Identification of a domain in rOCT2 that is responsible for higher affinity for corticosterone of
rOCT2 versus rOCT1. a, schematic representation of polypeptide regions that were replaced by
the respective domains of rOCT2 to rOCT1 (N, 1–20; 1, 21–42; eL, 43–149; 2, 150–173; 3, 174–
198; 4, 199–238; 5, 239–264; 6, 265–283; iL, 284–347; 7, 348–377; 8, 378–403; 9, 404–426; 10, 427–
463; 11, 464–487; 12, 488–516; and C, 517–556). b, uptake rates of 10 μM[14C]TEA in oocytes
expressing rOCT1 or rOCT1 with inserted domains of rOCT2. c, apparent Km values measured
for TEA uptake by rOCT1, by rOCT1 with inserted domains of rOCT2, and by rOCT2. d, inhibition
of TEA uptake by 4 μM corticosterone.
Valentin Gorboulev et al. Mol Pharmacol 2005;67:1612-1619
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