ArticleBritish journal of cancer1998
Multidrug resistance protein-mediated transport of chlorambucil and melphalan conjugated to glutathione.
Article in British journal of cancer, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 91 citations in OpenAlex.
- Direct Detection of Glutathione Biosynthesis, Conjugation, Depletion and Recovery in Intact Hepatoma Cells.International journal of molecular sciences · 2022Article
- The role of photodynamic therapy on multidrug resistant breast cancer.Cancer cell international · 2019Review
- Genetic disruption of multidrug resistance-associated protein 1 improves endothelial function and attenuates atherosclerosis in MRP1Archives of medical science : AMS · 2017Article
- Nrf2 Regulates the Sensitivity of Mouse Keratinocytes to Nitrogen Mustard via Multidrug Resistance-Associated Protein 1 (Mrp1).Toxicological sciences : an official journal of the Society of Toxicology · 2016Article
- Article
- Protection of HepG2 cells against acrolein toxicity by 2-cyano-3,12-dioxooleana-1,9-dien-28-imidazolide via glutathione-mediated mechanism.Experimental biology and medicine (Maywood, N.J.) · 2015Article
- Effects of hyperglycemia on lonidamine-induced acidification and de-energization of human melanoma xenografts and sensitization to melphalan.NMR in biomedicine · 2015Article
- Multidrug resistance: Physiological principles and nanomedical solutions.Advanced drug delivery reviews · 2013Review
- Portrait of multifaceted transporter, the multidrug resistance-associated protein 1 (MRP1/ABCC1).Pflugers Archiv : European journal of physiology · 2007Review
- A fluorometric screening assay for drug efflux transporter activity in the blood-brain barrier.Pharmaceutical research · 2005Article
- Article
- Development of multidrug-resistance convertors: sense or nonsense?Investigational new drugs · 2000Review
- Differences in substrate specificity among glutathione conjugates (GS-X) pump family members: comparison between multidrug resistance-associated protein and a novel transporter expressed on a cisplatin-resistant cell line (KCP-4).Japanese journal of cancer research : Gann · 1999Article
- ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1.British journal of pharmacology · 1999Article
- Epitope mapping of monoclonal antibodies specific for the 190-kDa multidrug resistance protein (MRP).British journal of cancer · 1998Article
- The extended-MDR phenotype.Cytotechnology · 1998Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human multidrug resistance protein (MRP1) confers resistance of cells to a number of different cytostatic drugs and functions as an export pump for glutathione S-conjugates, glucuronides and other amphiphilic anions. The present study details for the first time MRP1-mediated ATP-dependent transport of various glutathione S-conjugates of the bifunctional alkylating agents chlorambucil and melphalan. In membrane vesicles prepared from cells expressing recombinant MRP1, the conjugates were transported at rates in the following order: monoglutathionyl chlorambucil > bisglutathionyl chlorambucil > monohydroxy monoglutathionyl chlorambucil and monoglutathionyl melphalan > monohydroxy monoglutathionyl melphalan. In addition, we show that membranes from chlorambucil-resistant GST-alpha-overexpressing CHO cells as well as from their parental cells express the hamster homologue of MRP1. With both CHO cell membrane preparations, we observed ATP-dependent transport of monoglutathionyl chlorambucil and of leukotriene C4, a glutathione S-conjugate and high-affinity substrate of MRP1. The transport rates measured in the resistant cells were only two- to three-fold higher than those measured in the control cells. These results together with cytotoxicity assays comparing MRP1-overexpressing cell pairs with the CHO cell pair indicate that, although MRP1-mediated transport is active, it may not be the rate-limiting step in chlorambucil resistance in these cell lines.
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