ABCB1 p.Tyr307Arg
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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."
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Sentence
Comment
164
By contrast, the Y307R mutation inhibited rescue with both tariquidar and cyclosporine A.
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ABCB1 p.Tyr307Arg 26507655:164:17
status: NEW167 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.Tyr307Arg 26507655:167:99
status: NEW175 In the N-terminal TMD1 domain, the largest number of arginine mutations predicted to line the drug-binding pocket that inhibited tariquidar rescue were located in TM1 (H61R, G64R, L65R, M68R, M69R, and F72R) and TM5 (F303R, I306R, Y307R, S309R, and Y310R) (Fig. 4, A and E).
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ABCB1 p.Tyr307Arg 26507655:175:231
status: NEW194 The other 12 mutants in TM1 (F72R), TM5 (Y307R and Y310R), TM6 (F336R and F343R), TM7 (F732R), TM10 (V865R), TM11 (M949R, Y950R, S952R, and Y953R), and TM12 (L975R and F978R) were not rescued by cyclosporine A (Fig. 7).
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ABCB1 p.Tyr307Arg 26507655:194:41
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.Tyr307Arg 26507655:212:80
status: NEW