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Breast cancer resistance protein and P-glycoprotein in brain cancer: two gatekeepers team up.
TLDR
A new paradigm of P-gp and BCRP working as a "cooperative team of gatekeepers" at the blood-brain barrier is highlighted, its ramifications for brain cancer therapy are discussed, and the latest findings on dual P- gp/BCRP inhibitors are summarized.
Plasma Membrane Localization of Multidrug Resistance-Associated Protein Homologs in Brain Capillary Endothelial Cells
TLDR
The present studies indicate that the localization of MRPs in the endothelial cells forming the BBB is different from that observed in polarized epithelial cells and thus may contribute to the reduced entry and enhanced elimination of organic anions and nucleotides in the brain.
Distribution of Gefitinib to the Brain Is Limited by P-glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2)-Mediated Active Efflux
TLDR
Results show that brain distribution of gefitinib is restricted due to active efflux by P-gp and BCRP, which is of clinical significance for therapy in brain tumors such as glioma, where concurrent administration of a dual inhibitor such as elacridar can increase delivery and thus enhance efficacy of gfitinIB.
Distribution of STI-571 to the Brain Is Limited by P-Glycoprotein-Mediated Efflux
TLDR
It is indicated that STI-571 is a substrate of P-glycoprotein, and that the inhibition of P -glycop protein affects the transport of STI -571 across MDCKII monolayers.
Delivery of molecularly targeted therapy to malignant glioma, a disease of the whole brain
TLDR
The challenge of glioma as a disease of the whole brain is discussed, which lends emphasis to the need to deliver drugs effectively across the blood–brain barrier to reach both the central tumour and the invasiveglioma cells.
P-glycoprotein and Breast Cancer Resistance Protein Influence Brain Distribution of Dasatinib
TLDR
In vitro and in vivo studies demonstrate that dasatinib is a substrate for the important efflux transporters p-glycoprotein and BCRP and these transport systems play a significant role in limiting the CNS delivery of d asatinib and may have direct implications in the treatment of primary and metastatic brain tumors.
Drug efflux transporters in the CNS.
Expression of multidrug resistance-associated protein (MRP) in brain microvessel endothelial cells.
TLDR
Functional and biochemical data are presented demonstrating the presence of MRP in the brain microvessel endothelial cells that form the blood-brain barrier (BBB) and its function as a drug efflux transport system.
Abcg2/Bcrp1 Mediates the Polarized Transport of Antiretroviral Nucleosides Abacavir and Zidovudine
TLDR
These studies characterize the Bcrp1-mediated transport of abacavir and AZT and show that prototypical BCRP inhibitors GF120918 and Ko143 can inhibit the B CRP1- mediated transport of these important antiretroviral compounds.
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