ArticleAnnals of the rheumatic diseases2004
Development of sulfasalazine resistance in human T cells induces expression of the multidrug resistance transporter ABCG2 (BCRP) and augmented production of TNFalpha.
Article in Annals of the rheumatic diseases, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21 citing papers in PubMed, 78 citations in OpenAlex.
- ATP-Binding Cassette Subfamily G Member 2 in Acute Myeloid Leukemia: A New Molecular Target?Biomedicines · 2024Review
- Toward Overcoming Treatment Failure in Rheumatoid Arthritis.Frontiers in immunology · 2021Review
- Beta1 integrin blockade overcomes doxorubicin resistance in human T-cell acute lymphoblastic leukemia.Cell death & disease · 2019Article
- Rheumatoid Arthritis Disease Activity Is Determinant for ABCB1 and ABCG2 Drug-Efflux Transporters Function.PloS one · 2016Article
- Novel understanding of ABC transporters ABCB1/MDR/P-glycoprotein, ABCC2/MRP2, and ABCG2/BCRP in colorectal pathophysiology.World journal of gastroenterology · 2015Article
- Role of the breast cancer resistance protein (BCRP/ABCG2) in drug transport--an update.The AAPS journal · 2015Review
- Targeting the Achilles heel of multidrug-resistant cancer by exploiting the fitness cost of resistance.Chemical reviews · 2014Review
- Inhibition of human MDR1 and BCRP transporter ATPase activity by organochlorine and pyrethroid insecticides.Journal of biochemical and molecular toxicology · 2013Article
- Collagen/β1 integrin signaling up-regulates the ABCC1/MRP-1 transporter in an ERK/MAPK-dependent manner.Molecular biology of the cell · 2012Article
- Breast cancer resistance protein (BCRP/ABCG2): its role in multidrug resistance and regulation of its gene expression.Chinese journal of cancer · 2012Review
- The challenge of exploiting ABCG2 in the clinic.Current pharmaceutical biotechnology · 2011Review
- Chemotherapeutic drug-induced ABCG2 promoter demethylation as a novel mechanism of acquired multidrug resistance.Neoplasia (New York, N.Y.) · 2009Article
- Interleukin-1 beta and tumor necrosis factor-alpha increase ABCG2 expression in MCF-7 breast carcinoma cell line and its mitoxantrone-resistant derivative, MCF-7/MX.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2009Article
- Expression of multidrug resistance-1 protein correlates with disease activity rather than the refractoriness to methotrexate therapy in rheumatoid arthritis.Clinical rheumatology · 2009Article
- Breast cancer resistance protein (ABCG2) and drug disposition: intestinal expression, polymorphisms and sulfasalazine as an in vivo probe.Pharmacogenetics and genomics · 2008Article
- Sulfasalazine sensitises human monocytic/macrophage cells for glucocorticoids by upregulation of glucocorticoid receptor alpha and glucocorticoid induced apoptosis.Annals of the rheumatic diseases · 2007Article
- Modulation of the cellular accumulation and intracellular activity of daptomycin towards phagocytized Staphylococcus aureus by the P-glycoprotein (MDR1) efflux transporter in human THP-1 macrophages and madin-darby canine kidney cells.Antimicrobial agents and chemotherapy · 2007Article
- Evidence for differential acquired drug resistance to anti-tumour necrosis factor agents in rheumatoid arthritis.Annals of the rheumatic diseases · 2006Article
- Multidrug transporter activity in lymphocytes.British journal of pharmacology · 2004Article
- Acquired resistance of human T cells to sulfasalazine: stability of the resistant phenotype and sensitivity to non-related DMARDs.Annals of the rheumatic diseases · 2004Article
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10 authors at 1 institution in 1 country.
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Abstract
objectiveTo determine whether overexpression of cell membrane associated drug efflux pumps belonging to the family of ATP binding cassette (ABC) proteins contributes to a diminished efficacy of sulfasalazine (SSZ) after prolonged cellular exposure to this disease modifying antirheumatic drug (DMARD).
methodsA model system of human T cells (CEM) was used to expose cells in vitro to increasing concentrations of SSZ for a period of six months. Cells were then characterised for the expression of drug efflux pumps: P-glycoprotein (Pgp, ABCB1), multidrug resistance protein 1 (MRP1, ABCC1), and breast cancer resistance protein (BCRP, ABCG2).
resultsProlonged exposure of CEM cells to SSZ provoked resistance to SSZ as manifested by a 6.4-fold diminished antiproliferative effect of SSZ compared with parental CEM cells. CEM cells resistant to SSZ (CEM/SSZ) showed a marked induction of ABCG2/BCRP, Pgp expression was not detectable, while MRP1 expression was even down regulated. A functional role of ABCG2 in SSZ resistance was demonstrated by 60% reversal of SSZ resistance by the ABCG2 blocker Ko143. Release of the proinflammatory cytokine tumour necrosis factor alpha (TNFalpha) was threefold higher in CEM/SSZ cells than in CEM cells. Moreover, twofold higher concentrations of SSZ were required to inhibit TNFalpha release from CEM/SSZ cells compared with CEM cells.
conclusionCollectively, ABCG2 induction, augmented TNFalpha release, and less efficient inhibition of TNFalpha production by SSZ may contribute to diminished efficacy after prolonged exposure to SSZ. These results warrant further clinical studies to verify whether drug efflux pumps, originally identified for their roles in cytostatic drug resistance, can also be induced by SSZ or other DMARDs.
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