TABLE 1

Selected substrates for recombinant human MRP2 and MRP3 assayed in vesicles

KmReference(s)
μM
MRP2
 Bisglucuronosyl bilirubin0.7Kamisako et al., 1999
 Monoglucuronosyl bilirubin0.9Kamisako et al., 1999
 Leukotriene C41.8Cui et al.,1999
 S-Glutathionyl 2,4-dinitrobenzene6.5Evers et al., 1998
 17β-Glucuronosyl estradiol7.2Cui et al.,1999
 Cholyl-l-lysyl fluorescein3.3De Waart et al., 2010
 Fluo-33.7Nies et al., 1998; Cui et al., 2001a
 Bromosulfophthalein12Cui et al., 2001a
MRP3
 Bisglucuronosyl bilirubin++Lee et al., 2004
 Monoglucuronosyl bilirubin++Lee et al., 2004
 17β-Glucuronosyl estradiol26Zeng et al., 2000
 Dehydroepiandrosterone 3-sulfate46Lee et al., 2004
 Leukotriene C45.3Zeng et al., 2000
  • ++, Substrate property proven, but no Km determined.