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        Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates

        Author
        Zloh, Mire
        Kaatz, G.W.
        Gibbons, S.
        Attention
        2299/10924
        Abstract
        Multidrug-resistance (MDR) occurs in many bacterial species and tumour cells. MDR functions by membrane proteins which export drugs from cells, resulting in a low ineffective concentration of the drug. We have shown by molecular modelling that inhibitors of MDR have affinity for substrates of MDR transporters. This affinity may facilitate drug entry into cells and a large inhibitor-drug complex may be a poorer substrate for the MDR mechanism. This complex would effectively 'cloak' the drug rendering it unavailable for efflux.
        Publication date
        2004-02-23
        Published in
        Bioorganic and Medicinal Chemistry Letters
        Published version
        https://doi.org/10.1016/j.bmcl.2003.12.015
        Other links
        http://hdl.handle.net/2299/10924
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