Metabolism of ATP-binding cassette drug transporter inhibitors: complicating factor for multidrug resistance

N.H.P. Cnubben, H.M. Wortelboer, J.J. van Zanden, I.M.C.M. Rietjens, P.J. van Bladeren

Research output: Contribution to journalArticleAcademicpeer-review

14 Citations (Scopus)

Abstract

Membrane transport proteins belonging to the ATP-binding cassette (ABC) family of transport proteins play a central role in the defence of organisms against toxic compounds, including anticancer drugs. However, for compounds that are designed to display a toxic effect, this defence system diminishes their effectiveness. This is typically the case in the development of cellular resistance to anticancer drugs. Inhibitors of these transporters are thus potentially useful tools to reverse this transporter-mediated cellular resistance to anticancer drugs and, eventually, to enhance the effectiveness of the treatment of patients with drug-resistant cancer. This review highlights the various types of inhibitors of several multidrug resistance-related ABC proteins, and demonstrates that the metabolism of inhibitors, as illustrated by recent data obtained for various natural compound inhibitors, may have considerable implications for their effect on drug transport and their potential for treatment of drug resistance.
Original languageEnglish
Pages (from-to)219-232
Number of pages14
JournalExpert Opinion on Drug Metabolism and Toxicology
Volume1
Issue number2
DOIs
Publication statusPublished - 2005

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