Print Email Facebook Twitter Metabolism of ATP-binding cassette drug transporter inhibitors: Complicating factor for multidrug resistance. Title Metabolism of ATP-binding cassette drug transporter inhibitors: Complicating factor for multidrug resistance. Author Cnubben, N.H. Wortelboer, H.M. van Zanden, J.J. Rietjens, I.M. van Bladeren, P.J. TNO Kwaliteit van Leven Publication year 2005 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. Subject Health PharmacologyPhysiological SciencesABC transportercyclosporin derivativedibenzo[a,d]cycloheptene derivativeglycoprotein Pquinoline derivativevalspodarzosuquidardrug antagonismdrug designdrug effectgeneticshumanmetabolismmultidrug resistancereviewRNA interferencetransport at the cellular levelATP-Binding Cassette TransportersBiological TransportCyclosporinsDibenzocycloheptenesDrug DesignDrug Resistance, MultipleHumansP-GlycoproteinsQuinolinesRNA Interference To reference this document use: http://resolver.tudelft.nl/uuid:3e4c2a55-5dbd-4060-8396-40324ab05e79 TNO identifier 238623 ISSN 1742-5255 Source Expert opinion on drug metabolism & toxicology., 1 (2), 219-232 Document type article Files To receive the publication files, please send an e-mail request to TNO Library.