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

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Zloh, Mire, Kaatz, Glenn W. and Gibbons, Simon (2004) Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates. Bioorganic & Medicinal Chemistry Letters, 14 (4). pp. 881-885. ISSN 0960-894X

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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. Here we show by molecular modelling that inhibitors of MDR have affinity for substrates of MDR transporters.

Item Type:	Article
Faculty \ School:	Faculty of Science > School of Pharmacy
Related URLs:	https://linkinghub.elsevier.com/retrieve...
Depositing User:	LivePure Connector
Date Deposited:	01 Jul 2020 00:00
Last Modified:	22 Oct 2022 06:24
URI:	https://ueaeprints.uea.ac.uk/id/eprint/75850
DOI:	10.1016/j.bmcl.2003.12.015

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