PMID: 8947498Nov 15, 1996Paper

MOAT4, a novel multispecific organic-anion transporter for glucuronides and mercapturates in mouse L1210 cells and human erythrocytes

The Biochemical Journal
M Saxena, G B Henderson

Abstract

Glucuronides and mercapturates were examined as possible high-affinity substrates for a low-affinity ATP-dependent transport system for 2,4-dinitrophenyl S-glutathione (DNP-SG) in mouse L1210 cells. Initial inhibitor studies with inside-out vesicles revealed that the low-affinity transport of [3H]DNP-SG (Km 450 microM) exhibits a high sensitivity to N-acetyl 2,4-dinitrophenyl cysteine (NAc-DNP-Cys) (Ki 5.0 microM) and alpha-naphthyl beta-D-glucuronide (naphthyl glucuronide) (Ki 8.5 microM). Direct transport measurements showed the presence of ATP-dependent uptake activities for NAc-DNP-[35S]Cys and naphthyl [14C] glucuronide, and Km values for half-maximal transport were comparable to the Ki values of these compounds for inhibition of [3H]DNP-SG transport. Transport of [3H]DNP-SG, NAc-DNP-[35S]Cys and naphthyl [14C]glucuronide each showed the same sensitivity to various anions and anion conjugates. Inhibition was competitive and was most potent for bilirubin ditaurate, indoprofen, 4-biphenylacetic acid, 4-acridine 4 beta-D-glucuronide, N-acetyl leukotriene E4, 17 beta-oestradiol 3 beta-D-glucuronide and taurolithocholate 3-sulphate. Inside-out vesicles from human erythrocytes contain a comparable ATP-dependent transport system....Continue Reading

Citations

Mar 23, 2000·International Journal of Cancer. Journal International Du Cancer·T OguriM Yamakido
May 23, 2015·Frontiers in Pharmacology·Katherine BasoreSanjay A Desai
Oct 3, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Benoît CossecManuella Burgart
May 18, 1999·The Journal of Biological Chemistry·T HirohashiY Sugiyama
Oct 23, 2004·Drug Metabolism and Pharmacokinetics·Takashi MizumaMasahiro Hayashi
Mar 3, 2007·Cancer Metastasis Reviews·Yehuda G Assaraf
Jun 9, 1999·Proceedings of the National Academy of Sciences of the United States of America·M KoolP Borst
Mar 19, 2005·Journal of Bacteriology·Wei-Jun LiangRichard A Jefferson
Nov 10, 2006·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·Yehuda G Assaraf

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