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.
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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 |
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