Multispecificity of Drug Transporters: Probing Inhibitor Selectivity for the Human Drug Efflux Transporters ABCB1 and ABCG2

ChemMedChem ◽  
2007 ◽  
Vol 2 (12) ◽  
pp. 1783-1788 ◽  
Author(s):  
Joerg Cramer ◽  
Stephan Kopp ◽  
Susan E. Bates ◽  
Peter Chiba ◽  
Gerhard F. Ecker
Keyword(s):  
Drug Transporters ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Inhibitor Selectivity ◽  
Drug Efflux Transporters

scholarly journals THE MODULATION OF DRUG EFFLUX TRANSPORTER BY CURCUMIN IN MCF7 BREAST CANCER CELLS AFTER REPEATED EXPOSURE OF ENDOXIFEN AND ESTRADIOL

2018 ◽  
Vol 10 (1) ◽  
pp. 102
Author(s):  
Robby Hertanto ◽  
Wilson Bastian ◽  
Paramita . ◽  
Melva Louisa
Keyword(s):  
Breast Cancer ◽  
Cell Viability ◽  
Mrna Expression ◽  
Rna Extraction ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Mcf7 Cells ◽  
Total Rna ◽  
P Glycoprotein ◽  
Drug Efflux Transporters

Objective: The aim of the present study was to determine whether curcumin (CM) can prevent drug sensitivity of breast cancer (BC) cells when E andβ-E2 are administered together and whether the underlying mechanism involves modulation of drug efflux transporters.Methods: MCF7 BC cells were treated with the vehicle only, E+β-E2, or E+β-E2+CM repeatedly for 8 weeks. Afterward, the cells were harvested,counted, and isolated for total RNA extraction. Total RNA was then processed into cDNA and further processed for the determination of mRNAexpression patterns of drug efflux transporters (P-glycoprotein, BCRP, and MRP1).Results: Decreased sensitivity of BC cells was shown by the increased cell viability of MCF7 cells after 8 weeks. This condition was accompanied withincreased mRNA expression of P-glycoprotein, BCRP, and MRP1 in cells treated with E+β-E2, as compared with the vehicle only. CM, administered incombination with E+β-E2, resulted in decreased cell viability versus E and β-E2 and also decreased in mRNA expression of P-glycoprotein, BCRP, andMRP1.Conclusion: CM partially reversed the sensitivity loss of BC cells to E in the presence of β-E2 by modulating drug efflux transporters.

Expression of drug efflux transporters in poultry tissues

2010 ◽  
Vol 89 (1) ◽  
pp. 104-107 ◽  
Author(s):  
Aneliya M. Haritova ◽  
J. Schrickx ◽  
Johanna Fink-Gremmels
Keyword(s):  
Efflux Transporters ◽  
Drug Efflux ◽  
Poultry Tissues ◽  
Drug Efflux Transporters

Genetic Polymorphisms of Copper-and Platinum Drug-efflux Transporters ATP7A and ATP7B in Japanese Cancer Patients

2009 ◽  
Vol 24 (6) ◽  
pp. 565-574 ◽  
Author(s):  
Hiromi Fukushima-Uesaka ◽  
Yoshiro Saito ◽  
Keiko Maekawa ◽  
Kouichi Kurose ◽  
Emiko Sugiyama ◽  
...  
Keyword(s):  
Cancer Patients ◽  
Genetic Polymorphisms ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Platinum Drug ◽  
Drug Efflux Transporters

scholarly journals Identification of a Novel Topoisomerase Inhibitor Effective in Cells Overexpressing Drug Efflux Transporters

PLoS ONE ◽  
2009 ◽  
Vol 4 (10) ◽  
pp. e7238 ◽  
Author(s):  
Walid Fayad ◽  
Mårten Fryknäs ◽  
Slavica Brnjic ◽  
Maria Hägg Olofsson ◽  
Rolf Larsson ◽  
...  
Keyword(s):  
Efflux Transporters ◽  
Drug Efflux ◽  
Topoisomerase Inhibitor ◽  
Drug Efflux Transporters ◽  
In Cells

Functional intravital assay of anticancer drug efflux transporters in breast cancer biopsy specimens

1998 ◽  
Vol 34 ◽  
pp. S106
Author(s):  
T. Bogush ◽  
G. Smirnova ◽  
E. Koldaeva ◽  
E. Bogush ◽  
V. Kirsanov ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Drug ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Biopsy Specimens ◽  
Cancer Biopsy ◽  
Drug Efflux Transporters

scholarly journals Assessment of three Resistance-Nodulation-Cell Division drug efflux transporters of Burkholderia cenocepacia in intrinsic antibiotic resistance

2009 ◽  
Vol 9 (1) ◽  
pp. 200 ◽  
Author(s):  
Silvia Buroni ◽  
Maria R Pasca ◽  
Ronald S Flannagan ◽  
Silvia Bazzini ◽  
Anna Milano ◽  
...  
Keyword(s):  
Antibiotic Resistance ◽  
Cell Division ◽  
Burkholderia Cenocepacia ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Drug Efflux Transporters

scholarly journals Polarized macrophage subsets differentially express the drug efflux transporters MRP1 and BCRP, resulting in altered HIV production

2018 ◽  
Vol 26 ◽  
pp. 204020661774516 ◽  
Author(s):  
Hui He ◽  
Merrion Buckley ◽  
Bernard Britton ◽  
Ying Mu ◽  
Kristin Warner ◽  
...  
Keyword(s):  
Protein Expression ◽  
Viral Replication ◽  
Efflux Transporters ◽  
Enzyme Linked Immunosorbent Assay ◽  
Drug Efflux ◽  
M1 Macrophages ◽  
Altered Expression ◽  
The Difference ◽  
Transporter Expression ◽  
Drug Efflux Transporters

Introduction Macrophages play an important role in HIV, where they are a cellular reservoir. Macrophages are polarized into two phenotypes: pro-inflammatory M1 macrophages and anti-inflammatory M2 macrophages, which may have altered expression of drug efflux transporters, including BCRP and MRP1. These differences may result in subtherapeutic concentrations of antiretrovirals inside of macrophages and viral replication. Methods U937 and U1 cells were polarized to the M1 or M2 phenotype via IFN-γ and LPS, or IL-4, IL-13, and LPS. Transporter expression was assessed via PCR and Western blotting, and transporter function was assessed via fluorescent dye assays. Transporter function was blocked with the inhibitors MK571 or KO143. Protein expression was confirmed in monocyte-derived macrophages. p24 production was assessed in U1 cells via enzyme-linked immunosorbent assay. Results mRNA and protein analysis demonstrated higher expression of MRP1 in M1 macrophages, while BCRP expression was downregulated in M1 macrophages. Treatment with inhibitors of transporter function decreased the difference in intracellular fluorescence between polarized macrophages. Differences in protein expression, which were observed with U937 cells, were confirmed in monocyte-derived macrophages. M1, but not M2 cells treated with MK571, showed decreased p24 production, consistent with reported MRP1 transporter expression. Conclusions These results support our hypothesis that there is differential expression of MRP1 and BCRP on M1 and M2 polarized macrophages and suggests that these differences may result in altered intracellular concentrations of antiretrovirals in macrophages and alter viral production in these cells. Targeting these differences may be a strategy to decrease viral replication in HIV-infected individuals.

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