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. Author manuscript; available in PMC: 2009 Sep 2.
Published in final edited form as: Biochemistry. 2008 Aug 9;47(35):9090–9097. doi: 10.1021/bi8008455

FIGURE 6.

FIGURE 6

Sequence alignment of TM10 and uptake of CCK-8 by mutant OATP1B3. (A) Residues 528–560 of OATP1B1 and 1B3 were aligned and fourteen amino acids were identified as different between OATP1B3 and 1B1 in this domain: (1B3)N528D(1B1), T529A, F535Y, I536F, Y537F, I543L, S545L, L546F, T550L, T554S, F555H, I556V, L557M and T559I. (B) Uptake of 0.1 μM CCK-8 by OATP1B1, 1B3, fourteen OATP1B3 single point mutants, S545L/T550L double mutant and Y537F/S545L/T550L and S545L/T550L/T554S triple mutants in TM10 was measured at 37 °C for 1 min with empty vector and OATP-expressing HEK293 cells. The net uptakes were obtained by subtracting the uptake of cells transfected with empty vector from the uptake of OATP-expressing cells. Final results were obtained by normalizing net uptakes to the surface expression levels of the respective proteins. * p < 0.05 significantly different from OATP1B3.