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Transport proteins in drug resistance: biology and approaches to circumvention
Author(s) -
TWENTYMAN P.R.
Publication year - 1997
Publication title -
journal of internal medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.625
H-Index - 160
eISSN - 1365-2796
pISSN - 0954-6820
DOI - 10.1111/joim.1997.242.s740.133
Subject(s) - p glycoprotein , efflux , atp binding cassette transporter , intracellular , drug resistance , drug , multiple drug resistance , glutathione , pharmacology , transporter , multidrug resistance associated proteins , transport protein , mechanism of action , drug action , medicine , membrane protein , biology , microbiology and biotechnology , membrane , biochemistry , gene , in vitro , genetics , enzyme
At least two transport proteins, P‐glycoprotein (Pgp) and the multidrug resistance associated protein (MRP), are believed to play a significant role in clinical resistance to cytotoxic therapy. These proteins are expressed at relatively high levels in a number of malignant diseases including various types of leukaemias. They are variably expressed on both the plasma membrane and intracellular vesicular membranes resulting in cellular drug efflux or vesicular drug sequestration, respectively. The action of MRP as a drug transporter depends on intracellular levels of glutathione. A number of strategies for circumvention of these drug resistance mechanisms have been developed and some of these are now in clinical trial. [Note: In this paper, references are used to direct the reader to recent reviews rather than acknowledging the original work of very many authors.]