PMID: 9523723Apr 2, 1998Paper

Comparison of the kinetics of active efflux of 99mTc-MIBI in cells with P-glycoprotein-mediated and multidrug-resistance protein-associated multidrug-resistance phenotypes

European Journal of Biochemistry
J VergoteA Garnier-Suillerot

Abstract

The overexpression of two membrane glycoproteins, P-glycoprotein and multidrug-resistance protein (MRP1) is a major cause of resistance to chemotherapeutic agents in the treatment of human cancers. Both proteins confer a similar multidrug-resistant (MDR) phenotype. 99mTc-MIBI, a myocardial imaging agent, which is also useful for the detection of a variety of tumours, has been shown to be a substrate for P-glycoprotein and MRP1. It thus may provide additional information about the P-glycoprotein and MRP1 status of tumour cells. In order to obtain information on the substrate specificity of these proteins, we have studied the transport kinetics of Tc-MIBI in two cell lines, K562/ADR and GLC4/ADR, which overexpress P-glycoprotein and MRP1, respectively. The mean active efflux coefficient ka, which is proportional to the ratio of maximal efflux rate VM to the apparent Michaelis-Menten constant Km, used to characterise the efficiency of the active efflux, was very similar being 1.9 +/- 0.6 x 10(-11) s(-1) x cells x ml and 1.3 +/- 0.5 x 10(-11) s(-1) x cells x ml for drug-resistant K562 and GLC4, respectively. These values are 50-100-times lower than for daunorubicin and other anthracycline derivatives, strongly suggesting that the e...Continue Reading

Citations

Jun 16, 2004·Annals of Nuclear Medicine·Mitsutaka Fukumoto
Mar 24, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Teréz MáriánZoltán Krasznai
Feb 28, 2001·European Journal of Pharmacology·K Tkaczyk-GobisA Garnier-Suillerot
Jul 2, 2003·Journal of Biochemical and Biophysical Methods·Paiboon ReungpatthanaphongSamlee Mankhetkorn
Jun 9, 1997·Journal of Biochemical and Biophysical Methods·R GravesG O'Beirne
Jan 25, 2003·European Journal of Biochemistry·Chatchanok LoetchutinatArlette Garnier-Suillerot
Apr 5, 2013·Journal of Biomedical Research·Xiangting ChaiHai Wang
Mar 15, 2001·European Journal of Biochemistry·F FrézardA Garnier-Suillerot
Feb 13, 2007·The Breast : Official Journal of the European Society of Mastology·Laura Lavinia TravainiGiovanni Paganelli
Jun 17, 2015·Medical Science Monitor : International Medical Journal of Experimental and Clinical Research·Luis Mauricio Hurtado-LópezNorma Estela Herrera González
Jan 24, 2017·European Journal of Medicinal Chemistry·Elisabetta TeodoriMilena Salerno
Mar 9, 2011·Dalton Transactions : an International Journal of Inorganic Chemistry·Filipa MendesIsabel Santos

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