Abstract
Multidrug resistance is one of the main obstacles in the chemotherapy of cancer. Its inhibition by combination of chemosensitizers with antitumor compounds is a very active field of research, since safe and potent reversal agents would be beneficial for clinical use. Most modulators act by binding to membrane transport proteins (specially P-gp and MRP) and inhibiting their drug-effluxing activity, or by indirect mechanisms related to phosphorylation of the transport proteins or expression of the mdr1 and mrp1 genes. The main body of the review focuses on the study of the known MDR modulators, which are classified according to their chemical structures. General structure-activity studies of this therapeutic group are hampered by the very heterogeneous chemical structure of the compounds, although some conclusions have been drawn from the study of homogeneous series of molecules.
Keywords: Multidrug Resistance, Antitumor Agents, P-gp, topoisomerase II, Doxorubicin, Daunorub icin, Vincristine, Vinblastine, Colchicine, P acli ta xel
Current Medicinal Chemistry
Title: Inhibitors of Multidrug Resistance to Antitumor Agents (MDR)
Volume: 9 Issue: 2
Author(s): Carmen Avendano and J. Carlos Menendez
Affiliation:
Keywords: Multidrug Resistance, Antitumor Agents, P-gp, topoisomerase II, Doxorubicin, Daunorub icin, Vincristine, Vinblastine, Colchicine, P acli ta xel
Abstract: Multidrug resistance is one of the main obstacles in the chemotherapy of cancer. Its inhibition by combination of chemosensitizers with antitumor compounds is a very active field of research, since safe and potent reversal agents would be beneficial for clinical use. Most modulators act by binding to membrane transport proteins (specially P-gp and MRP) and inhibiting their drug-effluxing activity, or by indirect mechanisms related to phosphorylation of the transport proteins or expression of the mdr1 and mrp1 genes. The main body of the review focuses on the study of the known MDR modulators, which are classified according to their chemical structures. General structure-activity studies of this therapeutic group are hampered by the very heterogeneous chemical structure of the compounds, although some conclusions have been drawn from the study of homogeneous series of molecules.
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Cite this article as:
Avendano Carmen and Menendez Carlos J., Inhibitors of Multidrug Resistance to Antitumor Agents (MDR), Current Medicinal Chemistry 2002; 9 (2) . https://dx.doi.org/10.2174/0929867023371175
DOI https://dx.doi.org/10.2174/0929867023371175 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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