By Thomas Efferth

This severe overview quantity explores the topic of ABC transporters within the context of uncomplicated melanoma learn and its function in drug-resistant tumors. The chapters supplied supplement easy study by way of together with investigations from translational functions to scientific oncology. the advance of resistance is an important problem in melanoma chemotherapy and the sector has been relocating quickly by way of identifying the mechanisms for blockading ABC transporter-mediated drug efflux through particular inhibitors and thereby overcoming multidrug resistance. the quantity covers those matters in cautious element. extra themes contain the relevance of ABC transporters in resistance to novel and confirmed anticancer medicinal drugs and diagnosis of sufferers to compounds, compounds utilized in photodynamic treatment, tyrosine kinase inhibitors and others. in addition, the opportunity of radiopharmaceuticals for prognosis of multidrug-resistant tumors and of nanotechnology to wrestle drug-resistant tumors is additionally discussed.

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Extra info for Resistance to Targeted ABC Transporters in Cancer

Sample text

In additional to enhanced drug efflux, which may be mediated by multiple transporters, alterations in the ability of cancer cells to take up drugs, and alterations affecting the ability of drugs to kill cells, including increased drug metabolism activity, increased DNA repair capacity, alterations to the cell cycle, and increased resistance to apoptosis, can all contribute to multidrug resistance. Secondly, many of the clinical correlations described above have been determined in the context of combination chemotherapy that may include both substrates and non-substrates for a given transporter.

Clinical relevance of the MDR-1 gene and its gene product, P-glycoprotein, for cancer chemotherapy: a meta-analysis. Tumor Diagn Ther. 1993;14:238–43. 56. Sauerbrey A, Zintl F, Volm M. P-glycoprotein and glutathione S-transferase pi in childhood acute lymphoblastic leukaemia. Br J Cancer. 1994;70:1144–9. 57. Verrelle P, Meissonnier F, Fonck Y, Feillel V, Dionet C, Kwiatkowski F, et al. Clinical relevance of immunohistochemical detection of multidrug resistance P-glycoprotein in breast carcinoma.

A. I. Fletcher, M. D. Norris Abstract Chemoresistance in cancer is frequently associated with elevated levels of multidrug transporters. While P-glycoprotein is the best known, the majority of multidrug transporters belong to the Multidrug Resistance Protein (MRP) family, also known as the ABCC family, which includes MRP1–9. These proteins are typically found in the plasma membrane of cells, where they efflux a broad range of both physiological substrates and xenobiotics, including anticancer drugs.

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