ABCB1 p.Ile868Arg
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PMID: 26507655
[PubMed]
Loo TW et al: "Mapping the Binding Site of the Inhibitor Tariquidar That Stabilizes the First Transmembrane Domain of P-glycoprotein."
No.
Sentence
Comment
167
A, whole cell SDS extracts of cells expressing P-gp processing mutant G251V, G251V/I868R, or G251V/Y307R in the presence of various concentrations of tariquidar or cyclosporine A were subjected to immunoblot analysis.
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ABCB1 p.Ile868Arg 26507655:167:83
status: NEW188 These were in TM7 (Q725R, F728R, and F732R) (Fig. 6A), TM10 (V865R, I868R, and G872R) (Fig. 6D), TM11 (F942R, T945R, Q946R, M949R, Y950R, and Y953R) (Fig. 6E), and TM12 (L975R, F978R, and V982R) (Fig. 6F).
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ABCB1 p.Ile868Arg 26507655:188:68
status: NEW193 It was found that 16 of the 28 mutants resembled the G251V/I868R mutant as expression in the presence of 5 òe;M cyclosporine A yielded mature P-gp as the major product in TM1 (H61R, G64R, L65R, M68R, and M69R), TM5 (F303R, I306R, and S309R), TM7 (Q725R and F728R), TM10 (I868R and G872R), TM11 (F942R, T945R, and Q946R), and TM12 (V982R) (Fig. 7).
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ABCB1 p.Ile868Arg 26507655:193:59
status: NEWX
ABCB1 p.Ile868Arg 26507655:193:275
status: NEW212 Seventeen of the 30 G251V/arginine mutants (M68R, M69R, and F72R in TM1; I306R, Y307R, S309R, and Y310R in TM5; F336R in TM6; F728R and F732R in TM7; I868R and G872R in TM10; F942R, T945R, M949R, and S952R in TM11; and V982R in TM12) that could not be rescued with tariquidar showed little or no stimulation of ATPase activity with tariquidar (Fig. 8A).
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ABCB1 p.Ile868Arg 26507655:212:150
status: NEW