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Multidrug resistance in cancer: role of ATP–dependent transporters
Chemotherapeutics are the most effective treatment for metastatic tumours. However, the ability of cancer cells to become simultaneously resistant to different drugs — a trait known as multidrug… Expand
Biochemistry of multidrug resistance mediated by the multidrug transporter.
Targeting multidrug resistance in cancer
- G. Szakács, Jill K. Paterson, J. Ludwig, Catherine L. Booth-Genthe, M. Gottesman
- Nature Reviews Drug Discovery
- 1 March 2006
Effective treatment of metastatic cancers usually requires the use of toxic chemotherapy. In most cases, multiple drugs are used, as resistance to single agents occurs almost universally. For this… Expand
Biochemical, cellular, and pharmacological aspects of the multidrug transporter.
- S. Ambudkar, S. Dey, C. Hrycyna, M. Ramachandra, I. Pastan, M. Gottesman
- Medicine, Biology
- Annual review of pharmacology and toxicology
Considerable evidence has accumulated indicating that the multidrug transporter or P-glycoprotein plays a role in the development of simultaneous resistance to multiple cytotoxic drugs in cancer… Expand
Mechanisms of cancer drug resistance.
- M. Gottesman
- Annual review of medicine
The design of cancer chemotherapy has become increasingly sophisticated, yet there is no cancer treatment that is 100% effective against disseminated cancer. Resistance to treatment with anticancer… Expand
A "Silent" Polymorphism in the MDR1 Gene Changes Substrate Specificity
Synonymous single-nucleotide polymorphisms (SNPs) do not produce altered coding sequences, and therefore they are not expected to change the function of the protein in which they occur. We report… Expand
P-glycoprotein: from genomics to mechanism
Resistance to chemically different natural product anti-cancer drugs (multidrug resistance, or MDR) results from decreased drug accumulation, resulting from expression of one or more ATP-dependent… Expand
Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues.
- Franz Thiebaut, T. Tsuruo, H. Hamada, M. Gottesman, I. Pastan, M. Willingham
- Medicine, Biology
- Proceedings of the National Academy of Sciences…
- 1 November 1987
Monoclonal antibody MRK16 was used to determine the location of P-glycoprotein, the product of the multidrug-resistance gene (MDR1), in normal human tissues. The protein was found to be concentrated… Expand
A synonymous polymorphism in a common MDR1 (ABCB1) haplotype shapes protein function.
The MDR1 (ABCB1) gene encodes a membrane-bound transporter that actively effluxes a wide range of compounds from cells. The overexpression of MDR1 by multidrug-resistant cancer cells is a serious… Expand
Isolation and genetic characterization of human KB cell lines resistant to multiple drugs
- S. Akiyama, A. Fojo, J. Hanover, I. Pastan, M. Gottesman
- Biology, Medicine
- Somatic cell and molecular genetics
- 1 March 1985
Human KB cell lines resistant to high levels of colchicine were isolated by several successive single-step selections. Most of these selection steps resulted in cross-resistance to vincristine,… Expand