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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Blood-Brain Barrier and Breast Cancer Resistance Protein: A Limit to the Therapy of CNS Tumors and Neurodegenerative Diseases

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

Volume 16, Issue 7, 2016

Page: [810 - 815] Pages: 6

DOI: 10.2174/1871520616666151120121928

open access plus


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.

Graphical Abstract

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