Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade

2016 ◽  
Vol 370 (1) ◽  
pp. 153-164 ◽  
Author(s):  
Zhaolin Chen ◽  
Tianlu Shi ◽  
Lei Zhang ◽  
Pengli Zhu ◽  
Mingying Deng ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Efflux Transporters ◽  
Atp Binding ◽  
Drug Efflux ◽  
The Past ◽  
Drug Efflux Transporters ◽  
Atp Binding Cassette

Functional ATP-Binding Cassette Drug Efflux Transporters in Isolated Human and Rat Hepatocytes Significantly Affect Assessment of Drug Disposition

2014 ◽  
Vol 42 (3) ◽  
pp. 448-458 ◽  
Author(s):  
Patrik Lundquist ◽  
Gunilla Englund ◽  
Cristine Skogastierna ◽  
Johan Lööf ◽  
Jenny Johansson ◽  
...  
Keyword(s):  
Drug Disposition ◽  
Rat Hepatocytes ◽  
Efflux Transporters ◽  
Atp Binding ◽  
Drug Efflux ◽  
Drug Efflux Transporters ◽  
Atp Binding Cassette

scholarly journals Expressional Study of Permeability glycoprotein (P-gp) and Multidrug Resistance Protein 1 (MRP-1) in Drug-Resistant Mesial Temporal Lobe Epilepsy

2021 ◽  
pp. 1-31
Author(s):  
Mandeep Kaur ◽  
◽  
Tulika Gupta ◽  
Mili Gupta ◽  
Parampreet S. Kharbanda ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Multidrug Resistance ◽  
Mesial Temporal Lobe Epilepsy ◽  
Efflux Transporters ◽  
P Value ◽  
Drug Efflux ◽  
Drug Resistant ◽  
Glycoprotein P ◽  
Mesial Temporal Lobe ◽  
Drug Efflux Transporters

About 30% of epileptic patients do not react to anti-epileptic drugs leading to refractory seizures. The pathogenesis of drug-resistance in Mesial Temporal Lobe Epilepsy (MTLE) is not completely understood. Increased activity of drug-efflux transporters might be involved, resulting in subclinical concentrations of the drug at the target site. The major drug-efflux transporters are permeability glycoprotein (P-gp) and multidrug-resistance associated protein-1 (MRP-1). The major drawback so far is the expressional analysis of transporters in equal numbers of drug-resistant epileptic tissue and age-matched non-epileptic tissue. We have studied these two transporters in the sclerotic hippocampal tissues resected from the epilepsy surgery (n=15) and compared their expression profile with the tissues resected from non-epileptic autopsy cases (n=15). Statistically significant over expression of both P-gp (p-value <0.0001) and MRP-1 (p-value 0.01) at gene and protein levels was found in the MTLE cases. The fold change of P-gp was more pronounced than MRP-1. Immunohistochemistry of patient group showed increased immunoreactivity of P-gp at blood brain barrier and increased reactivity of MRP-1 in parenchyma. The results were confirmed by confocal immunofluorescence microscopy. The study demonstrated that P-gp in association with MRP-1 might be responsible for the multi-drug resistance in epilepsy

scholarly journals Drug Efflux Transporters Are Overexpressed in Short-Term Tamoxifen-Induced MCF7 Breast Cancer Cells

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Desak Gede Budi Krisnamurti ◽  
Melva Louisa ◽  
Erlia Anggraeni ◽  
Septelia Inawati Wanandi
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Short Period ◽  
Drug Efflux Transporters

Tamoxifen is the first line drug used in the treatment of estrogen receptor-positive (ER+) breast cancer. The development of multidrug resistance (MDR) to tamoxifen remains a major challenge in the treatment of cancer. One of the mechanisms related to MDR is decrease of drug influx via overexpression of drug efflux transporters such as P-glycoprotein (P-gp/MDR1), multidrug resistance associated protein (MRP), or BCRP (breast cancer resistance protein). We aimed to investigate whether the sensitivity of tamoxifen to the cells is maintained through the short period and whether the expressions of several drug efflux transporters have been upregulated. We exposed MCF7 breast cancer cells with tamoxifen 1 μM for 10 passages (MCF7 (T)). The result showed that MCF7 began to lose their sensitivity to tamoxifen from the second passage. MCF7 (T) also showed a significant increase in all transporters examined compared with MCF7 parent cells. The result also showed a significant increase of CC50 in MCF7 (T) compared to that in MCF7 (97.54 μM and 3.04 μM, resp.). In conclusion, we suggest that the expression of several drug efflux transporters such as P-glycoprotein, MRP2, and BCRP might be used and further studied as a marker in the development of tamoxifen resistance.

Relationship between cytotoxic drug response patterns and activity of drug efflux transporters mediating multidrug resistance

1998 ◽  
Vol 346 (2-3) ◽  
pp. 315-322 ◽  
Author(s):  
Sumeer Dhar ◽  
Peter Nygren ◽  
Gunnar Liminga ◽  
Christer Sundström ◽  
Manuel de la Torre ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Drug Response ◽  
Cytotoxic Drug ◽  
Efflux Transporters ◽  
Drug Efflux ◽  
Response Patterns ◽  
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.

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