TABLE 15

In vitro characterization of genetic polymorphisms in BCRP

In vitro function was assessed using prototypical substrates BCRP (mitoxantrone, estrone-3-sulfate, dehydroepiandrosterone). Nucleotide position was confirmed by PharmGKB (Hewett et al., 2002). Data are from Honjo et al. (2002); Kondo et al. (2004); Mizuarai et al. (2004); Morisaki et al. (2005); Vethanayagam et al. (2005); Tamura et al., 2006a,b, 2007b).

Nucleotide ChangeAmino Acid ChangeIn Vitro FunctionProtein Expression/Localization
ABCG2BCRP
    G34A    V12M↔Normal/intracellular
    C376T    Gln126STOPN.D.Absent
    C421A    Q141K↓Normal/reduced
    G445C    A149P↔Normal
    G448A    R163K↔Normal
    C496G    Q166E↔Normal/reduced
    A616C    I206L↓↔Normal
    T623C    F208SN.D.Reduced
    T742C    S248PN.D.Normal
    C805T    P269S↓↔Normal
    T1291C    F431L↓Normal/reduced
    G1322A    S441N↓Reduced
    T1465C    F489L↓↔Normal/reduced
    A1768T    N590Y↓↔Increased
    G1858A    D620N↓↔Normal

  • ↓, reduced function; ↔, no change in function; N.D. not determined.