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
Jun 14, 2001·British Journal of Haematology·C H KaoS P Changlai
Jan 25, 2003·European Journal of Biochemistry·Chatchanok LoetchutinatArlette Garnier-Suillerot
Mar 31, 2001·Cancer Biotherapy & Radiopharmaceuticals·X F LiN Tonami
Nov 25, 2003·Cancer Biotherapy & Radiopharmaceuticals·Delphine DenoyerFrancis Dubois
Sep 30, 2004·Cancer Biotherapy & Radiopharmaceuticals·Nathalie Le JeuneFrancis Dubois
Apr 5, 2013·Journal of Biomedical Research·Xiangting ChaiHai Wang
Aug 27, 2005·Dento Maxillo Facial Radiology·T SatoK Sugihara
Mar 15, 2001·European Journal of Biochemistry·F FrézardA Garnier-Suillerot
Mar 13, 2014·Nuclear Medicine and Biology·Masato KobayashiKeiichi Kawai
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
Sep 6, 2006·The Journal of Medical Investigation : JMI·Katsuzo KunishioYoshihiro Nishiyama
Sep 6, 2003·The Journal of Pharmacy and Pharmacology·Zhi LiuXiao Yu Wu
Jan 24, 2017·European Journal of Medicinal Chemistry·Elisabetta TeodoriMilena Salerno
May 30, 2006·Journal of Bioenergetics and Biomembranes·Simplice DzamitikaArlette Garnier-Suillerot
Mar 9, 2011·Dalton Transactions : an International Journal of Inorganic Chemistry·Filipa MendesIsabel Santos
Apr 28, 2004·World Journal of Gastroenterology : WJG·Hai WangFa-Zu Qiu
Jun 16, 2001·International Journal of Cancer. Journal International Du Cancer·C H KaoS P Changlai
Oct 5, 2016·Oncology Letters·Jian YangQi Song
Jan 15, 2009·Journal of Medicinal Chemistry·Cecilia MartelliElisabetta Teodori
Jul 27, 1999·Chemico-biological Interactions·S MankhetkornA Garnier-Suillerot
Jan 29, 2010·Journal of Medicinal Chemistry·Cecilia MartelliElisabetta Teodori