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

Mire Zloh, G.W. Kaatz, S. Gibbons

Research output: Contribution to journalArticlepeer-review

36 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)881-885
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
Publication statusPublished - 23 Feb 2004


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