TABLE 12.

In vitro characterization of genetic polymorphisms in OATP1A2, -1B1, and -1B3

In vitro function was assessed using prototypical substrates for OATP1A2 (estrone-3-sulfate), OATP1B1 (estrone-3-sulfate, estradiol 17β-glucuronide, rifampin), and OATP1B3 (estrone-3-sulfate, estradiol 17β-glucuronide). Some nucleotide positions were confirmed by PharmGKB (Hewett et al., 2002). OATP1A2 data from Lee et al. (2005a) and Badagnani et al. (2006). OATP1B1 data from Tirona et al. (2001); Michalski et al. (2002); Nozawa et al. (2002); Nishizato et al. (2003); Tirona et al. (2003); Iwai et al. (2004a); Morimoto et al. (2004); Kameyama et al. (2005). OATP1B3 data from Letschert et al. (2004).

Nucleotide Change	Amino Acid Change	In Vitro Function	Protein Expression/Localization
SLCO1A2	OATP1A2
T38C	I13T	↑↔	Normal
A382T	N128Y	↔	N.D.
A404T	N135I	↓↔	N.D.
C502T	R168C	↓	N.D.
A516C	E172D	↓	Intracellular
G559A	A187T	↓	Normal
A833-	Asn278STOP	↓	N.D.
C2003G	T668S	↔	Intracellular
SLCO1B1	OATP1B1
T217C	F73L	↓	Intracellular
T245C	V82A	↓	Intracellular
A388G	N130D	↓↔	Normal
A452G	N151S	N.D.	N.D.
C463A	P155T	↔	Normal
A467G	E156G	↓	Normal
T521C	V174A	↓	Intracellular/normal
T578G	L193R	↓	Intracellular
C1007G	P336R	N.D.	N.D.
T1058C	I353T	↓	Intracellular
A1294G	N432D	↓↔	Normal
A1385G	D462G	↔	Normal
G1454T	C485F	N.D.	N.D.
G1463C	G488A	↓	Intracellular
T1628G	L543W	N.D.	N.D.
A1964G	D655G	↓↔	Normal
A2000G	E667G	↓↔	Normal
SLCO1B3	OATP1B3
T334G	S112A	↑↔	Normal
G699A	M233I	↔	Normal
G1564T	G522C	↓↔	Reduced
G1748A	G583E	↓↔	Reduced

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