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 Change	Amino Acid Change	In Vitro Function	Protein Expression/Localization
ABCG2	BCRP
G34A	V12M	↔	Normal/intracellular
C376T	Gln126STOP	N.D.	Absent
C421A	Q141K	↓	Normal/reduced
G445C	A149P	↔	Normal
G448A	R163K	↔	Normal
C496G	Q166E	↔	Normal/reduced
A616C	I206L	↓↔	Normal
T623C	F208S	N.D.	Reduced
T742C	S248P	N.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.