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

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

doi:10.1016/j.bmcl.2003.12.015

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

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

School of Life and Medical Sciences

Research output: Contribution to journal › Article › peer-review

36 Citations (Scopus)

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.

Original language	English
Pages (from-to)	881-885
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2003.12.015
Publication status	Published - 23 Feb 2004

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

Abstract

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