ABCB1 p.Phe336Arg
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PMID: 22647192
[PubMed]
Wise JG et al: "Catalytic transitions in the human MDR1 P-glycoprotein drug binding sites."
No.
Sentence
Comment
333
A novel arginine mutagenesis approach for rescuing Pgp folding mutants was used by Loo and Clarke to argue that the bulky arginine side chain, when present in the drug binding site, mimicked the rescue of folding of certain mutations by transport substrates that has been observed.81 Alteration of known substrate affinities was taken as evidence that the A302R, F336R, L339R, G872R, F942R, Q946R, V982R, S993R, and M986R mutations were at drug binding locations.
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ABCB1 p.Phe336Arg 22647192:333:363
status: NEW
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
176
One arginine mutation predicted to line the drug-binding pocket inhibited rescue in TM2 (A129R) (Fig. 4B) and two arginines predicted to line the drug-binding pocket in TM6 (F336R and F343R) were FIGURE 4.
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ABCB1 p.Phe336Arg 26507655:176:174
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.Phe336Arg 26507655:194:64
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.Phe336Arg 26507655:212:112
status: NEW