ABCB1 p.Val982Arg
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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.Val982Arg 22647192:333:398
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
188
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.Val982Arg 26507655:188:188
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.Val982Arg 26507655:193:335
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.Val982Arg 26507655:212:219
status: NEW