Human and rat ABC transporter efflux of bisphenol a and bisphenol a glucuronide: interspecies comparison and implications for pharmacokinetic assessment

Toxicological Sciences : an Official Journal of the Society of Toxicology
Christopher S MazurJeff Fisher

Abstract

Significant interspecies differences exist between human and rodent with respect to absorption, distribution, and excretion of bisphenol A (BPA) and its primary metabolite, BPA-glucuronide (BPA-G). ATP-Binding Cassette (ABC) transporter enzymes play important roles in these physiological processes, and their enzyme localization (apical vs. basolateral) in the plasma membrane allows for different cellular efflux pathways. In this study, we utilized an ATPase assay to evaluate BPA and BPA-G as potential substrates for the human and rat ABC transporters: P-glycoprotein (MDR1), multidrug resistance-associated proteins (MRPs), and breast cancer-resistant protein (BCRP). Based on high ATPase activity, BPA is likely a substrate for rat mdr1b but not for human MDR1 or rat mdr1a. Results indicate that BPA is a potential substrate for rat mrp2 and human MRP2, BCRP, and MRP3. The metabolite BPA-G demonstrated the highest apparent substrate binding affinity for rat mrp2 and human MRP3 but appeared to be a nonsubstrate or potential inhibitor for human MRP2, MDR1, and BCRP and for rat mdr1a, mdr1b, and bcrp. Analysis of ABC transporter amino acid sequences revealed key differences in putative binding site composition that may explain substra...Continue Reading

References

Aug 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·P GrosF Talbot
Apr 4, 2000·Toxicological Sciences : an Official Journal of the Society of Toxicology·L H PottengerJ M Waechter
Aug 31, 2000·Journal of Molecular Biology·C NotredameJ Heringa
Jun 21, 2002·Toxicological Sciences : an Official Journal of the Society of Toxicology·Hideo KurebayashiYasuo Ohno
Oct 19, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·J J PritchettI G Sipes
Oct 22, 2002·Chemical Research in Toxicology·Wolfgang VölkelWolfgang Dekant
Dec 18, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Hiroki InoueSeiyu Kato
Mar 5, 2005·Toxicological Sciences : an Official Journal of the Society of Toxicology·Justin G TeeguardenHugh A Barton
Apr 23, 2005·Toxicology and Applied Pharmacology·Elaine M LeslieSusan P C Cole
Nov 25, 2005·Current Drug Delivery·Hristos GlavinasBalázs Sarkadi
Jul 25, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·R K Kuester, I G Sipes
Oct 31, 2007·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S OswaldH K Kroemer
Nov 7, 2009·Molecular Pharmaceutics·K Sandy PangJianghong Fan
Mar 2, 2010·Nature Reviews. Drug Discovery·UNKNOWN International Transporter ConsortiumLei Zhang
Mar 11, 2010·Reproductive Toxicology·Thit J MørckLisbeth E Knudsen
Jul 8, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Caroline Prouillac, Sylvaine Lecoeur
Jul 27, 2010·Toxicology and Applied Pharmacology·Daniel R DoergeJeffrey W Fisher
Aug 26, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Christopher S MazurJohn C Lipscomb
Jun 29, 2011·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Maciej J Zamek-GliszczynskiDiane L Phillips
Aug 9, 2011·Toxicology and Applied Pharmacology·Daniel R DoergeJeffrey W Fisher

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Citations

Sep 10, 2013·Toxicological Sciences : an Official Journal of the Society of Toxicology·Anita C A DankersRosalinde Masereeuw
Nov 8, 2015·Human Reproduction Update·E BloiseS G Matthews
Dec 30, 2015·Toxicology and Applied Pharmacology·Emine B YalcinRoberta King
Nov 3, 2015·Toxicology and Applied Pharmacology·Xiaoxia YangJeffrey W Fisher
Feb 20, 2016·Molecular Pharmacology·Shannon DallasNico Scheer
Apr 4, 2016·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Justin G TeeguardenDaniel R Doerge
Jun 20, 2014·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Sabrina Nickel, Anne Mahringer
May 13, 2015·The American Journal of Pathology·Phetcharawan LyeStephen G Matthews
May 6, 2014·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Ludovic PeyreRoger Rahmani
Jan 27, 2015·Frontiers in Pharmacology·Xiaoxia Yang, Jeffrey W Fisher
Feb 7, 2016·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jamie E MoscovitzLauren M Aleksunes
May 29, 2016·The Journal of Pharmacology and Experimental Therapeutics·Anika L DzierlengaNathan J Cherrington
Nov 24, 2016·Journal of Biochemical and Molecular Toxicology·Yixin LinLauren M Aleksunes
Mar 8, 2017·Drug Metabolism Reviews·Guangyi YangMing Hu
Apr 25, 2018·Journal of Cellular and Molecular Medicine·Phetcharawan LyeStephen G Matthews
May 29, 2015·Environmental Health Perspectives·Jonathan G BoucherElla Atlas
Mar 11, 2018·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Nico HolmstockPieter Annaert
Feb 11, 2014·Current Protocols in Pharmacology·Alan M Palmer, Mohammad S Alavijeh
Jun 17, 2020·Environmental Health : a Global Access Science Source·Richelle D BjörvangCarl-Gustaf Bornehag
Dec 30, 2016·Toxicological Sciences : an Official Journal of the Society of Toxicology·Satori A MarchittiJohn F Kenneke
Nov 23, 2020·FEBS Letters·Sascha C T Nicklisch, Amro Hamdoun
Oct 2, 2017·The Science of the Total Environment·Cory L StropeJohn F Wambaugh

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