Abstract
The treatment of brain tumors and neurodegenerative diseases, represents an ongoing challenge. In Central Nervous System (CNS) the achievement of therapeutic concentration of chemical agents is complicated by the presence of distinct set of efflux proteins, such as ATP-Binding Cassette (ABC) transporters localized on the Blood-Brain Barrier (BBB). The activity of ABC transporters seems to be a common mechanism that underlies the poor response of CNS diseases to therapies.
The molecular characterization of Breast Cancer Resistance Protein (BCRP/ABCG2), as an ABC transporter conferring multidrug resistance (MDR), has stimulated many studies to investigate its activity on the BBB, its involvement in physiology and CNS diseases and its role in limiting the delivery of drugs in CNS.
In this review, we highlight the activity and localization of BCRP on the BBB and the action that this efflux pump has on many conventional drugs or latest generation molecules used for the treatment of CNS tumors and other neurodegenerative diseases.
Keywords: BCRP, Blood-Brain Barrier, brain tumors, multidrug resistance, neurodegenerative diseases.
Anti-Cancer Agents in Medicinal Chemistry
Title:Blood-Brain Barrier and Breast Cancer Resistance Protein: A Limit to the Therapy of CNS Tumors and Neurodegenerative Diseases
Volume: 16 Issue: 7
Author(s): Anna Lisa Iorio, Martina da Ros, Ornella Fantappiè, Maurizio Lucchesi, Ludovica Facchini, Alessia Stival, Sabrina Becciani, Milena Guidi, Claudio Favre, Maurizio de Martino, Lorenzo Genitori and Iacopo Sardi
Affiliation:
Keywords: BCRP, Blood-Brain Barrier, brain tumors, multidrug resistance, neurodegenerative diseases.
Abstract: The treatment of brain tumors and neurodegenerative diseases, represents an ongoing challenge. In Central Nervous System (CNS) the achievement of therapeutic concentration of chemical agents is complicated by the presence of distinct set of efflux proteins, such as ATP-Binding Cassette (ABC) transporters localized on the Blood-Brain Barrier (BBB). The activity of ABC transporters seems to be a common mechanism that underlies the poor response of CNS diseases to therapies.
The molecular characterization of Breast Cancer Resistance Protein (BCRP/ABCG2), as an ABC transporter conferring multidrug resistance (MDR), has stimulated many studies to investigate its activity on the BBB, its involvement in physiology and CNS diseases and its role in limiting the delivery of drugs in CNS.
In this review, we highlight the activity and localization of BCRP on the BBB and the action that this efflux pump has on many conventional drugs or latest generation molecules used for the treatment of CNS tumors and other neurodegenerative diseases.
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Cite this article as:
Iorio Lisa Anna, Ros da Martina, Fantappiè Ornella, Lucchesi Maurizio, Facchini Ludovica, Stival Alessia, Becciani Sabrina, Guidi Milena, Favre Claudio, Martino de Maurizio, Genitori Lorenzo and Sardi Iacopo, Blood-Brain Barrier and Breast Cancer Resistance Protein: A Limit to the Therapy of CNS Tumors and Neurodegenerative Diseases, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (7) . https://dx.doi.org/10.2174/1871520616666151120121928
DOI https://dx.doi.org/10.2174/1871520616666151120121928 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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