Open AccessJournal Article
Cellular mechanisms of multidrug resistance of tumor cells.
TLDR
Cellular drug resistance is mediated by different mechanisms operating at different steps of the cytotoxic action of the drug from a decrease of drug accumulation in the cell to the abrogation of apoptosis induced by the chemical substance.Abstract:
Multidrug resistance (MDR) is the protection of a tumor cell population against numerous drugs differing in chemical structure and mechanisms of influence on the cells. MDR is one of the major causes of failures of chemotherapy of human malignancies. Recent studies show that the molecular mechanisms of MDR are numerous. Cellular drug resistance is mediated by different mechanisms operating at different steps of the cytotoxic action of the drug from a decrease of drug accumulation in the cell to the abrogation of apoptosis induced by the chemical substance. Often several different mechanisms are switched on in the cells, but usually one major mechanism is operating. The most investigated mechanisms with known clinical significance are: a) activation of transmembrane proteins effluxing different chemical substances from the cells (P-glycoprotein is the most known efflux pump); b) activation of the enzymes of the glutathione detoxification system; c) alterations of the genes and the proteins involved into the control of apoptosis (especially p53 and Bcl-2).read more
Citations
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Journal ArticleDOI
Drug Resistance in Cancer: An Overview
Genevieve Housman,Shannon Byler,Sarah Heerboth,Karolina Lapinska,Mckenna Longacre,Nicole A. Snyder,Sibaji Sarkar +6 more
TL;DR: The current knowledge of mechanisms that promote or enable drug resistance, such as drug inactivation, drug target alteration, drug efflux, DNA damage repair, cell death inhibition, and the epithelial-mesenchymal transition, as well as how inherent tumor cell heterogeneity plays a role in drug resistance are outlined.
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Glutathione in Cancer Biology and Therapy
TL;DR: An analysis of links among GSH, adaptive responses to stress, molecular mechanisms of invasive cancer cell survival and death, and sensitization of metastatic cells to therapy shows that acceleration of GSH efflux facilitates selective GSH depletion in metastasis cells.
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Recent progress in tumor pH targeting nanotechnology
TL;DR: This review highlights recent progress of the pH-sensitive nanotechnology developed in Bae research group to overcome multidrug resistance of various tumors.
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Enhanced Chemotherapy Efficacy by Sequential Delivery of siRNA and Anticancer Drugs Using PEI‐Grafted Graphene Oxide
TL;DR: It is demonstrated that the PEI-GO is an excellent nanocarrier for effective delivery of siRNA and chemical drugs, and that sequential delivery of the siRNAs and the anticancer drug doxorubicin by PEi-GO into cancer cells exhibits a synergistic effect, which leads to a signifi cantly enhanced chemotherapy effi cacy.
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Enzyme-Catalyzed Activation of Anticancer Prodrugs
TL;DR: The most important enzymes involved in prodrug activation notably with respect to tissue distribution, up-regulation in tumor cells and turnover rates are described and it is concluded that the development of prodrugs has been relatively successful.
References
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Book
Molecular and Cellular Biology of Multidrug Resistance in Tumor Cells
TL;DR: These essays summarize the results of molecular biological, pharmacological, biochemical, cytogenetic, immunological, and pathological studies on the ability of neoplastic cells to survive exposure to various chemotherapeutic drugs.
Journal ArticleDOI
Expression of human glutathione S-transferases in Saccharomyces cerevisiae confers resistance to the anticancer drugs adriamycin and chlorambucil
TL;DR: Examining human Alpha-class and Pi-class GST cDNAs that encode GST B1B1 and GST pi in the yeast Saccharomyces cerevisiae provides direct evidence that the over-expression of GST in cells can confer resistance to anticancer drugs.
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Do cMOAT (MRP2), other MRP homologues, and LRP play a role in MDR?
TL;DR: The discovery of the Multidrug Resistance-associated Protein (MRP or MRP1) as a GS-X pump able to transport both anionic drug conjugates and unmodified anti-cancer drugs out of the cell, has raised the question whether other members of the MRP family might contribute to drug resistance of human tumours.