Effects of a series of dihydroanthracene derivatives on drug efflux in multidrug resistant cancer cells

2003 ◽  
Vol 38 (3) ◽  
pp. 253-263 ◽  
Author(s):  
Sandrine Alibert ◽  
Christiane Santelli-Rouvier ◽  
Madeleine Castaing ◽  
Michel Berthelot ◽  
Gabriella Spengler ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Multidrug Resistant ◽  
Drug Efflux

scholarly journals The Second-Generation PIM Kinase Inhibitor TP-3654 Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Cytotoxic Anticancer Drugs

2021 ◽  
Vol 22 (17) ◽  
pp. 9440
Author(s):  
Chung-Pu Wu ◽  
Yan-Qing Li ◽  
Ya-Chen Chi ◽  
Yang-Hui Huang ◽  
Tai-Ho Hung ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Anticancer Drugs ◽  
Drug Transport ◽  
Second Generation ◽  
Kinase Inhibitor ◽  
Multidrug Resistant ◽  
Drug Efflux ◽  
Transport Function ◽  
Therapy Option ◽  
Induction Of Resistance

Human ATP-binding cassette (ABC) subfamily G member 2 (ABCG2) mediates the transport of a wide variety of conventional cytotoxic anticancer drugs and molecular targeted agents. Consequently, the overexpression of ABCG2 in cancer cells is linked to the development of the multidrug resistance (MDR) phenotype. TP-3654 is an experimental second-generation inhibitor of PIM kinase that is currently under investigation in clinical trials to treat advanced solid tumors and myelofibrosis. In this study, we discovered that by attenuating the drug transport function of ABCG2, TP-3654 resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic ABCG2 substrate drugs topotecan, SN-38 and mitoxantrone. Moreover, our results indicate that ABCG2 does not mediate resistance to TP-3654 and may not play a major role in the induction of resistance to TP-3654 in cancer patients. Taken together, our findings reveal that TP-3654 is a selective, potent modulator of ABCG2 drug efflux function that may offer an additional combination therapy option for the treatment of multidrug-resistant cancers.

scholarly journals Incorporation of drug efflux inhibitor and chemotherapeutic agent into an inorganic/organic platform for the effective treatment of multidrug resistant breast cancer

2019 ◽  
Vol 17 (1) ◽  
Author(s):  
Yang Dong ◽  
Hongze Liao ◽  
Jian Yu ◽  
Hao Fu ◽  
De Zhao ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Inner Core ◽  
Chemotherapeutic Agent ◽  
Multidrug Resistant ◽  
Active Targeting ◽  
Drug Efflux ◽  
Concurrent Administration ◽  
Promising Therapeutic Approach

Abstract Background Multidrug resistance (MDR) is a pressing obstacle in clinical chemotherapy for breast cancer. Based on the fact that the drug efflux is an important factor in MDR, we designed a codelivery system to guide the drug efflux inhibitor verapamil (VRP) and the chemotherapeutic agent novantrone (NVT) synergistically into breast cancer cells to reverse MDR. Results This co-delivery system consists of following components: the active targeting peptide RGD, an inorganic calcium phosphate (CaP) shell and an organic inner core. VRP and NVT were loaded into CaP shell and phosphatidylserine polyethylene glycol (PS-PEG) core of nanoparticles (NPs) separately to obtain NVT- and VRP-loaded NPs (NV@CaP-RGD). These codelivered NPs allowed VRP to prevent the efflux of NVT from breast cancer cells by competitively combining with drug efflux pumps. Additionally, NV@CaP-RGD was effectively internalized into breast cancer cells by precise delivery through the effects of the active targeting peptides RGD and EPR. The pH-triggered profile of CaP was also able to assist the NPs to successfully escape from lysosomes, leading to a greatly increased effective intracellular drug concentration. Conclusion The concurrent administration of VRP and NVT by organic/inorganic NPs is a promising therapeutic approach to reverse MDR in breast cancer.

Triterpene derivatives and their reversing activity against multidrug resistant cancer cells

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
Y Kashiwada ◽  
M Taniguchi ◽  
X Juan ◽  
T Yamagishi ◽  
Y Takaishi
Keyword(s):  
Cancer Cells ◽  
Multidrug Resistant

Cancer Treatment with Liposomes Based Drugs and Genes Co-delivery Systems

2018 ◽  
Vol 25 (28) ◽  
pp. 3319-3332 ◽  
Author(s):  
Chuanmin Zhang ◽  
Shubiao Zhang ◽  
Defu Zhi ◽  
Jingnan Cui
Keyword(s):  
Cell Cycle ◽  
Cancer Cells ◽  
Synergistic Effects ◽  
Resistance Mechanisms ◽  
Delivery Systems ◽  
Cell Cycle Checkpoints ◽  
Drug Efflux ◽  
Cancer Resistance ◽  
Cancer Models ◽  
Anti Cancer

There are several mechanisms by which cancer cells develop resistance to treatments, including increasing anti-apoptosis, increasing drug efflux, inducing angiogenesis, enhancing DNA repair and altering cell cycle checkpoints. The drugs are hard to reach curative effects due to these resistance mechanisms. It has been suggested that liposomes based co-delivery systems, which can deliver drugs and genes to the same tumor cells and exhibit synergistic anti-cancer effects, could be used to overcome the resistance of cancer cells. As the co-delivery systems could simultaneously block two or more pathways, this might promote the death of cancer cells by sensitizing cells to death stimuli. This article provides a brief review on the liposomes based co-delivery systems to overcome cancer resistance by the synergistic effects of drugs and genes. Particularly, the synergistic effects of combinatorial anticancer drugs and genes in various cancer models employing multifunctional liposomes based co-delivery systems have been discussed. This review also gives new insights into the challenges of liposomes based co-delivery systems in the field of cancer therapy, by which we hope to provide some suggestions on the development of liposomes based co-delivery systems.

ChemInform Abstract: Novel Halogenated Sulfonamides Inhibit the Growth of Multidrug Resistant MCF-7/ADR Cancer Cells.

ChemInform ◽  
2010 ◽  
Vol 30 (43) ◽  
pp. no-no
Author(s):  
Julio C. Medina ◽  
Daniel Roche ◽  
Bei Shan ◽  
R. Marc Learned ◽  
Walter P. Frankmoelle ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Multidrug Resistant ◽  
Mcf 7
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