, 11C-verapamil, Alzheimer's Disease (AD), Creutzfeldt-Jakob disease
Current Topics in Medicinal Chemistry
Title: Probing Multidrug Resistance P-glycoprotein Transporter Activity with SPECT Radiopharmaceuticals
Volume: 10 Issue: 17
Author(s): David Piwnica-Worms and Vijay Sharma
Affiliation:
Keywords: Multidrug resistance, ABC transporters, P-glycoprotein, SPECT, PET, metal complexes, radiopharmaceuticals, technetium-99m, blood-brain barrier, cancer, gene therapy, ATP-binding cassette (ABC), Transmembrane domains, Nucleotide-binding domains (NBDs), 99mTc-Sestamibi, Pgp expression, Verapamil, Cyclosporin, Pgp inhibitors, Quinidine, Q-complexes, 99mTc-Furifosmin, PSC 833, LY335979, Pgp activity, Pgp substrate, Schiff-base Ga(III) complexes, Multiple myeloma (MM), valspodar, Tariquidar, Parkinsonian syndrome, 11C-verapamil, Alzheimer's Disease (AD), Creutzfeldt-Jakob disease
Abstract: Multidrug resistance (MDR) mediated by overexpression of MDR1 (ABCB1) P-glycoprotein (Pgp) is one of the best characterized transporter-mediated barriers to successful chemotherapy in cancer patients and is also a rapidly emerging target in the progression of neurodegenerative disorders, such as Alzheimers and Parkinsons diseases. Therefore, molecular imaging probes capable of imaging noninvasively Pgp and closely related transporter activities in tissues as well as tumors would be expected to contribute to personalized medicine. Interrogation of Pgp-mediated transport activity in vivo via noninvasive SPECT imaging could be beneficial for stratification of patient populations likely to benefit from a given therapeutic treatment, assist in the management of chemotherapy and aid the study of neurodegenerative diseases.
Export Options
About this article
Cite this article as:
Piwnica-Worms David and Sharma Vijay, Probing Multidrug Resistance P-glycoprotein Transporter Activity with SPECT Radiopharmaceuticals, Current Topics in Medicinal Chemistry 2010; 10 (17) . https://dx.doi.org/10.2174/156802610792928086
DOI https://dx.doi.org/10.2174/156802610792928086 |
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
-
GABAA Receptor Specific Pyrazolopyrimidines as Potential Imaging Agents: In Vivo Characteristics of a New 18F-labelled Indiplon Derivative
Current Radiopharmaceuticals The Chemistry and Bio-Medicinal Significance of Pyrimidines & Condensed Pyrimidines
Current Topics in Medicinal Chemistry Interrelationships Among Gut Microbiota and Host: Paradigms, Role in Neurodegenerative Diseases and Future Prospects
CNS & Neurological Disorders - Drug Targets The Impact of Natural Compounds on the Treatment of Neurodegenerative Diseases
Current Organic Chemistry Molecular Mechanism of Autophagy: Its Role in the Therapy of Alzheimer’s Disease
Current Neuropharmacology Resveratrol Inhibits the Epithelial-Mesenchymal Transition of Pancreatic Cancer Cells Via Suppression of the PI-3K/Akt/NF-κB Pathway
Current Medicinal Chemistry Cyclooxygenases in the Central Nervous System: Implications for Treatment of Neurological Disorders
Current Pharmaceutical Design Novel Kynurenic Acid Analogues in the Treatment of Migraine and Neurodegenerative Disorders: Preclinical Studies and Pharmaceutical Design
Current Pharmaceutical Design Oxidative/Nitrosative Brain Damage in Stress: Possible Target for Neuropsychopharmacological Drugs
Current Medicinal Chemistry - Central Nervous System Agents Transcriptomics
Current Drug Metabolism Genetics and Pathophysiology of Neurodegeneration with Brain Iron Accumulation (NBIA)
Current Neuropharmacology Editorial [Hot Topic:Active and Passive Aβ-Immunotherapy: Preclinical and Clinical Studies and Future Directions: Part I (Guest Editors: Michael G. Agadjanyan and David H. Cribbs)]
CNS & Neurological Disorders - Drug Targets Correlation of Alzheimer-like Tau Hyperphosphorylation and fMRI Bold Intensity
Current Alzheimer Research Adult Neural Stem Cells: Response to Stroke Injury and Potential for Therapeutic Applications
Current Stem Cell Research & Therapy Alcohol and Smoking Mediated Oxidative Stress in Organ Toxicities: Role of Cytochrome P450 Systems
Mini-Reviews in Organic Chemistry The Metabotropic Glutamate Receptor System: G-Protein Mediated Pathways that Modulate Neuronal and Vascular Cellular Injury
Current Medicinal Chemistry - Central Nervous System Agents Postischemic-Anoxic Encephalopathy After Global Forebrain Ischemia
Central Nervous System Agents in Medicinal Chemistry Stem Cell and Gene Therapeutic Strategies for the Treatment of Multiple Sclerosis
Current Molecular Medicine Peroxynitrite-Driven Mechanisms in Diabetes and Insulin Resistance – the Latest Advances
Current Medicinal Chemistry Patent Selections:
Recent Patents on CNS Drug Discovery (Discontinued)