Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2 by the mycotoxin fumitremorgin C

European Journal of Pharmacology
Lucía González-LobatoGracia Merino

Abstract

Breast Cancer Resistance Protein (ABCG2/BCRP) is an ATP-binding cassette transporter expressed in absorptive and excretory organs whose main physiological role is protection of cells against xenobiotics. In addition, ABCG2/BCRP expression has been linked to cellular resistance to anticancer drugs due to the acquisition of a multidrug resistance phenotype. Fumitremorgin C (FTC) is a mycotoxin described as a potent ABCG2/BCRP inhibitor that reverses multidrug resistance. However, little is known about its species-specificity. This issue is scientifically relevant since FTC is widely used to evaluate the in vitro role of BCRP. We compared the FTC-mediated inhibition of human BCRP and its murine orthologue, overexpressed in two independent cell lines, MDCKII and MEF3.8 transduced cell lines. Accumulation experiments, using mitoxantrone and chlorine e6 as substrates, revealed that although FTC inhibits both Bcrp1 and BCRP, the human transporter is more potently inhibited, resulting in significantly lower IC(50) values. Transcellular transport of known Bcrp1/BCRP substrates, such as nitrofurantoin and mitoxantrone, was completely inhibited by FTC 1muM in human BCRP-transduced cells but only moderately in murine Bcrp1-transduced cells...Continue Reading

References

May 21, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Phillip M GerkPatrick J McNamara
Feb 20, 2004·Cancer Research·Robert W RobeySusan E Bates
Feb 3, 2005·Cancer Biology & Therapy·Robert W RobeySusan E Bates
Aug 12, 2005·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Mitchell E TaubIliana Almeida
Oct 26, 2005·Pharmaceutical Research·Yi ZhangQingcheng Mao
Jan 26, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Gracia MerinoJulio G Prieto
Aug 8, 2006·Journal of Pharmaceutical Sciences·Miki KatohTsuyoshi Yokoi
Jan 9, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Christian ZimmermannAlfred H Schinkel
Jul 22, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Meng LiYurong Lai
Aug 7, 2008·Pharmacogenomics·George Cusatis, Alex Sparreboom
Sep 20, 2008·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Martina CeckovaFrantisek Staud
Oct 7, 2008·European Journal of Pharmacology·Francesca RiversRichard Callaghan
Dec 6, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Nagdeep GiriWilliam F Elmquist
Dec 30, 2008·Advanced Drug Delivery Reviews·Kohji NoguchiYoshikazu Sugimoto
Jan 3, 2009·Advanced Drug Delivery Reviews·Maria L H VlamingAlfred H Schinkel
Mar 4, 2009·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·M-K ChoiC-K Shim
May 22, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Stefanie HauswaldThomas Licht
May 30, 2009·Lung Cancer : Journal of the International Association for the Study of Lung Cancer·Jitsuo UsudaNorihiko Ikeda
Sep 29, 2009·International Journal of Pharmaceutics·Durga Kalyani PaturiAshim K Mitra

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Citations

Feb 20, 2013·Clinical Pharmacokinetics·Frederik E StuurmanJan H M Schellens
Sep 3, 2013·Assay and Drug Development Technologies·Christophe AntczakHakim Djaballah
Dec 17, 2011·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Jakub HofmanFrantisek Staud
Dec 8, 2011·Molecular Nutrition & Food Research·Dennis MulacHans-Ulrich Humpf
Feb 20, 2016·Molecular Pharmacology·Shannon DallasNico Scheer
Jul 12, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Solida LongMadalena M M Pinto
Jun 12, 2018·Expert Opinion on Drug Metabolism & Toxicology·Petar D PetrovRamiro Jover
Dec 29, 2020·Journal of Neuroscience Research·Luis Exequiel IbarraLaura Natalia Milla Sanabria
Jul 10, 2013·Molecular Pharmaceutics·Anne Sophie GrandvuinetBente Steffansen
Aug 14, 2021·Journal of Evidence-based Medicine·Jing-Quan WangZhe-Sheng Chen
Aug 17, 2021·Beilstein Journal of Organic Chemistry·Jana M BoysenFalk Hillmann

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